Correction to: Transdermal Permeation of Caffeine Aided by Ionic Liquids: Potential for Enhanced Treatment of Cellulites
AAPS PharmSciTech. 2021 Apr 28;22(4):144. doi: 10.1208/s12249-021-02015-9.NO ABSTRACTPMID:33945009 | DOI:10.1208/s12249-021-02015-9 (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - May 4, 2021 Category: Drugs & Pharmacology Authors: Audrey N Hernandes Rodrigo Boscariol Victor M Balc ão Marta M D C Vila Source Type: research

Formulation, Pharmacokinetics evaluation, and IVIVC Assessment of Gliclazide Multiparticulates in Rat Model
AAPS PharmSciTech. 2021 Apr 30;22(4):146. doi: 10.1208/s12249-021-02008-8.ABSTRACTIn vitro and in vivo studies of gliclazide (GLZ)-loaded freeze-dried alginate-gelatin (AL-GL) beads were carried out, aiming to modify its oral bioavailability. Crosslinked freeze-dried GLZ AL-GL beads (particle size: 1.5- and 3.0-mm) were prepared. In vitro evaluation of GLZ AL-GL beads included SEM, DSC, FT-IR, and release rate study in gradient media. In vivo study was single-dose (4 mg/kg), randomized, parallel-group design, two-treatment (T: test GLZ AL-GL beads and R: reference product Diamicron® 30-mg MR tablet) conducted in 96 hea...
Source: AAPS PharmSciTech - April 30, 2021 Category: Drugs & Pharmacology Authors: Ahmed A El-Ashmawy Aya R Abdou Nesrin F Taha Ebtesam W Elsayed Khaled M Mahmoud Laila H Emara Source Type: research

Formulation, Pharmacokinetics evaluation, and IVIVC Assessment of Gliclazide Multiparticulates in Rat Model
AAPS PharmSciTech. 2021 Apr 30;22(4):146. doi: 10.1208/s12249-021-02008-8.ABSTRACTIn vitro and in vivo studies of gliclazide (GLZ)-loaded freeze-dried alginate-gelatin (AL-GL) beads were carried out, aiming to modify its oral bioavailability. Crosslinked freeze-dried GLZ AL-GL beads (particle size: 1.5- and 3.0-mm) were prepared. In vitro evaluation of GLZ AL-GL beads included SEM, DSC, FT-IR, and release rate study in gradient media. In vivo study was single-dose (4 mg/kg), randomized, parallel-group design, two-treatment (T: test GLZ AL-GL beads and R: reference product Diamicron® 30-mg MR tablet) conducted in 96 hea...
Source: AAPS PharmSciTech - April 30, 2021 Category: Drugs & Pharmacology Authors: Ahmed A El-Ashmawy Aya R Abdou Nesrin F Taha Ebtesam W Elsayed Khaled M Mahmoud Laila H Emara Source Type: research

Formulation, Pharmacokinetics evaluation, and IVIVC Assessment of Gliclazide Multiparticulates in Rat Model
AAPS PharmSciTech. 2021 Apr 30;22(4):146. doi: 10.1208/s12249-021-02008-8.ABSTRACTIn vitro and in vivo studies of gliclazide (GLZ)-loaded freeze-dried alginate-gelatin (AL-GL) beads were carried out, aiming to modify its oral bioavailability. Crosslinked freeze-dried GLZ AL-GL beads (particle size: 1.5- and 3.0-mm) were prepared. In vitro evaluation of GLZ AL-GL beads included SEM, DSC, FT-IR, and release rate study in gradient media. In vivo study was single-dose (4 mg/kg), randomized, parallel-group design, two-treatment (T: test GLZ AL-GL beads and R: reference product Diamicron® 30-mg MR tablet) conducted in 96 hea...
Source: AAPS PharmSciTech - April 30, 2021 Category: Drugs & Pharmacology Authors: Ahmed A El-Ashmawy Aya R Abdou Nesrin F Taha Ebtesam W Elsayed Khaled M Mahmoud Laila H Emara Source Type: research

Borneol: a Promising Monoterpenoid in Enhancing Drug Delivery Across Various Physiological Barriers
AAPS PharmSciTech. 2021 Apr 28;22(4):145. doi: 10.1208/s12249-021-01999-8.ABSTRACTIncorporation of permeation enhancers is one of the most widely employed approaches for delivering drugs across biological membranes. Permeation enhancers aid in delivering drugs across various physiological barriers such as brain capillary endothelium, stratum corneum, corneal epithelium, and mucosal membranes that pose resistance to the entry of a majority of drugs. Borneol is a natural, plant-derived, lipophilic, volatile, bicyclic monoterpenoid belonging to the class of camphene. It has been used under the names "Bing Pian" or &...
Source: AAPS PharmSciTech - April 29, 2021 Category: Drugs & Pharmacology Authors: Madhur Kulkarni Niserga Sawant Anjali Kolapkar Aishwarya Huprikar Namita Desai Source Type: research

Borneol: a Promising Monoterpenoid in Enhancing Drug Delivery Across Various Physiological Barriers
AAPS PharmSciTech. 2021 Apr 28;22(4):145. doi: 10.1208/s12249-021-01999-8.ABSTRACTIncorporation of permeation enhancers is one of the most widely employed approaches for delivering drugs across biological membranes. Permeation enhancers aid in delivering drugs across various physiological barriers such as brain capillary endothelium, stratum corneum, corneal epithelium, and mucosal membranes that pose resistance to the entry of a majority of drugs. Borneol is a natural, plant-derived, lipophilic, volatile, bicyclic monoterpenoid belonging to the class of camphene. It has been used under the names "Bing Pian" or &...
Source: AAPS PharmSciTech - April 29, 2021 Category: Drugs & Pharmacology Authors: Madhur Kulkarni Niserga Sawant Anjali Kolapkar Aishwarya Huprikar Namita Desai Source Type: research

