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目的:制备新型癌症化疗制剂载阿霉素(Adriamycin)、聚乳酸-羟基乙酸共聚物(PLGA)纳米微球(ADM-PLGA-NP),研究其性质及体外释药特点。方法:以聚乳酸-羟基乙酸共聚物为包封材料,阿霉素为模型药物,采用复乳蒸发法制备ADM-PLGA-NP,扫描电镜观察微球形态,激光粒度分析仪检测粒径分布,紫外分光光度法计算载药率及包封率,体外药物释放实验考察微球对ADM的缓释作用。结果:ADM-PLGA-NP外观呈球形,平均粒径约(237±12.7)nm,载药量及包封率分别为(6.42±1.67)%和(53.82±8.34)%,药物在体外缓慢释放,5 d累积释放量达85%。结论:通过复乳蒸发法制备的ADM-PLGA-NP性质稳定,具有药物缓释性,有望成为一种新型的药物化疗载体。
OBJECTIVE: To prepare novel cancer chemotherapeutic agents containing Adriamycin and PLGA nanospheres (ADM-PLGA-NP) and study their properties and in vitro release characteristics. METHODS: ADM-PLGA-NP was prepared by double emulsion evaporation with polylactic-co-glycolic acid as encapsulating material and doxorubicin as model drug. Morphology of microspheres was observed by scanning electron microscopy. Particle size distribution was detected by laser particle size analyzer. The drug-loading rate and entrapment efficiency were calculated by ultraviolet spectrophotometry. The in vitro drug release test was used to investigate the sustained-release effect of microspheres on ADM. Results: The appearance of ADM-PLGA-NP was spherical with an average size of (237 ± 12.7) nm and drug loading and entrapment efficiency of (6.42 ± 1.67)% and (53.82 ± 8.34)%, respectively. , 5 d cumulative release of 85%. CONCLUSION: ADM-PLGA-NP prepared by double emulsion evaporation is stable in nature and has drug-controlled release properties. It is expected to become a new type of drug and chemotherapy carrier.