重组水蛭素乳酸－羟基乙酸共聚物微球的制备及体外释放的考察

Objective: To make recombinant hirudin-2 (rHV2) poly( lactic-co-glycolic acid) (PLGA) microspheres and rHV2 PLGA microspheres coated with Eudragit L100-55 to reduce the degradation in the gastro-intestinal (GI) tract for them. Methods: Evaporation method based on the formation of double emulsion W/O/W was adopted to prepare rHV2 microspheres, and the morphology, particle size and in vitro release of microspheres were investigated. Results: The mean diameter of PLGA microspheres prepared was 31.45 μm. The rHV2 contents, drug loading and entrapment rate of PLGA microspheres were 2.92±0.15 mg, 3.01±0.16 mg, and 75.25±4.01 % respectively. The mean diameter of PLGA microspheres coated with Eudragit L100-55 was 31.45 μm. The rHV2 contents, drug loading and entrapment rate of PLGA microspheres coated with Eudragit L100-55 were 3.00±0.10 mg, 3.09±0.08 mg, and 76.17±2.84 % respectively. The release experiments of two types of rHV2 microspheres were identical, and the release amount arrived at 70% in 60 minutes and 90% after 6 hours.