Cycle Development in a Mini-Freeze Dryer: Evaluation of Manometric Temperature Measurement in Small-Scale Equipment
The objective of this research was to assess the applicability of manometric temperature measurement (MTM) and SMART™ for cycle development and monitoring of critical product and process parameters in a mini-freeze dryer using a small set of seven vials. Freeze drying cycles were developed using SMART™ which automatically defines and adapts process parameters based on input data and MTM feedback information. The freeze drying behavior and product characteristics of an amorphous model system were studied at varying wall temperature control settings of the cylindrical wall surrounding the shelf in the mini-freeze...
Source: AAPS PharmSciTech - April 27, 2021 Category: Drugs & Pharmacology Authors: Tim Wenzel Margit Gieseler Ahmad M Abdul-Fattah Henning Gieseler Source Type: research

Cycle Development in a Mini-Freeze Dryer: Evaluation of Manometric Temperature Measurement in Small-Scale Equipment
The objective of this research was to assess the applicability of manometric temperature measurement (MTM) and SMART™ for cycle development and monitoring of critical product and process parameters in a mini-freeze dryer using a small set of seven vials. Freeze drying cycles were developed using SMART™ which automatically defines and adapts process parameters based on input data and MTM feedback information. The freeze drying behavior and product characteristics of an amorphous model system were studied at varying wall temperature control settings of the cylindrical wall surrounding the shelf in the mini-freeze...
Source: AAPS PharmSciTech - April 27, 2021 Category: Drugs & Pharmacology Authors: Tim Wenzel Margit Gieseler Ahmad M Abdul-Fattah Henning Gieseler Source Type: research

Cycle Development in a Mini-Freeze Dryer: Evaluation of Manometric Temperature Measurement in Small-Scale Equipment
The objective of this research was to assess the applicability of manometric temperature measurement (MTM) and SMART™ for cycle development and monitoring of critical product and process parameters in a mini-freeze dryer using a small set of seven vials. Freeze drying cycles were developed using SMART™ which automatically defines and adapts process parameters based on input data and MTM feedback information. The freeze drying behavior and product characteristics of an amorphous model system were studied at varying wall temperature control settings of the cylindrical wall surrounding the shelf in the mini-freeze...
Source: AAPS PharmSciTech - April 27, 2021 Category: Drugs & Pharmacology Authors: Tim Wenzel Margit Gieseler Ahmad M Abdul-Fattah Henning Gieseler Source Type: research

Development of Apremilast Solid Dispersion Using TPGS and PVPVA with Enhanced Solubility and Bioavailability
In conclusion, APST solid dispersion with TPGS and PVPVA is an alternative drug delivery system to improve the solubility and oral bioavailability of APST.PMID:33893566 | DOI:10.1208/s12249-021-02005-x (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - April 24, 2021 Category: Drugs & Pharmacology Authors: Liuhong Yang Penghui Wu Jinchao Xu Dihuan Xie Zhongqing Wang Qian Wang Yong Chen Chuan Hua Li Jiaxin Zhang Hangping Chen Guilan Quan Source Type: research

Development of Apremilast Solid Dispersion Using TPGS and PVPVA with Enhanced Solubility and Bioavailability
In conclusion, APST solid dispersion with TPGS and PVPVA is an alternative drug delivery system to improve the solubility and oral bioavailability of APST.PMID:33893566 | DOI:10.1208/s12249-021-02005-x (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - April 24, 2021 Category: Drugs & Pharmacology Authors: Liuhong Yang Penghui Wu Jinchao Xu Dihuan Xie Zhongqing Wang Qian Wang Yong Chen Chuan Hua Li Jiaxin Zhang Hangping Chen Guilan Quan Source Type: research

Development of Apremilast Solid Dispersion Using TPGS and PVPVA with Enhanced Solubility and Bioavailability
In conclusion, APST solid dispersion with TPGS and PVPVA is an alternative drug delivery system to improve the solubility and oral bioavailability of APST.PMID:33893566 | DOI:10.1208/s12249-021-02005-x (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - April 24, 2021 Category: Drugs & Pharmacology Authors: Liuhong Yang Penghui Wu Jinchao Xu Dihuan Xie Zhongqing Wang Qian Wang Yong Chen Chuan Hua Li Jiaxin Zhang Hangping Chen Guilan Quan Source Type: research

Development and Validation of a Discriminatory Dissolution Model for an Immediately Release Dosage Form by DOE and Statistical Approaches
AAPS PharmSciTech. 2021 Apr 21;22(4):140. doi: 10.1208/s12249-021-02011-z.ABSTRACTA discriminatory dissolution model was built through DOE with multivariate analysis of variance (MANOVA) and multiple linear regression (MLR) modeling to assess dissolution operational space for a highly water soluble immediate-release solid dosage drug product. The dissolution was utilized in the following five aspects: (1) understand the impact of individual variables and their interactions on dissolution performance through effect analysis; (2) explain the lack of discriminatory power of the initial dissolution condition used in early phas...
Source: AAPS PharmSciTech - April 22, 2021 Category: Drugs & Pharmacology Authors: Mingkun Fu Ellen Conroy Michael Byers Lakshminarasimhan Pranatharthiharan Thierry Bilbault Source Type: research

