Please use this identifier to cite or link to this item:
Title: Poly(2-Ethyl-2-Oxazoline) as an alternative to poly(Vinylpyrrolidone) in solid dispersions for solubility and dissolution rate enhancement of drugs
Author: Fael, Hanan
Ràfols Llach, Clara
Demirel, A. Levent
Keywords: Solubilitat dels medicaments
Disseny de medicaments
Drug solubility
Drug design
Issue Date: 31-May-2018
Publisher: Wiley
Abstract: Poly(2-ethyl-2-oxazoline) (PEOX), a biocompatible polymer considered as pseudopolypeptide, was introduced as a potential alternative to the commonly used polymer, poly(vinylpyrrolidone) (PVP) for the preparation of solid dispersion with a poorly soluble drug. Glipizide (GPZ), a Biopharmaceutical Classification System class II model drug, was selected for solubility and dissolution rate study. GPZ-polymer solid dispersions and physical mixtures were characterized and investigated by X-ray diffractometry, differential scanning calorimetry, scanning electron microscopy, and FTIR spectroscopy. The impact of polymers on crystal nucleation kinetics was studied, and PEOX exhibited strong inhibitory effect compared with PVP. Solubility and dissolution behavior of the prepared solid dispersions and their physical blends were in vitro examined and evaluated. A significant enhancement in GPZ solubility was obtained with PEOX compared with the pure drug and solid dispersion with PVP. A big improvement in the intrinsic dissolution rate (45 times) and dissolved amount of GPZ (58 times) was achieved with PEOX in fasted state simulated intestinal fluid, against comparable enhancement observed with PEOX and PVP in phosphate buffer at pH 6.8. Lower molecular weight of PEOX-5K (5000 g/mol) was found to be superior to higher molecular weight PEOX-50K (50,000 g/mol) in the improvement of dissolution behavior. The findings of this study with GPZ as a model drug introduce lower molecular weight PEOX as a promising polymeric carrier toward better oral bioavailability of poorly soluble drugs.
Note: Versió postprint del document publicat a:
It is part of: Journal of Pharmaceutical Sciences, 2018, vol. 107, num. 9, p. 2428-2438
Related resource:
ISSN: 0022-3549
Appears in Collections:Articles publicats en revistes (Enginyeria Química i Química Analítica)

Files in This Item:
File Description SizeFormat 
689220.pdf2.85 MBAdobe PDFView/Open

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.