The Effect of Inflammatory Bowel Disease and Irritable Bowel Syndrome on Pravastatin Oral Bioavailability: In vivo and in silico evaluation using bottom-up wbPBPK modeling
AAPS PharmSciTech. 2024 Apr 11;25(4):86. doi: 10.1208/s12249-024-02803-z.ABSTRACTThe common disorders irritable bowel syndrome (IBS) and inflammatory bowel disease (IBD) can modify the drugs' pharmacokinetics via their induced pathophysiological changes. This work aimed to investigate the impact of these two diseases on pravastatin oral bioavailability. Rat models for IBS and IBD were used to experimentally test the effects of IBS and IBD on pravastatin pharmacokinetics. Then, the observations made in rats were extrapolated to humans using a mechanistic whole-body physiologically-based pharmacokinetic (wbPBPK) model. The r...
Source: AAPS PharmSciTech - April 11, 2024 Category: Drugs & Pharmacology Authors: Motasem M Alsmadi Alla A Abudaqqa Nasir Idkaidek Nidal A Qinna Ahmad Al-Ghazawi Source Type: research

Natural Polymer-Based Nanogel for pH-Responsive Delivery of Sorafenib Tosylate in Hemangiosarcoma
This study is promising but challenging depending on the in vivo study. The nanogel was successfully prepared and evaluated for pH-responsive release. As hemangiosarcoma commonly occurs in dogs, this formulation helps to limit the difficulties with administration.PMID:38605211 | DOI:10.1208/s12249-024-02797-8 (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - April 11, 2024 Category: Drugs & Pharmacology Authors: Kiran K Mali Yogeshkumar N Gavhane Rita D Chakole Source Type: research

Multicomponent Amorphous Solid Forms of Telmisartan: Insights into Mechanochemical Activation and Physicochemical Attributes
AAPS PharmSciTech. 2024 Apr 11;25(4):84. doi: 10.1208/s12249-024-02799-6.ABSTRACTThe present work aims to explore the new solid forms of telmisartan (TEL) with alpha-ketoglutaric acid (KGA) and glutamic acid (GA) as potential coformers using mechanochemical approach and their role in augmentation in physicochemical parameters over pure crystalline TEL. Mechanochemical synthesis was performed using 1:1 stoichiometric ratio of TEL and the selected coformers in the presence of catalytic amount of ethanol for 1 h. The ground product was characterized by PXRD, DSC, and FTIR. The new solid forms were evaluated for apparent solub...
Source: AAPS PharmSciTech - April 11, 2024 Category: Drugs & Pharmacology Authors: Jamshed Haneef Shakir Ali Source Type: research

Novel Drug Delivery Approaches for the Localized Treatment of Cervical Cancer
AAPS PharmSciTech. 2024 Apr 11;25(4):85. doi: 10.1208/s12249-024-02801-1.ABSTRACTCervical cancer (CC) is the fourth leading cancer type in females globally. Being an ailment of the birth canal, primitive treatment strategies, including surgery, radiation, or laser therapy, bring along the risk of infertility, neonate mortality, premature parturition, etc. Systemic chemotherapy led to systemic toxicity. Therefore, delivering a smaller cargo of therapeutics to the local site is more beneficial in terms of efficacy as well as safety. Due to the regeneration of cervicovaginal mucus, conventional dosage forms come with the limi...
Source: AAPS PharmSciTech - April 11, 2024 Category: Drugs & Pharmacology Authors: Ivy Saha Jitu Halder Tushar Kanti Rajwar Ritu Mahanty Deepak Pradhan Priyanka Dash Chandan Das Vineet Kumar Rai Biswakanth Kar Goutam Ghosh Goutam Rath Source Type: research

The Effect of Inflammatory Bowel Disease and Irritable Bowel Syndrome on Pravastatin Oral Bioavailability: In vivo and in silico evaluation using bottom-up wbPBPK modeling
AAPS PharmSciTech. 2024 Apr 11;25(4):86. doi: 10.1208/s12249-024-02803-z.ABSTRACTThe common disorders irritable bowel syndrome (IBS) and inflammatory bowel disease (IBD) can modify the drugs' pharmacokinetics via their induced pathophysiological changes. This work aimed to investigate the impact of these two diseases on pravastatin oral bioavailability. Rat models for IBS and IBD were used to experimentally test the effects of IBS and IBD on pravastatin pharmacokinetics. Then, the observations made in rats were extrapolated to humans using a mechanistic whole-body physiologically-based pharmacokinetic (wbPBPK) model. The r...
Source: AAPS PharmSciTech - April 11, 2024 Category: Drugs & Pharmacology Authors: Motasem M Alsmadi Alla A Abudaqqa Nasir Idkaidek Nidal A Qinna Ahmad Al-Ghazawi Source Type: research