Comparative taste-masking evaluation of microencapsulated bitter drugs using Smartseal 30D and ReadyMix for paediatric dosage forms
AAPS PharmSciTech. 2021 Apr 21;22(4):141. doi: 10.1208/s12249-021-02002-0.ABSTRACTThe taste of drug substances plays a key role in the development of paediatric formulations with suitable organoleptic properties. The aim of the study was to evaluate the taste masking effectiveness of Smartseal 30D and ReadyMix on a range of bitter drug substances such as diphenhydramine HCl (DPD), ibuprofen lysine (IBU-LS), and phenylephrine HCl (PPH) for the development of paediatric dosage forms. The drugs were microencapsulated in the polymer carriers at 10-20% loadings using spray-drying processing. Spray drying of drug formulations wa...
Source: AAPS PharmSciTech - April 22, 2021 Category: Drugs & Pharmacology Authors: Leona Chidinma Muoka Steven A Ross Md Sadeque Hossain Mithu Uttom Nandi Dennis Douroumis Source Type: research

Development and Validation of a Discriminatory Dissolution Model for an Immediately Release Dosage Form by DOE and Statistical Approaches
AAPS PharmSciTech. 2021 Apr 21;22(4):140. doi: 10.1208/s12249-021-02011-z.ABSTRACTA discriminatory dissolution model was built through DOE with multivariate analysis of variance (MANOVA) and multiple linear regression (MLR) modeling to assess dissolution operational space for a highly water soluble immediate-release solid dosage drug product. The dissolution was utilized in the following five aspects: (1) understand the impact of individual variables and their interactions on dissolution performance through effect analysis; (2) explain the lack of discriminatory power of the initial dissolution condition used in early phas...
Source: AAPS PharmSciTech - April 22, 2021 Category: Drugs & Pharmacology Authors: Mingkun Fu Ellen Conroy Michael Byers Lakshminarasimhan Pranatharthiharan Thierry Bilbault Source Type: research

Comparative taste-masking evaluation of microencapsulated bitter drugs using Smartseal 30D and ReadyMix for paediatric dosage forms
AAPS PharmSciTech. 2021 Apr 21;22(4):141. doi: 10.1208/s12249-021-02002-0.ABSTRACTThe taste of drug substances plays a key role in the development of paediatric formulations with suitable organoleptic properties. The aim of the study was to evaluate the taste masking effectiveness of Smartseal 30D and ReadyMix on a range of bitter drug substances such as diphenhydramine HCl (DPD), ibuprofen lysine (IBU-LS), and phenylephrine HCl (PPH) for the development of paediatric dosage forms. The drugs were microencapsulated in the polymer carriers at 10-20% loadings using spray-drying processing. Spray drying of drug formulations wa...
Source: AAPS PharmSciTech - April 22, 2021 Category: Drugs & Pharmacology Authors: Leona Chidinma Muoka Steven A Ross Md Sadeque Hossain Mithu Uttom Nandi Dennis Douroumis Source Type: research

Fabrication of Three-Dimensional Bioactive Composite Scaffolds for Hemostasis and Wound Healing
AAPS PharmSciTech. 2021 Apr 20;22(4):138. doi: 10.1208/s12249-021-02010-0.ABSTRACTFabrication of 3D composite scaffolds was carried out by lyophilization of variable concentrations of collagen and chitosan gel solutions. Fibrinogen and thrombin aerosol were deposited over the surface of scaffolds to enhance hemostasis and wound healing. Composite scaffolds were characterized using differential scanning calorimetry, thermogravimetric analysis, and Fourier-transform infrared spectrophotometer to ascertain the aerosol deposition and stability. Scanning electron microscope showed multilayered porosity with pore size of ~30 &mu...
Source: AAPS PharmSciTech - April 21, 2021 Category: Drugs & Pharmacology Authors: Divya Tripathi Arpit Sharma Priyanka Tyagi Chandra Shekhar Beniwal Gaurav Mittal Abhinav Jamini Harpal Singh Amit Tyagi Source Type: research

Probing Dynamic Behavior of Chemical Enhancers Passing In and Out of the Stratum Corneum and Modulation by Biodegradable Enhancer
AAPS PharmSciTech. 2021 Apr 20;22(4):139. doi: 10.1208/s12249-021-02009-7.ABSTRACTChemical enhancers (CEs) decreased the barrier of the stratum corneum (SC) to enhance drug permeation. This was a "dynamic" behavior, which involved three processes including passing in, acting on, and passing out of the SC. However, compared with mature "static" researches about acting on the SC, the other two processes were poorly understood. This work aimed to probe the dynamic behavior of CEs and modulate it for satisfactory effectiveness. The investigating method of CEs' dynamic behavior was established to obtain the ...
Source: AAPS PharmSciTech - April 21, 2021 Category: Drugs & Pharmacology Authors: Lijuan Zeng Guangqiang Yang Jianping Liu Danyi Quan Wenting Song Source Type: research

Tumor-Targeted Delivery of Bufalin-Loaded Modified Albumin-Polymer Hybrid for Enhanced Antitumor Therapy and Attenuated Hemolysis Toxicity and Cardiotoxicity
AAPS PharmSciTech. 2021 Apr 20;22(4):137. doi: 10.1208/s12249-021-02000-2.ABSTRACTA novel albumin polymer hybrid with a core-shell structure was designed to target delivery of bufalin, which is an antineoplastic monomer with serious cardiotoxicity. The sheath layer was composed of ursodeoxycholic acid (UA)-modified bovine serum albumin (UA-BSA), while the stable core consisted of poly n-butyl cyanoacrylate (PBCA) nanoparticles. The UA-BSA was synthetized, and the substitution degree was characterized. The physical properties of bufalin-loaded UA-modified protein-PBCA nanocomplexes (BF-uPPNCs), such as morphology, particle ...
Source: AAPS PharmSciTech - April 21, 2021 Category: Drugs & Pharmacology Authors: Ying Xu Lei Tang Peng Chen Mei Chen Miaomiao Zheng Feng Shi Yanchun Wang Source Type: research

