胶原-壳聚糖载硫酸长春新碱微球缓释药膜的研究

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目的本研究制备载硫酸长春新碱(vincristinesulfate,VCR)微球的胶原-壳聚糖缓释药膜。并考察加入壳聚糖对药膜性质的影响。选定适当的胶原壳聚糖比例制备药膜。方法采用W/O/O溶剂挥发法制备VCR的聚乳酸-羟基乙酸(poly(lactic-co-glycolicacid),PLGA)微球,并对微球性质表征,采用二次冻干法制备载VCR微球的胶原-壳聚糖药膜,对药膜的表面形态、降解性质、热力学性质及释放性质进行表征,并与释放2周后的药膜进行比较。采用高效液相法分析药物含量。结果VCR制成PLGA微球后再制备成药膜,可达到双重缓释的作用,明显减少药物突释,并延缓药物释放。添加了壳聚糖的药膜降解速度明显小于单纯的胶原药膜。在体外释放实验中,微球突释为(27.2±1.2)%,而胶原药膜的突释为(20.4±1.9)%,胶原与壳聚糖比例为9∶1、4∶1、3∶2的药膜突释分别为(20.2±2.1)%、(18.0±1.1)%和(16.3±1.8)%。结论胶原壳聚糖载VCR的缓释药膜能不同程度减少药物的突释,使药物释放更加平稳缓慢,优于单纯的胶原药膜。 OBJECTIVE: To prepare collagen-chitosan sustained-release membrane containing vincristine sulfate (VCR) microspheres. The effects of adding chitosan on the properties of the film were also investigated. Select the appropriate proportion of collagen chitosan prepared membrane. Methods VCR poly (lactic-co-glycolic acid) (PLGA) microspheres were prepared by W / O / O solvent evaporation method. The properties of the microspheres were characterized by secondary freeze-drying. Ball of collagen - chitosan membrane, the membrane surface morphology, degradation properties, thermodynamic properties and the nature of the release were characterized and compared with the release of two weeks after the film. High-performance liquid chromatography analysis of drug content. Results VCR made of PLGA microspheres and then prepared into a film, can achieve the dual release of sustained release, significantly reduce the drug burst, and delay the release of drugs. The degradation rate of the chitosan-added membrane was significantly lower than that of the pure collagen membrane. In in vitro release experiments, the microspheres burst was (27.2 ± 1.2)%, while the burst of collagen membrane was (20.4 ± 1.9)%, the ratio of collagen to chitosan was 9:1, 4:1, 3: 2 were (20.2 ± 2.1)%, (18.0 ± 1.1)% and (16.3 ± 1.8)%, respectively. CONCLUSION: The sustained-release membrane coated with collagen chitosan loaded VCR can reduce the burst of drug to some extent, and release the drug more smoothly and slowly, which is better than simple collagen membrane.
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