Enhancing Anticancer Efficacy of Formononetin Microspheres via Microfluidic Fabrication
AAPS PharmSciTech. 2023 Nov 28;24(8):241. doi: 10.1208/s12249-023-02691-9.ABSTRACTFormononetin is a flavonoid compound with anti-tumor and anti-inflammatory properties. However, its low solubility limits its clinical use. We employed microfluidic technology to prepare formononetin-loaded PLGA-PEGDA microspheres (Degradable polymer PLGA, Crosslinking agent PEGDA), which can encapsulate and release drugs in a controlled manner. We optimized and characterized the microspheres, and evaluated their antitumor effects. The microspheres had uniform size, high drug loading efficiency, high encapsulation efficiency, and stable relea...
Source: AAPS PharmSciTech - November 28, 2023 Category: Drugs & Pharmacology Authors: Xia Cao Qingwen Li Xiaoli Li Qi Liu Kai Liu Tianwen Deng Xuedi Weng Qintong Yu Wenwen Deng Jiangnan Yu Qilong Wang Gao Xiao Ximing Xu Source Type: research
Thyme Oil-Containing Fluconazole-Loaded Transferosomal Bigel for Transdermal Delivery
The objective of the present research was to develop fluconazole-loaded transferosomal bigels for transdermal delivery by employing statistical optimization (23 factorial design-based). Thin-film hydration was employed to prepare fluconazole-loaded transferomal suspensions, which were then incorporated into bigel system. A 23 factorial design was employed where ratios of lipids to edge activators, lipids (soya lecithin to cholesterol), and edge activators (sodium deoxycholate to Tween 80) were factors. Ex vivo permeation flux (Jss) of transferosomal bigels across porcine skin was analyzed as response. The optimal setting f...
Source: AAPS PharmSciTech - November 22, 2023 Category: Drugs & Pharmacology Authors: Biswarup Das Amit Kumar Nayak Subrata Mallick Source Type: research
Pharmacokinetics of Two Nanoemulsion Formulations of Δ < sup > 8 < /sup > -Tetrahydrocannabinol in Rats
AAPS PharmSciTech. 2023 Nov 21;24(8):239. doi: 10.1208/s12249-023-02699-1.ABSTRACTThe use of Δ8-tetrahydrocannabinol (Δ8-THC) has increased in recent years. Given that the oral absorption of cannabinoids in oil formulations is typically slow and variable, nanoemulsions may be an improved delivery vehicle. Therefore, we characterized the pharmacokinetics (PK) in Sprague-Dawley rats following the administration of three different oral formulations containing 10 mg/kg Δ8-THC: a translucent liquid nanoemulsion, a reconstituted powder nanoemulsion, and a medium chain triglyceride (MCT) oil solution for comparison. Δ8-THC wa...
Source: AAPS PharmSciTech - November 22, 2023 Category: Drugs & Pharmacology Authors: Michael Tagen Linda E Klumpers Alexey Peshkovsky Source Type: research
Sticking Detection by Repeated Compactions on a Single Tablet
AAPS PharmSciTech. 2023 Nov 21;24(8):237. doi: 10.1208/s12249-023-02694-6.ABSTRACT"Sticking" during tablet manufacture is the term used to describe the accumulation of adhered tablet material on the punch over the course of several compaction cycles. The occurrence of sticking can affect tablet weight, image, and structural integrity and halt manufacturing operations. The earlier the risk of sticking is detected during R&D, the more options are available for mitigation and the less potential there is for significant delays and costs. The detection osf sticking, however, during the early stages of drug development is ch...
Source: AAPS PharmSciTech - November 22, 2023 Category: Drugs & Pharmacology Authors: James Thomas Phuong Bui Antonios Zavaliangos Source Type: research
Systemically Administered Anti-uPAR Antibody Plasma and Lung ELF Pharmacokinetics Characterized by Minimal Lung PBPK Model
In this study, we evaluated the exposure of two different uPAR (urokinase-type plasminogen activator receptor) targeting full-length monoclonal IgGs in plasma and lung epithelial lining fluid (ELF) of mice after IP and IV administration. Antibody AK17 exhibited linear pharmacokinetics (PK) in plasma and ELF at 3 and 30 mg/kg single IV dose. The average plasma and ELF half-lives for AK17 and AK21 ranged between ~321-411 h and ~230-345 h, respectively, indicating sustained systemic and lung exposure of antibodies. The average ELF to the plasma concentration ratio of antibodies was ~0.01 and ~0.03 with IP and IV dosing, respe...