Fabrication of Three-Dimensional Bioactive Composite Scaffolds for Hemostasis and Wound Healing
AAPS PharmSciTech. 2021 Apr 20;22(4):138. doi: 10.1208/s12249-021-02010-0.ABSTRACTFabrication of 3D composite scaffolds was carried out by lyophilization of variable concentrations of collagen and chitosan gel solutions. Fibrinogen and thrombin aerosol were deposited over the surface of scaffolds to enhance hemostasis and wound healing. Composite scaffolds were characterized using differential scanning calorimetry, thermogravimetric analysis, and Fourier-transform infrared spectrophotometer to ascertain the aerosol deposition and stability. Scanning electron microscope showed multilayered porosity with pore size of ~30 &mu...
Source: AAPS PharmSciTech - April 21, 2021 Category: Drugs & Pharmacology Authors: Divya Tripathi Arpit Sharma Priyanka Tyagi Chandra Shekhar Beniwal Gaurav Mittal Abhinav Jamini Harpal Singh Amit Tyagi Source Type: research

Probing Dynamic Behavior of Chemical Enhancers Passing In and Out of the Stratum Corneum and Modulation by Biodegradable Enhancer
AAPS PharmSciTech. 2021 Apr 20;22(4):139. doi: 10.1208/s12249-021-02009-7.ABSTRACTChemical enhancers (CEs) decreased the barrier of the stratum corneum (SC) to enhance drug permeation. This was a "dynamic" behavior, which involved three processes including passing in, acting on, and passing out of the SC. However, compared with mature "static" researches about acting on the SC, the other two processes were poorly understood. This work aimed to probe the dynamic behavior of CEs and modulate it for satisfactory effectiveness. The investigating method of CEs' dynamic behavior was established to obtain the ...
Source: AAPS PharmSciTech - April 21, 2021 Category: Drugs & Pharmacology Authors: Lijuan Zeng Guangqiang Yang Jianping Liu Danyi Quan Wenting Song Source Type: research

Tumor-Targeted Delivery of Bufalin-Loaded Modified Albumin-Polymer Hybrid for Enhanced Antitumor Therapy and Attenuated Hemolysis Toxicity and Cardiotoxicity
AAPS PharmSciTech. 2021 Apr 20;22(4):137. doi: 10.1208/s12249-021-02000-2.ABSTRACTA novel albumin polymer hybrid with a core-shell structure was designed to target delivery of bufalin, which is an antineoplastic monomer with serious cardiotoxicity. The sheath layer was composed of ursodeoxycholic acid (UA)-modified bovine serum albumin (UA-BSA), while the stable core consisted of poly n-butyl cyanoacrylate (PBCA) nanoparticles. The UA-BSA was synthetized, and the substitution degree was characterized. The physical properties of bufalin-loaded UA-modified protein-PBCA nanocomplexes (BF-uPPNCs), such as morphology, particle ...
Source: AAPS PharmSciTech - April 21, 2021 Category: Drugs & Pharmacology Authors: Ying Xu Lei Tang Peng Chen Mei Chen Miaomiao Zheng Feng Shi Yanchun Wang Source Type: research

Performance of Low Air Volume Dry Powder Inhalers (LV-DPI) when Aerosolizing Excipient Enhanced Growth (EEG) Surfactant Powder Formulations
This study aims to develop an efficient dry powder inhaler (DPI) capable of delivering spray-dried Survanta-EEG powders (3-10 mg) with a low volume (3 mL) of dispersion air. A series of iterative design modifications were made to a base low air volume actuated DPI. The modifications included the replacement of the original capsule chamber with an integral dose containment chamber, alteration of the entrainment air flow path through the device (from single-sided (SS) to straight through (ST)), change in the number of air inlet holes (from one to three), varying the outlet delivery tube length (45, 55, and 90 mm) and interna...
Source: AAPS PharmSciTech - April 16, 2021 Category: Drugs & Pharmacology Authors: Susan Boc Mohammad A M Momin Dale R Farkas Worth Longest Michael Hindle Source Type: research

Development and Characterization of Excipient Enhanced Growth (EEG) Surfactant Powder Formulations for Treating Neonatal Respiratory Distress Syndrome
This study aimed to develop and characterize a spray-dried powder aerosol formulation of a commercially available surfactant formulation, Survanta® intratracheal suspension, using the excipient enhanced growth (EEG) approach. Survanta EEG powders were prepared by spray drying of the feed dispersions containing Survanta® (beractant) intratracheal suspension, hygroscopic excipients (mannitol and sodium chloride), and a dispersion enhancer (l-leucine or trileucine) in 5 or 20% v/v ethanol in water using the Buchi Nano Spray Dryer B-90 HP. Powders were characterized for primary particle size, morphology, phospholipid c...
Source: AAPS PharmSciTech - April 16, 2021 Category: Drugs & Pharmacology Authors: Susan Boc Mohammad A M Momin Dale R Farkas Worth Longest Michael Hindle Source Type: research

Performance of Low Air Volume Dry Powder Inhalers (LV-DPI) when Aerosolizing Excipient Enhanced Growth (EEG) Surfactant Powder Formulations
This study aims to develop an efficient dry powder inhaler (DPI) capable of delivering spray-dried Survanta-EEG powders (3-10 mg) with a low volume (3 mL) of dispersion air. A series of iterative design modifications were made to a base low air volume actuated DPI. The modifications included the replacement of the original capsule chamber with an integral dose containment chamber, alteration of the entrainment air flow path through the device (from single-sided (SS) to straight through (ST)), change in the number of air inlet holes (from one to three), varying the outlet delivery tube length (45, 55, and 90 mm) and interna...
Source: AAPS PharmSciTech - April 16, 2021 Category: Drugs & Pharmacology Authors: Susan Boc Mohammad A M Momin Dale R Farkas Worth Longest Michael Hindle Source Type: research

