重组α-2b干扰素缓释微囊制备工艺及体外释药过程研究

Study on the Preparation of Recombinant Human α-2b Interferon Slowly Realeasing Microcapsules and its in-vitro Release Properties

以聚乳酸乙醇酸(PLGA)为囊材,对制备a-2b干扰素缓释微囊的工艺条件进行优化,研究了不同PLGA浓度、搅拌速度和搅拌时间对缓释微囊粒径分布、载药量、包封率和体外释药过程的影响。结果显示,在PLGA浓度为0.7gmL-1,搅拌速度2100rmin-1,搅拌时间4min条件下,制备的微囊平均粒径为2.8721m ,表面平滑、形态规整且不聚集,载药量为3.91%,包封率为85.8%,体外可连续释药10天,没有明显突释效应,释药量达93.3%,符合临床药用标准。

The preparation condition of poly (D,L-lactide-co-glycolide) (PLGA) microcapsules and its in-vitro release properties was studied. a-2b interferon was encapsulated in PLGA microcapsules by using a water-in-oil-water solvent evaporation technique. The effect of PLGA concentration, stirring speed and stirring time on the average diameters, final loading, encapsulation efficiency, and in-vitro release properties of the microcapsules was investigated. Results indicate that the appropriate preparation conditions are 0.7gmL-1 PLGA, stirring speed at 2100 rmin-1 and stirring time for 4 minute. The obtained microcapsules with smooth surface and regular geometric shapes have a smaller size of 2.872 mm, carry 3.91% of the interferon and its encapsulation efficiency is 85.8%. The drug releasing in vitro proves that the PLGA microcapsules provide a continuous delivery of the active interferon for 10 days and the cumulative releasing rate is 93.3%. It is concluded that prepared PLGA microcapsules with entrapped a-2b interferon conform with the principles of clinical drug.