In vitro and in vivo delivery of gliclazide loaded mPEG-PCL micelles and its kinetic release and solubility study. (17th November 2018)

• Record Type: Journal Article
• Authors: Danafar, Hossein; Jaberizadeh, Hoda; Andalib, Sina
• Is Part Of: Artificial cells, nanomedicine, and biotechnology. Volume 46:Number 8(2018)
• Page Start: 1625
• Page End: 1636
• Publication Date: 2018-11-17
• Subjects: Copolymer -- sustained release -- micelles -- gliclazide; Artificial cells -- Periodicals; Nanotechnology -- Periodicals; Blood substitutes -- Periodicals; Tissue engineering -- Periodicals; Molecules -- Periodicals; Biotechnology -- Periodicals; 615.39
• DOI: 10.1080/21691401.2017.1386191
• Languages: English
• ISSNs: 2169-1401

Abstract

Abstract: In this study, drug delivery system of gliclazide, a poorly soluble drug, was developed and evaluated in vitro and in vivo . We synthesized five series of mPEG-PCL di block copolymers. The structure of the copolymers was characterized by 1 H-NMR, Fourier transform infrared spectroscopy (FT-IR), differential scanning calorimetry (DSC) and gel permeation chromatography (GPC) techniques. In this study, gliclazide was encapsulated within micelles through a single-step nano-precipitation method, leading to formation of gliclazide/mPEG-PCL micelles. The resulting micelles were characterized further by various techniques such as DLS and AFM. The serum glucose lowering effect of gliclazide micelles was studied in streptozotocin-diabetic rats and were compared with the gliclazide treated rats. The results showed that the zeta potential of micelles was about −14.9 mV and the average size was 83.12 nm. Gliclazide was encapsulated into mPEG-PCL micelles with loading capacity of 21.05 ± 0.14% and entrapment efficiency of 94.11 ± 0.12%. In vivo testing of the gliclazide micelles in diabetic rats demonstrated a significant antidiabetic effect of gliclazide micelles after the 7 day that lasted for 21 days when compared with gliclazide powder. The results suggest that gliclazide micelles are a valuable system for the sustained delivery of gliclazide.