Development and Characterization of Excipient Enhanced Growth (EEG) Surfactant Powder Formulations for Treating Neonatal Respiratory Distress Syndrome
This study aimed to develop and characterize a spray-dried powder aerosol formulation of a commercially available surfactant formulation, Survanta® intratracheal suspension, using the excipient enhanced growth (EEG) approach. Survanta EEG powders were prepared by spray drying of the feed dispersions containing Survanta® (beractant) intratracheal suspension, hygroscopic excipients (mannitol and sodium chloride), and a dispersion enhancer (l-leucine or trileucine) in 5 or 20% v/v ethanol in water using the Buchi Nano Spray Dryer B-90 HP. Powders were characterized for primary particle size, morphology, phospholipid c...
Source: AAPS PharmSciTech - April 16, 2021 Category: Drugs & Pharmacology Authors: Susan Boc Mohammad A M Momin Dale R Farkas Worth Longest Michael Hindle Source Type: research

Performance of Low Air Volume Dry Powder Inhalers (LV-DPI) when Aerosolizing Excipient Enhanced Growth (EEG) Surfactant Powder Formulations
This study aims to develop an efficient dry powder inhaler (DPI) capable of delivering spray-dried Survanta-EEG powders (3-10 mg) with a low volume (3 mL) of dispersion air. A series of iterative design modifications were made to a base low air volume actuated DPI. The modifications included the replacement of the original capsule chamber with an integral dose containment chamber, alteration of the entrainment air flow path through the device (from single-sided (SS) to straight through (ST)), change in the number of air inlet holes (from one to three), varying the outlet delivery tube length (45, 55, and 90 mm) and interna...
Source: AAPS PharmSciTech - April 16, 2021 Category: Drugs & Pharmacology Authors: Susan Boc Mohammad A M Momin Dale R Farkas Worth Longest Michael Hindle Source Type: research

Development and Characterization of Excipient Enhanced Growth (EEG) Surfactant Powder Formulations for Treating Neonatal Respiratory Distress Syndrome
This study aimed to develop and characterize a spray-dried powder aerosol formulation of a commercially available surfactant formulation, Survanta® intratracheal suspension, using the excipient enhanced growth (EEG) approach. Survanta EEG powders were prepared by spray drying of the feed dispersions containing Survanta® (beractant) intratracheal suspension, hygroscopic excipients (mannitol and sodium chloride), and a dispersion enhancer (l-leucine or trileucine) in 5 or 20% v/v ethanol in water using the Buchi Nano Spray Dryer B-90 HP. Powders were characterized for primary particle size, morphology, phospholipid c...
Source: AAPS PharmSciTech - April 16, 2021 Category: Drugs & Pharmacology Authors: Susan Boc Mohammad A M Momin Dale R Farkas Worth Longest Michael Hindle Source Type: research

Performance of Low Air Volume Dry Powder Inhalers (LV-DPI) when Aerosolizing Excipient Enhanced Growth (EEG) Surfactant Powder Formulations
This study aims to develop an efficient dry powder inhaler (DPI) capable of delivering spray-dried Survanta-EEG powders (3-10 mg) with a low volume (3 mL) of dispersion air. A series of iterative design modifications were made to a base low air volume actuated DPI. The modifications included the replacement of the original capsule chamber with an integral dose containment chamber, alteration of the entrainment air flow path through the device (from single-sided (SS) to straight through (ST)), change in the number of air inlet holes (from one to three), varying the outlet delivery tube length (45, 55, and 90 mm) and interna...
Source: AAPS PharmSciTech - April 16, 2021 Category: Drugs & Pharmacology Authors: Susan Boc Mohammad A M Momin Dale R Farkas Worth Longest Michael Hindle Source Type: research

Development and Characterization of Excipient Enhanced Growth (EEG) Surfactant Powder Formulations for Treating Neonatal Respiratory Distress Syndrome
This study aimed to develop and characterize a spray-dried powder aerosol formulation of a commercially available surfactant formulation, Survanta® intratracheal suspension, using the excipient enhanced growth (EEG) approach. Survanta EEG powders were prepared by spray drying of the feed dispersions containing Survanta® (beractant) intratracheal suspension, hygroscopic excipients (mannitol and sodium chloride), and a dispersion enhancer (l-leucine or trileucine) in 5 or 20% v/v ethanol in water using the Buchi Nano Spray Dryer B-90 HP. Powders were characterized for primary particle size, morphology, phospholipid c...
Source: AAPS PharmSciTech - April 16, 2021 Category: Drugs & Pharmacology Authors: Susan Boc Mohammad A M Momin Dale R Farkas Worth Longest Michael Hindle Source Type: research

Correction to: Effect of Surface Property on the Release and Oral Absorption of Solid Sirolimus-Containing Self-Microemulsifying Drug Delivery System
AAPS PharmSciTech. 2021 Apr 14;22(3):134. doi: 10.1208/s12249-021-01997-w.NO ABSTRACTPMID:33855633 | DOI:10.1208/s12249-021-01997-w (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - April 15, 2021 Category: Drugs & Pharmacology Authors: Xueting Zhang Zhenzhen Chen Chun Tao Jing Zhang Minxin Zhang Jialiang Zhang Zhihong Liu Jiao Lin Hang Xu Qian Zhang Hongtao Song Source Type: research

