幽门螺杆菌重组蛋白PLGA微球和PLGA-壳聚糖复合微球的制备及其释放性能研究

陈昱作; 刘人捷; 杨露; 李茂圆; 索朗斯珠; 李婉宜; 王保宁

doi:10.12182/20210960208

幽门螺杆菌重组蛋白PLGA微球和PLGA-壳聚糖复合微球的制备及其释放性能研究

Preparation and Release Properties of Helicobacter pylori Recombinant Protein PLGA Microspheres and PLGA-Chitosan Microspheres

摘要

摘要:
目的制备载有幽门螺杆菌重组蛋白（BIB蛋白）的聚乳酸-羟基乙酸共聚物（poly lactic-co-glycolic acid, PLGA）微球和PLGA-壳聚糖复合微球，优化微球制备参数，并分析两种微球在体外胃、肠液中的释放性能。
方法采用双乳化-溶剂挥发法（W1/O/W2）制备BIB-PLGA微球和BIB-PLGA-壳聚糖复合微球；通过单因素分析方法，研究水相/油相（W1/O）比例、PLGA质量分数、聚乙烯醇（polyvinyl alcohol, PVA）浓度等对微球外观、粒径、分散指数（polydispersity index, PDI）、包封率和载药率的影响，确定最优参数，采用BCA法测定蛋白浓度，计算微球累计释放率。
结果本研究的最佳参数条件为：W1/O为1∶2，PLGA质量分数5%，PVA质量分数0.2%。BIB-PLGA微球包封率（78.20±1.73）%，载药率（10.58±0.23）%，粒径（2.11±0.08） μm，PDI（0.35±0.18）；BIB-PLGA-壳聚糖复合微球包封率（78.87±1.30）%，载药率（15.50±0.25）%，粒径（2.28±0.52） μm，PDI（0.39±0.54）。BIB-PLGA微球和BIB-PLGA-壳聚糖复合微球在体外胃、肠液中均能缓慢释放，BIB-PLGA-壳聚糖复合微球的缓释效果更明显。
结论采用双乳化-溶剂挥发法制备的BIB-PLGA微球和BIB-PLGA-壳聚糖复合微球载药率和包封率都较高，粒径可控，外观分散，对胃肠液有缓释作用。

Abstract:
Objective To preparethe poly lactic-co-glycolic acid (PLGA) microspheres and PLGA-chitosan microspheres containing Helicobacter pylori recombinant protein, namely the BIB protein, and to explore their optimal preparation parameters and in vitro release performance in gastric and intestinal fluids.
Methods Double emulsions (water-in-oil-in-water, or W1/O/W2) solvent evaporation method was used to prepare the BIB-PLGA microspheres and the BIB-PLGA-chitosan microspheres. Univariate analysis was done to study the impact of the water-to-oil ratio (W1/O), PLGA mass fraction and PVA concentration on the morphology, particle size, polydispersity index (PDI), encapsulation efficiency (EE), and drug loading (DL) so as to identify the optimal parameters. Bicinchoninic acid (BCA) assay was used to determine the protein concentration and the release efficiency of BIB.
Results The optimal preparation parameters identified in the study were as follows: W1/O at 1∶2, PLGA mass fraction at 5%, and PVA mass fraction at 0.2%. The BIB-PLGA microspheres were found to be (2.11±0.08) μm in particle size, 0.35±0.18 in PDI, (78.20±1.73)% in EE and (10.58±0.23)% in DL. The BIB-PLGA-chitosan microspheres were (2.28±0.52) μm in particle size, 0.39±0.54 in PDI, and (78.87±1.30)% and (15.50±0.25)% in EE and DL, respectively. Both BIB-PLGA microspheres and BIB-PLGA-chitosan microspheres showed slow-release property in gastric and intestinal fluids in vitro, with BIB-PLGA-chitosan microspheres showing better slow-release performance.
Conclusion The BIB-PLGA microspheres and BIB-PLGA-chitosan microspheres prepared with the double emulsions solvent evaporation method showed high DL and EE, controllable particle sizes, dispersive appearance, and slow-release property in gastric and intestinal fluids in vitro.

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