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  • Title: Exendin-4 Loaded Nanoparticles with a Lipid Shell and Aqueous Core Containing Micelles for Enhanced Intestinal Absorption.
    Author: Chen C, Zhu X, Dou Y, Xu J, Zhang J, Fan T, Du J, Liu K, Deng Y, Zhao L, Huang Y.
    Journal: J Biomed Nanotechnol; 2015 May; 11(5):865-76. PubMed ID: 26349398.
    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.
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