Improving Oral Bioavailability of Luteolin Nanocrystals by Surface Modification of Sodium Dodecyl Sulfate
In this study, we employed sodium dodecyl sulfate (SDS), an efficient tight junction opening agent, to modify the surface of luteolin nanocrystals, aiming to enhance the bioavailability of luteolin (LUT) and luteolin nanocrystals (LNC). The particle sizes of SDS-modified luteolin nanocrystals (SLNC) were slightly larger than that of LNC, and the zeta potential of LNC and SLNC was -25.0 ± 0.7 mV and -43.5 ± 0.4 mV, respectively. Both LNC and SLNC exhibited enhanced saturation solubility and high stability in the liquid state. In the cellular study, we found that SDS has cytotoxicity on caco-2 cells and could o...
Source: AAPS PharmSciTech - April 15, 2021 Category: Drugs & Pharmacology Authors: Jiali Liu Yongbing Sun Meng Cheng Qiaoming Liu Wan Liu Chao Gao Jianfang Feng Yi Jin Liangxing Tu Source Type: research

Correction to: Effect of Surface Property on the Release and Oral Absorption of Solid Sirolimus-Containing Self-Microemulsifying Drug Delivery System
AAPS PharmSciTech. 2021 Apr 14;22(3):134. doi: 10.1208/s12249-021-01997-w.NO ABSTRACTPMID:33855633 | DOI:10.1208/s12249-021-01997-w (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - April 15, 2021 Category: Drugs & Pharmacology Authors: Xueting Zhang Zhenzhen Chen Chun Tao Jing Zhang Minxin Zhang Jialiang Zhang Zhihong Liu Jiao Lin Hang Xu Qian Zhang Hongtao Song Source Type: research

Improving Oral Bioavailability of Luteolin Nanocrystals by Surface Modification of Sodium Dodecyl Sulfate
In this study, we employed sodium dodecyl sulfate (SDS), an efficient tight junction opening agent, to modify the surface of luteolin nanocrystals, aiming to enhance the bioavailability of luteolin (LUT) and luteolin nanocrystals (LNC). The particle sizes of SDS-modified luteolin nanocrystals (SLNC) were slightly larger than that of LNC, and the zeta potential of LNC and SLNC was -25.0 ± 0.7 mV and -43.5 ± 0.4 mV, respectively. Both LNC and SLNC exhibited enhanced saturation solubility and high stability in the liquid state. In the cellular study, we found that SDS has cytotoxicity on caco-2 cells and could o...
Source: AAPS PharmSciTech - April 15, 2021 Category: Drugs & Pharmacology Authors: Jiali Liu Yongbing Sun Meng Cheng Qiaoming Liu Wan Liu Chao Gao Jianfang Feng Yi Jin Liangxing Tu Source Type: research

Development of an In Vivo Predictive Dissolution Methodology of Topiroxostat Immediate-Release Tablet Using In Silico Simulation
AAPS PharmSciTech. 2021 Apr 13;22(3):132. doi: 10.1208/s12249-021-01992-1.ABSTRACTThe main objective of this study was to develop an in vivo predictive dissolution (IVPD) model for topiroxostat immediate-release (IR) formulation by the combination of mechanistic absorption model (MAM) deconvolution method with time shifting factor (TSF) adjustment. The in vitro dissolution profiles in different biorelevant dissolution media containing different concentrations of sodium lauryl sulfate (SLS) were obtained from dissolution testing with the paddle method of the US Pharmacopeia, while the human pharmacokinetic profile was taken...
Source: AAPS PharmSciTech - April 14, 2021 Category: Drugs & Pharmacology Authors: Gang Li Haiyang Yang Wei Liu Chen Shen Yanhua Ji Yilu Sun Qing Huo Yang Liu Guopeng Wang Source Type: research

Development of an In Vivo Predictive Dissolution Methodology of Topiroxostat Immediate-Release Tablet Using In Silico Simulation
AAPS PharmSciTech. 2021 Apr 13;22(3):132. doi: 10.1208/s12249-021-01992-1.ABSTRACTThe main objective of this study was to develop an in vivo predictive dissolution (IVPD) model for topiroxostat immediate-release (IR) formulation by the combination of mechanistic absorption model (MAM) deconvolution method with time shifting factor (TSF) adjustment. The in vitro dissolution profiles in different biorelevant dissolution media containing different concentrations of sodium lauryl sulfate (SLS) were obtained from dissolution testing with the paddle method of the US Pharmacopeia, while the human pharmacokinetic profile was taken...
Source: AAPS PharmSciTech - April 14, 2021 Category: Drugs & Pharmacology Authors: Gang Li Haiyang Yang Wei Liu Chen Shen Yanhua Ji Yilu Sun Qing Huo Yang Liu Guopeng Wang Source Type: research

Preparation of High-Drug-Loaded Clarithromycin Gastric-Floating Sustained-Release Tablets Using 3D Printing
AAPS PharmSciTech. 2021 Apr 11;22(3):131. doi: 10.1208/s12249-021-01994-z.ABSTRACTThe high-drug-loaded sustained-release gastric-floating clarithromycin (CAM) tablets were proposed and manufactured via semisolid extrusion (SSE)-based 3D printing. The physical and mechanical properties, such as dimensions, weight variation, friability, and hardness, were accessed according to the quality standards of Chinese Pharmacopoeia (Ch.P). The interactions among the drug-excipients were evaluated via differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD) techniques. Next, ...
Source: AAPS PharmSciTech - April 11, 2021 Category: Drugs & Pharmacology Authors: Peihong Chen Haosen Luo Siyu Huang Jinling Liu Minmei Lin Fan Yang Junfeng Ban Zeju Huang Zhufen Lu Qingchun Xie YanZhong Chen Source Type: research

Preparation of High-Drug-Loaded Clarithromycin Gastric-Floating Sustained-Release Tablets Using 3D Printing
AAPS PharmSciTech. 2021 Apr 11;22(3):131. doi: 10.1208/s12249-021-01994-z.ABSTRACTThe high-drug-loaded sustained-release gastric-floating clarithromycin (CAM) tablets were proposed and manufactured via semisolid extrusion (SSE)-based 3D printing. The physical and mechanical properties, such as dimensions, weight variation, friability, and hardness, were accessed according to the quality standards of Chinese Pharmacopoeia (Ch.P). The interactions among the drug-excipients were evaluated via differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD) techniques. Next, ...
Source: AAPS PharmSciTech - April 11, 2021 Category: Drugs & Pharmacology Authors: Peihong Chen Haosen Luo Siyu Huang Jinling Liu Minmei Lin Fan Yang Junfeng Ban Zeju Huang Zhufen Lu Qingchun Xie YanZhong Chen Source Type: research