Natural Polymer-Based Nanogel for pH-Responsive Delivery of Sorafenib Tosylate in Hemangiosarcoma
This study is promising but challenging depending on the in vivo study. The nanogel was successfully prepared and evaluated for pH-responsive release. As hemangiosarcoma commonly occurs in dogs, this formulation helps to limit the difficulties with administration.PMID:38605211 | DOI:10.1208/s12249-024-02797-8 (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - April 11, 2024 Category: Drugs & Pharmacology Authors: Kiran K Mali Yogeshkumar N Gavhane Rita D Chakole Source Type: research

Multicomponent Amorphous Solid Forms of Telmisartan: Insights into Mechanochemical Activation and Physicochemical Attributes
AAPS PharmSciTech. 2024 Apr 11;25(4):84. doi: 10.1208/s12249-024-02799-6.ABSTRACTThe present work aims to explore the new solid forms of telmisartan (TEL) with alpha-ketoglutaric acid (KGA) and glutamic acid (GA) as potential coformers using mechanochemical approach and their role in augmentation in physicochemical parameters over pure crystalline TEL. Mechanochemical synthesis was performed using 1:1 stoichiometric ratio of TEL and the selected coformers in the presence of catalytic amount of ethanol for 1 h. The ground product was characterized by PXRD, DSC, and FTIR. The new solid forms were evaluated for apparent solub...
Source: AAPS PharmSciTech - April 11, 2024 Category: Drugs & Pharmacology Authors: Jamshed Haneef Shakir Ali Source Type: research

Novel Drug Delivery Approaches for the Localized Treatment of Cervical Cancer
AAPS PharmSciTech. 2024 Apr 11;25(4):85. doi: 10.1208/s12249-024-02801-1.ABSTRACTCervical cancer (CC) is the fourth leading cancer type in females globally. Being an ailment of the birth canal, primitive treatment strategies, including surgery, radiation, or laser therapy, bring along the risk of infertility, neonate mortality, premature parturition, etc. Systemic chemotherapy led to systemic toxicity. Therefore, delivering a smaller cargo of therapeutics to the local site is more beneficial in terms of efficacy as well as safety. Due to the regeneration of cervicovaginal mucus, conventional dosage forms come with the limi...
Source: AAPS PharmSciTech - April 11, 2024 Category: Drugs & Pharmacology Authors: Ivy Saha Jitu Halder Tushar Kanti Rajwar Ritu Mahanty Deepak Pradhan Priyanka Dash Chandan Das Vineet Kumar Rai Biswakanth Kar Goutam Ghosh Goutam Rath Source Type: research

The Effect of Inflammatory Bowel Disease and Irritable Bowel Syndrome on Pravastatin Oral Bioavailability: In vivo and in silico evaluation using bottom-up wbPBPK modeling
AAPS PharmSciTech. 2024 Apr 11;25(4):86. doi: 10.1208/s12249-024-02803-z.ABSTRACTThe common disorders irritable bowel syndrome (IBS) and inflammatory bowel disease (IBD) can modify the drugs' pharmacokinetics via their induced pathophysiological changes. This work aimed to investigate the impact of these two diseases on pravastatin oral bioavailability. Rat models for IBS and IBD were used to experimentally test the effects of IBS and IBD on pravastatin pharmacokinetics. Then, the observations made in rats were extrapolated to humans using a mechanistic whole-body physiologically-based pharmacokinetic (wbPBPK) model. The r...
Source: AAPS PharmSciTech - April 11, 2024 Category: Drugs & Pharmacology Authors: Motasem M Alsmadi Alla A Abudaqqa Nasir Idkaidek Nidal A Qinna Ahmad Al-Ghazawi Source Type: research

Natural Polymer-Based Nanogel for pH-Responsive Delivery of Sorafenib Tosylate in Hemangiosarcoma
This study is promising but challenging depending on the in vivo study. The nanogel was successfully prepared and evaluated for pH-responsive release. As hemangiosarcoma commonly occurs in dogs, this formulation helps to limit the difficulties with administration.PMID:38605211 | DOI:10.1208/s12249-024-02797-8 (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - April 11, 2024 Category: Drugs & Pharmacology Authors: Kiran K Mali Yogeshkumar N Gavhane Rita D Chakole Source Type: research

