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pH- sensitive nanoparticles developed and optimized using factorial design for oral delivery of gliclazide

Al-Kassas, R, Madni, A, Buchanan, C and Shelling, A (2021) pH- sensitive nanoparticles developed and optimized using factorial design for oral delivery of gliclazide. Journal of Pharmaceutical Innovation. ISSN 1872-5120

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The present study aimed at improving the oral absorption of gliclazide (GLZ) through preparation and optimization of pH-sensitive nanoparticles (NPs) based on Eudragit® S100 polymer for prolonging the residence time of the drug in the gastrointestinal tract and consequently improving its oral absorption. Nanoprecipitation technique was used for preparation of GLZ NPs. A 33 full factorial design was applied to study the effect of independent variables (polymer concentration, volume of the organic phase, and stabilizer's concentration) on the mean particle size, zeta potential and the incorporation efficiency of GLZ NPs. The developed optimal formulation was evaluated using various methods including X-ray diffraction (XRD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR) and scanning electron microscopy (SEM). The analysis of the results revealed transformation of GLZ from crystalline to unstructured form and the absence of any chemical interactions between GLZ and the polymer. The in vitro drug release was dependent on the dissolution behaviour of the polymer. The glucose stimulated insulin section test showed incorporation of GLZ into NPs has potentiated its effect on insulin secretion in β cells in presence of (10mM) glucose. Our study suggests that the optimized NPs have a potential to improve the oral absorption of GLZ.

Item Type: Article
Additional Information: This is a post-peer-review, pre-copyedit version of an article published in Journal of Pharmaceutical Innovation. The final authenticated version is available online at: http://dx.doi.org/10.1007/s12247-021-09536-7
Uncontrolled Keywords: 1115 Pharmacology and Pharmaceutical Sciences
Subjects: R Medicine > RM Therapeutics. Pharmacology
Divisions: Pharmacy & Biomolecular Sciences
Publisher: Springer
Date Deposited: 17 Feb 2021 10:48
Last Modified: 27 Feb 2022 00:50
DOI or ID number: 10.1007/s12247-021-09536-7
Editors: Asadullah, A and Buchanan, C
URI: https://researchonline.ljmu.ac.uk/id/eprint/13126
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