Preparation of sustained-release microspheres containing exenatide and their in vitro release / 第二军医大学学报

ABSTRACT

Objective: To prepare exenatide-loaded poly (lactic-co-glycolicacid)(PLGA) microspheres and to evaluate their release behavior in vitro. Methods: Exenatide-loaded PLGA microspheres were prepared by W/O/O method using PLGA as vectors. An HPLC approach was established to determine the content and in vitro cumulative release. The physicochemical characteristics of microspheres, including the mean diameter, morphology, drug entrapment efficiency and loading efficiency, were evaluated. Results: The prepared microspheres were well-shaped, with a mean diameter of (51.2±1.97) μm. The drug loading was (4.50±0.13)% and the encapsulation efficiency was (96.5±2.68)%. The first day burst release was (13.19 ± 1.39)% and the in vitro 28-day-cumulative-release was (88.6 ± 0.73)%. Conclusion: The W/O/O method is stable, controllable, and repeatable for preparing exenatide-loaded microspheres using biodegradable polymers PLGA as the vector; the microspheres yield a one-month continuous release and have a bright future in treatment of diabetes mellitus.