Long-Acting Release Microspheres Containing Novel GLP-1 Analog as an Antidiabetic System

Molecular Pharmaceutics
Sida RuanTing Cai

Abstract

Glucagon-like peptide 1 (GLP-1) has recently received significant attention as an efficacious way to treat diabetes mellitus. However, the short half-life of the peptide limits its clinical application in diabetes. In our previous study, a novel GLP-1 analog (PGLP-1) with a longer half-life was synthesized and evaluated. Herein, we prepared the PGLP-1-loaded poly(d,l-lactide- co-glycolide) microspheres to achieve long-term effects on blood glucose control. The incorporation of zinc ion into the formulation can effectively decrease the initial burst release, and a uniform drug distribution was obtained, in contrast to native PGLP-1 encapsulated microspheres. We demonstrated that the solubility of the drug encapsulated in microspheres played an important role in in vitro release behavior and drug distribution inside the microspheres. The Zn-PGLP-1 microspheres had a prominent acute glucose reduction effect in the healthy mice. A hypoglycemic effect was observed in the streptozotocin (STZ) induced diabetic mice through a 6-week treatment of Zn-PGLP-1-loaded microspheres. Meanwhile, the administration of Zn-PGLP-1 microspheres led to the β-cell protection and stimulation of insulin secretion. The novel GLP-1 analog-loaded sustained...Continue Reading

References

May 1, 1990·Journal of Biomedical Materials Research·J M SchakenraadP Nieuwenhuis
Aug 15, 1998·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·G Reich
Apr 22, 1999·Journal of Controlled Release : Official Journal of the Controlled Release Society·R V DiazC Evora
Dec 22, 1999·Endocrine Reviews·T J Kieffer, J F Habener
Jul 11, 2002·Journal of Controlled Release : Official Journal of the Controlled Release Society·Cory BerklandDaniel W Pack
Apr 25, 2003·Journal of Controlled Release : Official Journal of the Controlled Release Society·Meng ShiJorge Heller
Jul 26, 2003·Pharmaceutical Research·Cory BerklandDaniel W Pack
Jul 29, 2003·Journal of Pharmaceutical Sciences·Karen FuRobert Langer
Dec 20, 2003·Journal of Controlled Release : Official Journal of the Controlled Release Society·Gesine SchlieckerThomas Kissel
Apr 6, 2004·Journal of Controlled Release : Official Journal of the Controlled Release Society·J SiepmannJ P Benoit
Dec 14, 2004·Journal of Controlled Release : Official Journal of the Controlled Release Society·Lei Li, Steven P Schwendeman
Jan 18, 2005·Journal of Controlled Release : Official Journal of the Controlled Release Society·Alexis FrankSubbu S Venkatraman
May 24, 2005·Journal of Controlled Release : Official Journal of the Controlled Release Society·Jing ZengXiabin Jing
Mar 1, 2006·International Journal of Pharmaceutics·D KloseJ Siepmann
Mar 3, 2006·International Journal of Pharmaceutics·N FaisantJ Siepmann
Jan 2, 2007·International Journal of Pharmaceutics·Shirui MaoThomas Kissel
Apr 17, 2007·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·F TewesI Chourpa
Jul 24, 2007·Journal of Controlled Release : Official Journal of the Controlled Release Society·Banu S Zolnik, Diane J Burgess
Dec 7, 2007·International Journal of Pharmaceutics·D KloseJ Siepmann
Feb 20, 2008·Journal of Controlled Release : Official Journal of the Controlled Release Society·Banu S Zolnik, Diane J Burgess
Jun 6, 2008·Expert Opinion on Drug Delivery·S Dean Allison
May 19, 2009·International Journal of Pharmaceutics·Feng QianRonald L Smith
Nov 10, 2009·Diabetes Research and Clinical Practice·J E ShawP Z Zimmet
May 25, 2010·Journal of Controlled Release : Official Journal of the Controlled Release Society·Mingli YeKinam Park
Jun 7, 2011·International Journal of Pharmaceutics·Susanne FredenbergAnders Axelsson
Oct 25, 2011·Journal of Controlled Release : Official Journal of the Controlled Release Society·Juergen Siepmann, Florence Siepmann
Feb 23, 2012·Journal of Controlled Release : Official Journal of the Controlled Release Society·Fabienne DanhierVéronique Préat
Mar 15, 2012·The Journal of Endocrinology·Zhengu LiuJoel F Habener
May 4, 2013·ACS Nano·Zhen GuDaniel G Anderson
Sep 15, 2014·Journal of Controlled Release : Official Journal of the Controlled Release Society·Guanghui Ma
Sep 16, 2014·Journal of Controlled Release : Official Journal of the Controlled Release Society·Ronak B Shah, Steven P Schwendeman

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Citations

Aug 30, 2018·Langmuir : the ACS Journal of Surfaces and Colloids·Piotr MazurekAnne L Skov
Jul 8, 2020·Current Pharmaceutical Design·Somaraju R KumarUsha Y Nayak

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