Multicomponent Amorphous Solid Forms of Telmisartan: Insights into Mechanochemical Activation and Physicochemical Attributes
AAPS PharmSciTech. 2024 Apr 11;25(4):84. doi: 10.1208/s12249-024-02799-6.ABSTRACTThe present work aims to explore the new solid forms of telmisartan (TEL) with alpha-ketoglutaric acid (KGA) and glutamic acid (GA) as potential coformers using mechanochemical approach and their role in augmentation in physicochemical parameters over pure crystalline TEL. Mechanochemical synthesis was performed using 1:1 stoichiometric ratio of TEL and the selected coformers in the presence of catalytic amount of ethanol for 1 h. The ground product was characterized by PXRD, DSC, and FTIR. The new solid forms were evaluated for apparent solub...
Source: AAPS PharmSciTech - April 11, 2024 Category: Drugs & Pharmacology Authors: Jamshed Haneef Shakir Ali Source Type: research

Polymer Characteristics for Drug Layering on Particles Using a Novel Melt Granulation Technology, MALCORE < sup > ® < /sup >
In conclusion, understanding the properties required for polymers in the melt granulation process of MALCORE® allows for the optimization of manufacturing conditions, such as temperature and mixing ratios, for efficient and consistent drug layering.PMID:38600252 | DOI:10.1208/s12249-024-02798-7 (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - April 10, 2024 Category: Drugs & Pharmacology Authors: Ryota Kimata Naoki Yoshihara Yuya Tomita Takayuki Terukina Hiromu Kondo Source Type: research

On the Feasibility of Rugose Lipid Microparticles in Pressurized Metered Dose Inhalers with Established and New Propellants
This study investigates the feasibility of novel rugose lipid particles (RLPs) as potential drug carriers in pMDI formulations. The physical stability of RLPs was assessed in three different propellants: the established HFA-134a and HFA-227ea and the new low global-warming-potential (GWP) propellant HFO-1234ze. A feedstock containing DSPC and calcium chloride was prepared without pore forming agent to spray dry two RLP batches at inlet temperatures of 55 °C (RLP55) and 75 °C (RLP75). RLPs performance in pMDI formulations was compared to two reference samples that exhibit significantly different performance when suspended...
Source: AAPS PharmSciTech - April 10, 2024 Category: Drugs & Pharmacology Authors: Zahra Minootan Hui Wang Patrick Connaughton Kellisa Lachacz Nicholas Carrigy Mani Ordoubadi David Lechuga-Ballesteros Andrew R Martin Reinhard Vehring Source Type: research

Revolutionizing Knee Osteoarthritis Treatment: Innovative Self-Nano-Emulsifying Polyethylene Glycol Organogel of Curcumin for Effective Topical Delivery
AAPS PharmSciTech. 2024 Apr 10;25(4):80. doi: 10.1208/s12249-024-02789-8.ABSTRACTIn the current study, self-nano-emulsifying (SNE) physically cross-linked polyethylene glycol (PEG) organogel (SNE-POG) as an innovative hybrid system was fabricated for topical delivery of water-insoluble and unstable bioactive compound curcumin (CUR). Response surface methodology (RSM) based on Optimal Design was utilized to evaluate the formulation factors. Solid fiber mechanism with homogenization was used to prepare formulations. Pharmaceutical evaluation including rheological and texture analysis, their mathematical correlations besides ...
Source: AAPS PharmSciTech - April 10, 2024 Category: Drugs & Pharmacology Authors: Mahtab Baharizade Seyed Iman Ghetmiri Mohsen Mohammady Soliman Mohammadi-Samani Gholamhossein Yousefi Source Type: research

Polymer Characteristics for Drug Layering on Particles Using a Novel Melt Granulation Technology, MALCORE < sup > ® < /sup >
In conclusion, understanding the properties required for polymers in the melt granulation process of MALCORE® allows for the optimization of manufacturing conditions, such as temperature and mixing ratios, for efficient and consistent drug layering.PMID:38600252 | DOI:10.1208/s12249-024-02798-7 (Source: AAPS PharmSciTech)
Source: AAPS PharmSciTech - April 10, 2024 Category: Drugs & Pharmacology Authors: Ryota Kimata Naoki Yoshihara Yuya Tomita Takayuki Terukina Hiromu Kondo Source Type: research