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目的制备牛血清白蛋白(BSA)口服阳离子微球,考察天然阳离子物质壳聚糖(CHS)的加入对蛋白微球的粒径、电动电势、包封率、载药量及体外释放情况的影响。方法以乳酸/羟基乙酸共聚物(PLGA)和壳聚糖(CHS)为载体材料,采用W/O/W复乳-溶剂挥发法制备牛血清白蛋白乳酸/羟基乙酸共聚物-壳聚糖(PLGA/CHS)阳离子微球。通过正交设计优化制备工艺,确定最佳处方。建立准确而简便的蛋白含量测定方法,并对微球进行体外评价。结果最佳处方为:BSA浓度为150g·L-1、PLGA浓度为8%、外水相体积为80mL、壳聚糖浓度为0.2%。制得的微球形态圆整,平均粒径为(6.9±5.5)μm,为表面荷正电的阳离子微球[ζ电势=(10.0±0.6)mV],包封率为(75.4±4.6)%,载药量为(9.3±0.2)%。体外释放结果表明,在模拟胃液和模拟肠液中,壳聚糖的加入均能减少突释,延缓药物的释放。结论与PLGA微球相比,制得的PLGA/CHS阳离子微球表面带正电,具有较高的包封率和载药量,可以延缓药物释放,同时减少突释现象。
Objective To prepare bovine serum albumin (BSA) oral cationic microspheres and study the effect of natural cationic substance chitosan (CHS) on the particle size, electromotive potential, encapsulation efficiency, drug loading and in vitro release of protein microspheres . Methods Lactic acid / glycolic acid copolymer (PLGA) and chitosan (CHS) were used as carrier materials to prepare bovine serum albumin (LBAA) / chitosan PLGA / CHS) cationic microspheres. Optimize the preparation process through orthogonal design to determine the best prescription. The establishment of accurate and simple method for the determination of protein content, microspheres and in vitro evaluation. Results The best prescription was BSA concentration of 150g · L-1, PLGA concentration of 8%, outer aqueous phase volume of 80mL and chitosan concentration of 0.2%. The average diameter of the microspheres was (6.9 ± 5.5) μm, which was the positive charged cationic microspheres [ζ potential = (10.0 ± 0.6) mV] and the entrapment efficiency was (75.4 ± 4.6) %, Drug loading (9.3 ± 0.2)%. In vitro release results show that in the simulated gastric juice and simulated intestinal fluid, the addition of chitosan can reduce the burst release, delay the release of drugs. CONCLUSION: Compared with PLGA microspheres, PLGA / CHS cationic microspheres possessed positive charge, high entrapment efficiency and drug loading, which could delay drug release and reduce burst release.