Printing Methods in the Production of Orodispersible Films
AAPS PharmSciTech. 2021 Apr 9;22(3):129. doi: 10.1208/s12249-021-01990-3.ABSTRACTOrodispersible film (ODF) formulations are promising and progressive drug delivery systems that are widely accepted by subjects across all the age groups. They are traditionally fabricated using the most popular yet conventional method called solvent casting method. The most modern and evolving method is based on printing technologies and such printed products are generally termed as printed orodispersible films (POFs). This modern technology is well suited to fabricate ODFs across different settings (laboratory or industrial) in general and i...
Source: AAPS PharmSciTech - April 9, 2021 Category: Drugs & Pharmacology Authors: Maram Suresh Gupta Tegginamath Pramod Kumar Robert Davidson Guruprasad Rao Kuppu Kamla Pathak Devegowda Vishakante Gowda Source Type: research

Next-Generation COVID-19 Vaccines Should Take Efficiency of Distribution into Consideration
AAPS PharmSciTech. 2021 Apr 9;22(3):126. doi: 10.1208/s12249-021-01974-3.ABSTRACTThe dire need for safe and effective coronavirus disease (COVID-19) vaccines is met with many vaccine candidates being evaluated in pre-clinical and clinical studies. The COVID-19 vaccine candidates currently in phase 3 or phase 2/3 clinical trials as well as those that recently received emergency use authorization (EUA) from the United States Food and Drug Administration (FDA) and/or other regulatory agencies worldwide require either cold (i.e., 2-8°C) or even freezing temperatures as low as -70°C for storage and distribution. Thus, e...
Source: AAPS PharmSciTech - April 9, 2021 Category: Drugs & Pharmacology Authors: Khaled AboulFotouh Zhengrong Cui Robert O Williams Source Type: research

Analytical Method Lifecycle Management in Pharmaceutical Industry: a Review
AAPS PharmSciTech. 2021 Apr 9;22(3):128. doi: 10.1208/s12249-021-01960-9.ABSTRACTThe adoption of Quality by Design (QbD) and Analytical Method Lifecycle Management (AMLM) concepts to ensure the quality of pharmaceutical products has been applied and proposed over the last few years. These concepts are based on knowledge gained from the application of scientific and quality risk management approaches, throughout method lifecycle to assure continuous improvement and high reliability of analytical results. The overall AMLM starts with the definition of the method's intended use through the Analytical Target Profile definition...
Source: AAPS PharmSciTech - April 9, 2021 Category: Drugs & Pharmacology Authors: L úcia Volta E Sousa Ricardo Gon çalves Jos é C Menezes Ant ónio Ramos Source Type: research

Enhanced Solubility and Bioavailability of Dolutegravir by Solid Dispersion Method: In Vitro and In Vivo Evaluation-a Potential Approach for HIV Therapy
AAPS PharmSciTech. 2021 Apr 9;22(3):127. doi: 10.1208/s12249-021-01995-y.ABSTRACTBeing a candidate of BCS class II, dolutegravir (DTG), a recently approved antiretroviral drug, possesses solubility issues. The current research was aimed to improve the solubility of the DTG and thereby enhance its efficacy using the solid dispersion technique. In due course, the miscibility study of the drug was performed with different polymers, where Poloxamer 407 (P407) was found suitable to move forward. The solid dispersion of DTG and P407 was formulated using solvent evaporation technique with a 1:1 proportion of drug and polymer, whe...
Source: AAPS PharmSciTech - April 9, 2021 Category: Drugs & Pharmacology Authors: Sunita Chaudhary Anroop B Nair Jigar Shah Bapi Gorain Shery Jacob Hiral Shah Vimal Patel Source Type: research

Doxorubicin-Loaded Mixed Micelles for the Effective Management of Skin Carcinoma: In Vivo Anti-Tumor Activity and Biodistribution Studies
AAPS PharmSciTech. 2021 Apr 9;22(3):130. doi: 10.1208/s12249-021-01993-0.ABSTRACTSkin cancer is an alarming concern due to increased radiation and chemical exposure. Doxorubicin is a drug prescribed for various cancers by parenteral route. Apart from the pharmaceutical challenge of being a biopharmaceutical classification system (BCS) Class III drug, the side effects of doxorubicin are also a great concern. With an aim to enhance its safety and bioavailability, a phospholipid-based micellar system was developed. The developed nanometric and symmetric carriers not only offered substantial drug loading, but also offered a te...
Source: AAPS PharmSciTech - April 9, 2021 Category: Drugs & Pharmacology Authors: Nagarani Thotakura Anshul Panjeta Poonam Negi Simran Preet Kaisar Raza Source Type: research

Printing Methods in the Production of Orodispersible Films
AAPS PharmSciTech. 2021 Apr 9;22(3):129. doi: 10.1208/s12249-021-01990-3.ABSTRACTOrodispersible film (ODF) formulations are promising and progressive drug delivery systems that are widely accepted by subjects across all the age groups. They are traditionally fabricated using the most popular yet conventional method called solvent casting method. The most modern and evolving method is based on printing technologies and such printed products are generally termed as printed orodispersible films (POFs). This modern technology is well suited to fabricate ODFs across different settings (laboratory or industrial) in general and i...
Source: AAPS PharmSciTech - April 9, 2021 Category: Drugs & Pharmacology Authors: Maram Suresh Gupta Tegginamath Pramod Kumar Robert Davidson Guruprasad Rao Kuppu Kamla Pathak Devegowda Vishakante Gowda Source Type: research

