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دانشگاه علوم پزشکی و خدمات بهداشتی درمانی زنجان

Oral delivery of indinavir using mPEG-PCL nanoparticles: preparation, optimization, cellular uptake, transport and pharmacokinetic evaluationpharmacokinetic evaluation

(2019) Oral delivery of indinavir using mPEG-PCL nanoparticles: preparation, optimization, cellular uptake, transport and pharmacokinetic evaluationpharmacokinetic evaluation. Artificial Cells, Nanomedicine and Biotechnology. pp. 2123-2133. ISSN 2169-1401

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Abstract

Introduction: Indinavir (IDV) is a potent HIV protease inhibitor used in the treatment of human immunodeficiency virus (HIV). IDV is a weak base with limited aqueous solubility in its unprotonated form; therefore, solubility of IDV in the gastrointestinal tract fluids is the rate-limiting step of its absorption and onset of action. However, in many cases, drugs are not absorbed well in the gastrointestinal tract; polymer nanoparticles were recognized as an effective carrier system for drug encapsulation and are now studied as a vehicle for oral delivery of insoluble compounds. Preparation of methoxy poly (ethylene glycol)-poly (e-caprolactone) (mPEG-PCL) nanoparticles is among the strategies to overcome low bioavailability of drugs with poor aqueous solubility. Materials and method: The structure of the copolymers was characterized using1H NMR, FTIR, DSC and GPC techniques. IDV loaded mPEG-PCL nanoparticles prepared by emulsification solvent evaporation method were optimized using D-optimal experimental design and were characterized by various techniques such as DLS, DSC, XRD, AFM and SEM. Using Caco-2 cells as a cellular model, we studied the cellular uptake and transport. Results: In vivo pharmacokinetic studies were performed in rats. The plasma AUC (0ât), t1/2 and Cmax of IDV-mPEG-PCL NPs were increased by 5.30, 5.57 and 1.37 fold compared to the IDV solution, respectively. Conclusion: The results of this study are promising for the use of biodegradable polymeric nanoparticles to improve oral drug delivery. © 2019 The Author(s).

Item Type: Article
Keywords: Oral delivery of indinavir using mPEG-PCL nanoparticles: preparation, optimization, cellular uptake, transport and pharmacokinetic evaluation
Divisions: Education Vice-Chancellor Department > Faculty of Pharmacy > Department of Pharmacotherapy
Page Range: pp. 2123-2133
Journal or Publication Title: Artificial Cells, Nanomedicine and Biotechnology
Abstract and Indexing: ISI, Pubmed, Scopus, Other
Quartile : Q1
Volume: 47
Number: 1
Publisher: Taylor & Francis
Identification Number: https://doi.org/10.1080/21691401.2019.1616553
ISSN: 2169-1401
Depositing User: خانم فائزه مظفری
URI: http://repository.zums.ac.ir/id/eprint/5810

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