Source: AAPS PharmSciTech - November 22, 2023 Category: Drugs & Pharmacology Authors: Sharad Sharma Antony Leonard Kathryn Phoenix Hsueh Yuan Chang Jun Wang Steven Hansel Source Type: research
Unlocking the Potential of Bilosomes and Modified Bilosomes: a Comprehensive Journey into Advanced Drug Delivery Trends
AAPS PharmSciTech. 2023 Nov 21;24(8):238. doi: 10.1208/s12249-023-02696-4.ABSTRACTVesicular drug delivery systems have revolutionized the pharmaceutical field, offering a promising path for achieving targeted and sustained drug delivery. The oral, transdermal, and ocular routes of administration offer optimal ease in attaining desired therapeutic outcomes. However, conventional treatment strategies are all plagued with several challenges, such as poor skin permeability, ocular barriers, and gastrointestinal (GIT) degradation leading to vesicular disruption with the release of the encapsulated drug before reaching the targe...
Source: AAPS PharmSciTech - November 22, 2023 Category: Drugs & Pharmacology Authors: Devika Nayak Mahalaxmi Rathnanand Vamshi Krishna Tippavajhala Source Type: research
Thyme Oil-Containing Fluconazole-Loaded Transferosomal Bigel for Transdermal Delivery
The objective of the present research was to develop fluconazole-loaded transferosomal bigels for transdermal delivery by employing statistical optimization (23 factorial design-based). Thin-film hydration was employed to prepare fluconazole-loaded transferomal suspensions, which were then incorporated into bigel system. A 23 factorial design was employed where ratios of lipids to edge activators, lipids (soya lecithin to cholesterol), and edge activators (sodium deoxycholate to Tween 80) were factors. Ex vivo permeation flux (Jss) of transferosomal bigels across porcine skin was analyzed as response. The optimal setting f...
Source: AAPS PharmSciTech - November 22, 2023 Category: Drugs & Pharmacology Authors: Biswarup Das Amit Kumar Nayak Subrata Mallick Source Type: research
Pharmacokinetics of Two Nanoemulsion Formulations of Δ < sup > 8 < /sup > -Tetrahydrocannabinol in Rats
AAPS PharmSciTech. 2023 Nov 21;24(8):239. doi: 10.1208/s12249-023-02699-1.ABSTRACTThe use of Δ8-tetrahydrocannabinol (Δ8-THC) has increased in recent years. Given that the oral absorption of cannabinoids in oil formulations is typically slow and variable, nanoemulsions may be an improved delivery vehicle. Therefore, we characterized the pharmacokinetics (PK) in Sprague-Dawley rats following the administration of three different oral formulations containing 10 mg/kg Δ8-THC: a translucent liquid nanoemulsion, a reconstituted powder nanoemulsion, and a medium chain triglyceride (MCT) oil solution for comparison. Δ8-THC wa...
Source: AAPS PharmSciTech - November 22, 2023 Category: Drugs & Pharmacology Authors: Michael Tagen Linda E Klumpers Alexey Peshkovsky Source Type: research
Sticking Detection by Repeated Compactions on a Single Tablet
AAPS PharmSciTech. 2023 Nov 21;24(8):237. doi: 10.1208/s12249-023-02694-6.ABSTRACT"Sticking" during tablet manufacture is the term used to describe the accumulation of adhered tablet material on the punch over the course of several compaction cycles. The occurrence of sticking can affect tablet weight, image, and structural integrity and halt manufacturing operations. The earlier the risk of sticking is detected during R&D, the more options are available for mitigation and the less potential there is for significant delays and costs. The detection osf sticking, however, during the early stages of drug development is ch...
Source: AAPS PharmSciTech - November 22, 2023 Category: Drugs & Pharmacology Authors: James Thomas Phuong Bui Antonios Zavaliangos Source Type: research
Systemically Administered Anti-uPAR Antibody Plasma and Lung ELF Pharmacokinetics Characterized by Minimal Lung PBPK Model
In this study, we evaluated the exposure of two different uPAR (urokinase-type plasminogen activator receptor) targeting full-length monoclonal IgGs in plasma and lung epithelial lining fluid (ELF) of mice after IP and IV administration. Antibody AK17 exhibited linear pharmacokinetics (PK) in plasma and ELF at 3 and 30 mg/kg single IV dose. The average plasma and ELF half-lives for AK17 and AK21 ranged between ~321-411 h and ~230-345 h, respectively, indicating sustained systemic and lung exposure of antibodies. The average ELF to the plasma concentration ratio of antibodies was ~0.01 and ~0.03 with IP and IV dosing, respe...
