Role of P-Glycoprotein Inhibitors in the Bioavailability Enhancement of Solid Dispersion of Darunavir
Joint Authors
Baboota, Sanjula
Rehman, Saleha
Nabi, Bushra
Fazil, Mohammad
Khan, Saba
Bari, Naimat Kalim
Singh, Romi
Ahmad, Shavej
Kumar, Varinder
Ali, Javed
Source
Issue
Vol. 2017, Issue 2017 (31 Dec. 2017), pp.1-17, 17 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2017-10-31
Country of Publication
Egypt
No. of Pages
17
Main Subjects
Abstract EN
Objective.
The aim of the present study was to improve bioavailability of an important antiretroviral drug, Darunavir (DRV), which has low water solubility and poor intestinal absorption through solid dispersion (SD) approach incorporating polymer with P-glycoprotein inhibitory potential.
Methods.
A statistical approach where design of experiment (DoE) was used to prepare SD of DRV with incorporation of P-glycoprotein inhibitors.
Using DoE, different methods of preparation, like melt, solvent evaporation, and spray drying method, utilizing carriers like Kolliphor TPGS and Soluplus were evaluated.
The optimized SD was characterized by DSC, FTIR, XRD, and SEM and further evaluated for enhancement in absorption using everted gut sac model, effect of food on absorption of DRV, and in vivo prospect.
Results and Discussion.
DSC, FTIR, XRD, and SEM confirmed the amorphicity of drug in SD.
Oral bioavailability studies revealed better absorption of DRV when given with food.
Absorption studies and in vivo study findings demonstrated great potential of Kolliphor TPGS as P-glycoprotein inhibitor for increasing intestinal absorption and thus bioavailability of DRV.
Conclusion.
It is concluded that SD of DRV with the incorporation of Kolliphor TPGS was potential and promising approach in increasing bioavailability of DRV as well as minimizing its extrusion via P-glycoprotein efflux transporters.
American Psychological Association (APA)
Rehman, Saleha& Nabi, Bushra& Fazil, Mohammad& Khan, Saba& Bari, Naimat Kalim& Singh, Romi…[et al.]. 2017. Role of P-Glycoprotein Inhibitors in the Bioavailability Enhancement of Solid Dispersion of Darunavir. BioMed Research International،Vol. 2017, no. 2017, pp.1-17.
https://search.emarefa.net/detail/BIM-1139000
Modern Language Association (MLA)
Rehman, Saleha…[et al.]. Role of P-Glycoprotein Inhibitors in the Bioavailability Enhancement of Solid Dispersion of Darunavir. BioMed Research International No. 2017 (2017), pp.1-17.
https://search.emarefa.net/detail/BIM-1139000
American Medical Association (AMA)
Rehman, Saleha& Nabi, Bushra& Fazil, Mohammad& Khan, Saba& Bari, Naimat Kalim& Singh, Romi…[et al.]. Role of P-Glycoprotein Inhibitors in the Bioavailability Enhancement of Solid Dispersion of Darunavir. BioMed Research International. 2017. Vol. 2017, no. 2017, pp.1-17.
https://search.emarefa.net/detail/BIM-1139000
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1139000