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目的制备阿霉素聚酰胺-胺树状大分子脂质体包覆物(LLDs-PAMAM-DOX),并对制剂性质进行评价。方法采用逆向蒸发结合pH梯度法制备LLDs-PAMAM-DOX,观察形态,测定粒径分布及zeta电位;采用凝胶柱-UV法测定包封率;采用透析法测定体外释药;采用MTT法,考察其对人乳腺癌细胞MCF-7的细胞毒作用。结果LLDs-PAMAM-DOX的粒径约为80~120nm;zeta电位约为22.5~32.4mV;包封率大于85%,缓释作用明显。LLDs-PAMAM-DOX呈剂量依赖性抑制肿瘤细胞的生长,对MCF-7的抑制作用明显优于普通脂质体L-DOX。结论聚酰胺-胺树状大分子脂质体包覆物(LLDs-PAMAM)作为阿霉素(doxorubicin,DOX)的载体,具有较好的缓释作用及良好的抑制肿瘤细胞作用,有望成为一种有潜力的新型药物载体。
Objective To prepare doxorubicin polyamidoamine dendrimer (LLDs-PAMAM-DOX) and evaluate its properties. Methods LLDs-PAMAM-DOX was prepared by reverse-phase evaporation combined with pH gradient method. Morphology, particle size distribution and zeta potential were measured. The encapsulation efficiency was determined by gel column-UV method. The drug release in vitro was determined by dialysis method. Investigate its cytotoxic effect on human breast cancer cells MCF-7. Results The particle size of LLDs-PAMAM-DOX was about 80-120 nm. The zeta potential was about 22.5-32.4 mV. The entrapment efficiency was greater than 85% and the sustained-release effect was obvious. LLDs-PAMAM-DOX inhibited the growth of tumor cells in a dose-dependent manner, and the inhibitory effect of LLDs-PAMAM-DOX on MCF-7 was better than that of L-DOX. Conclusions Polyamidoamine dendrimer (LLDs-PAMAM), a carrier of doxorubicin (DOX), has a good sustained-release effect and a good inhibitory effect on tumor cells and is expected to become a Potential new drug carrier.