Exendin-4 Loaded Nanoparticles with a Lipid Shell and Aqueous Core Containing Micelles for Enhanced Intestinal Absorption

Journal of Biomedical Nanotechnology
Chunhui ChenYuan Huang

Abstract

The purpose of this study was to formulate nanoparticles with an elaborate structure for oral delivery of exendin-4 using a simple preparation process. The nanoparticles possessed a mixed lipid shell and an aqueous core which contained drug-loaded micelles. Formulation was optimized by a central composite design and the structure of the nanoparticles was validated. The efficacy for delivery of exendin-4 was evaluated both in vitro and in vivo. The drug encapsulation efficiency of the nanoparticles reached 97.7%. The nanoparticles greatly enhanced the cellular uptake and transport of encapsulated exendin-4 in vitro. The in situ study showed that exendin-4 could be transported across the epithelium into intestinal capillaries, while the lipid materials largely remained in the epithelium. Pharmacodynamic studies in diabetic KKAy mice demonstrated that the exendin-4-loaded nanoparticles exhibited a marked hypoglycemia effect with a pharmacological availability of 12.7% after intestinal administration.

Citations

Oct 30, 2016·Drug Discovery Today·Jianping QiWei Wu
Jun 16, 2017·ACS Applied Materials & Interfaces·Fei XiaWei Wu
Jun 22, 2019·Advanced Materials·Matilde Durán-LobatoMaría José Alonso
Jan 15, 2021·Drug Discovery Today·Sunil Kumar DubeyPrashant Kesharwani
Feb 28, 2018·ACS Applied Materials & Interfaces·Yining XuYuan Huang

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