Next-Generation COVID-19 Vaccines Should Take Efficiency of Distribution into Consideration
AAPS PharmSciTech. 2021 Apr 9;22(3):126. doi: 10.1208/s12249-021-01974-3.ABSTRACTThe dire need for safe and effective coronavirus disease (COVID-19) vaccines is met with many vaccine candidates being evaluated in pre-clinical and clinical studies. The COVID-19 vaccine candidates currently in phase 3 or phase 2/3 clinical trials as well as those that recently received emergency use authorization (EUA) from the United States Food and Drug Administration (FDA) and/or other regulatory agencies worldwide require either cold (i.e., 2-8°C) or even freezing temperatures as low as -70°C for storage and distribution. Thus, e...
Source: AAPS PharmSciTech - April 9, 2021 Category: Drugs & Pharmacology Authors: Khaled AboulFotouh Zhengrong Cui Robert O Williams Source Type: research

Analytical Method Lifecycle Management in Pharmaceutical Industry: a Review
AAPS PharmSciTech. 2021 Apr 9;22(3):128. doi: 10.1208/s12249-021-01960-9.ABSTRACTThe adoption of Quality by Design (QbD) and Analytical Method Lifecycle Management (AMLM) concepts to ensure the quality of pharmaceutical products has been applied and proposed over the last few years. These concepts are based on knowledge gained from the application of scientific and quality risk management approaches, throughout method lifecycle to assure continuous improvement and high reliability of analytical results. The overall AMLM starts with the definition of the method's intended use through the Analytical Target Profile definition...
Source: AAPS PharmSciTech - April 9, 2021 Category: Drugs & Pharmacology Authors: L úcia Volta E Sousa Ricardo Gon çalves Jos é C Menezes Ant ónio Ramos Source Type: research

Enhanced Solubility and Bioavailability of Dolutegravir by Solid Dispersion Method: In Vitro and In Vivo Evaluation-a Potential Approach for HIV Therapy
AAPS PharmSciTech. 2021 Apr 9;22(3):127. doi: 10.1208/s12249-021-01995-y.ABSTRACTBeing a candidate of BCS class II, dolutegravir (DTG), a recently approved antiretroviral drug, possesses solubility issues. The current research was aimed to improve the solubility of the DTG and thereby enhance its efficacy using the solid dispersion technique. In due course, the miscibility study of the drug was performed with different polymers, where Poloxamer 407 (P407) was found suitable to move forward. The solid dispersion of DTG and P407 was formulated using solvent evaporation technique with a 1:1 proportion of drug and polymer, whe...
Source: AAPS PharmSciTech - April 9, 2021 Category: Drugs & Pharmacology Authors: Sunita Chaudhary Anroop B Nair Jigar Shah Bapi Gorain Shery Jacob Hiral Shah Vimal Patel Source Type: research

Doxorubicin-Loaded Mixed Micelles for the Effective Management of Skin Carcinoma: In Vivo Anti-Tumor Activity and Biodistribution Studies
AAPS PharmSciTech. 2021 Apr 9;22(3):130. doi: 10.1208/s12249-021-01993-0.ABSTRACTSkin cancer is an alarming concern due to increased radiation and chemical exposure. Doxorubicin is a drug prescribed for various cancers by parenteral route. Apart from the pharmaceutical challenge of being a biopharmaceutical classification system (BCS) Class III drug, the side effects of doxorubicin are also a great concern. With an aim to enhance its safety and bioavailability, a phospholipid-based micellar system was developed. The developed nanometric and symmetric carriers not only offered substantial drug loading, but also offered a te...
Source: AAPS PharmSciTech - April 9, 2021 Category: Drugs & Pharmacology Authors: Nagarani Thotakura Anshul Panjeta Poonam Negi Simran Preet Kaisar Raza Source Type: research

Printing Methods in the Production of Orodispersible Films
AAPS PharmSciTech. 2021 Apr 9;22(3):129. doi: 10.1208/s12249-021-01990-3.ABSTRACTOrodispersible film (ODF) formulations are promising and progressive drug delivery systems that are widely accepted by subjects across all the age groups. They are traditionally fabricated using the most popular yet conventional method called solvent casting method. The most modern and evolving method is based on printing technologies and such printed products are generally termed as printed orodispersible films (POFs). This modern technology is well suited to fabricate ODFs across different settings (laboratory or industrial) in general and i...
Source: AAPS PharmSciTech - April 9, 2021 Category: Drugs & Pharmacology Authors: Maram Suresh Gupta Tegginamath Pramod Kumar Robert Davidson Guruprasad Rao Kuppu Kamla Pathak Devegowda Vishakante Gowda Source Type: research

Next-Generation COVID-19 Vaccines Should Take Efficiency of Distribution into Consideration
AAPS PharmSciTech. 2021 Apr 9;22(3):126. doi: 10.1208/s12249-021-01974-3.ABSTRACTThe dire need for safe and effective coronavirus disease (COVID-19) vaccines is met with many vaccine candidates being evaluated in pre-clinical and clinical studies. The COVID-19 vaccine candidates currently in phase 3 or phase 2/3 clinical trials as well as those that recently received emergency use authorization (EUA) from the United States Food and Drug Administration (FDA) and/or other regulatory agencies worldwide require either cold (i.e., 2-8°C) or even freezing temperatures as low as -70°C for storage and distribution. Thus, e...
Source: AAPS PharmSciTech - April 9, 2021 Category: Drugs & Pharmacology Authors: Khaled AboulFotouh Zhengrong Cui Robert O Williams Source Type: research