Source: AAPS PharmSciTech - November 22, 2023 Category: Drugs & Pharmacology Authors: Sharad Sharma Antony Leonard Kathryn Phoenix Hsueh Yuan Chang Jun Wang Steven Hansel Source Type: research
Unlocking the Potential of Bilosomes and Modified Bilosomes: a Comprehensive Journey into Advanced Drug Delivery Trends
AAPS PharmSciTech. 2023 Nov 21;24(8):238. doi: 10.1208/s12249-023-02696-4.ABSTRACTVesicular drug delivery systems have revolutionized the pharmaceutical field, offering a promising path for achieving targeted and sustained drug delivery. The oral, transdermal, and ocular routes of administration offer optimal ease in attaining desired therapeutic outcomes. However, conventional treatment strategies are all plagued with several challenges, such as poor skin permeability, ocular barriers, and gastrointestinal (GIT) degradation leading to vesicular disruption with the release of the encapsulated drug before reaching the targe...
Source: AAPS PharmSciTech - November 22, 2023 Category: Drugs & Pharmacology Authors: Devika Nayak Mahalaxmi Rathnanand Vamshi Krishna Tippavajhala Source Type: research
Thyme Oil-Containing Fluconazole-Loaded Transferosomal Bigel for Transdermal Delivery
The objective of the present research was to develop fluconazole-loaded transferosomal bigels for transdermal delivery by employing statistical optimization (23 factorial design-based). Thin-film hydration was employed to prepare fluconazole-loaded transferomal suspensions, which were then incorporated into bigel system. A 23 factorial design was employed where ratios of lipids to edge activators, lipids (soya lecithin to cholesterol), and edge activators (sodium deoxycholate to Tween 80) were factors. Ex vivo permeation flux (Jss) of transferosomal bigels across porcine skin was analyzed as response. The optimal setting f...
Source: AAPS PharmSciTech - November 22, 2023 Category: Drugs & Pharmacology Authors: Biswarup Das Amit Kumar Nayak Subrata Mallick Source Type: research
Pharmacokinetics of Two Nanoemulsion Formulations of Δ < sup > 8 < /sup > -Tetrahydrocannabinol in Rats
AAPS PharmSciTech. 2023 Nov 21;24(8):239. doi: 10.1208/s12249-023-02699-1.ABSTRACTThe use of Δ8-tetrahydrocannabinol (Δ8-THC) has increased in recent years. Given that the oral absorption of cannabinoids in oil formulations is typically slow and variable, nanoemulsions may be an improved delivery vehicle. Therefore, we characterized the pharmacokinetics (PK) in Sprague-Dawley rats following the administration of three different oral formulations containing 10 mg/kg Δ8-THC: a translucent liquid nanoemulsion, a reconstituted powder nanoemulsion, and a medium chain triglyceride (MCT) oil solution for comparison. Δ8-THC wa...
Source: AAPS PharmSciTech - November 22, 2023 Category: Drugs & Pharmacology Authors: Michael Tagen Linda E Klumpers Alexey Peshkovsky Source Type: research
Sticking Detection by Repeated Compactions on a Single Tablet
AAPS PharmSciTech. 2023 Nov 21;24(8):237. doi: 10.1208/s12249-023-02694-6.ABSTRACT"Sticking" during tablet manufacture is the term used to describe the accumulation of adhered tablet material on the punch over the course of several compaction cycles. The occurrence of sticking can affect tablet weight, image, and structural integrity and halt manufacturing operations. The earlier the risk of sticking is detected during R&D, the more options are available for mitigation and the less potential there is for significant delays and costs. The detection osf sticking, however, during the early stages of drug development is ch...
Source: AAPS PharmSciTech - November 22, 2023 Category: Drugs & Pharmacology Authors: James Thomas Phuong Bui Antonios Zavaliangos Source Type: research
Systemically Administered Anti-uPAR Antibody Plasma and Lung ELF Pharmacokinetics Characterized by Minimal Lung PBPK Model
In this study, we evaluated the exposure of two different uPAR (urokinase-type plasminogen activator receptor) targeting full-length monoclonal IgGs in plasma and lung epithelial lining fluid (ELF) of mice after IP and IV administration. Antibody AK17 exhibited linear pharmacokinetics (PK) in plasma and ELF at 3 and 30 mg/kg single IV dose. The average plasma and ELF half-lives for AK17 and AK21 ranged between ~321-411 h and ~230-345 h, respectively, indicating sustained systemic and lung exposure of antibodies. The average ELF to the plasma concentration ratio of antibodies was ~0.01 and ~0.03 with IP and IV dosing, respe...
Source: AAPS PharmSciTech - November 22, 2023 Category: Drugs & Pharmacology Authors: Sharad Sharma Antony Leonard Kathryn Phoenix Hsueh Yuan Chang Jun Wang Steven Hansel Source Type: research
