【摘要】 目的:本研究将虾青素与抗癌药物盐酸阿霉素联合载入脂质体中，旨在制备一种抗肿瘤性能优于盐酸阿霉素脂质体的新型靶向纳米制剂。方法：研究中以不同药脂比和不同磷脂和胆固醇质量比制备了8种盐酸阿霉素与虾青素共载脂质体，分别测定了制剂的载药量、包封率、粒径、释药和肿瘤细胞毒性。结果：共载脂质体能够将水溶性药物都包裹于内层水相中。药脂比为1:10的共载脂质体载药量较高。8种共载脂质体均具有纳米粒径。细胞毒性实验结果表明虾青素在递药过程中辅助盐酸阿霉素产生抗肿瘤毒性，4号盐酸阿霉素与虾青素共载脂质体的细胞毒性最强。结论：当磷脂用量多时，胆固醇的用量高不利于两种药物的共同载入；通常情况下，当磷脂用量一定时，胆固醇用量越低，盐酸阿霉素和虾青素从脂质体内相中释放的阻力越小，释放速度越快；盐酸阿霉素与虾青素共载脂质体的细胞毒性主要取决于载药量以及盐酸阿霉素的释放量。本研究为盐酸阿霉素的联合载药脂质体研发提供了新思路。更多还原

【Abstract】 Objective:In this study,astaxanthin and doxorubicin hydrochloride were combined into liposomes to prepare a novel targeted nanoagent with better antitumor performance than doxorubicin hydrochloride liposomes.Methods:8 kinds of adriamycin hydrochloride and astaxanthin co-loaded liposomes were prepared with different drug/lipid ratios and different phospholipid/cholesterol mass ratios.The drug loading,encapsulation rate,particle size,drug release and tumor cytotoxicity of the preparation were determined.Results:The results showed that coliposomes could encapsulate watersoluble drugs in the inner water phase.Coliposomes with drug to lipid ratio of 1:10 had higher drug loading capacity.The eight co-liposomes all had nano-particle sizes.Cytotoxicity experiments showed that astaxanthin assisted adriamycin hydrochloride to produce antitumor toxicity during drug delivery,and the cytotoxicity of adriamycin hydrochloride and astaxanthin co-loaded liposomes was the strongest.Conclusion:When the amount of phospholipid is high,the amount of cholesterol is high,which is not conducive to the co-loading of the two drugs;Generally,when the amount of phospholipid is constant,the lower the amount of cholesterol,the less resistance doxorubicin hydrochloride and astaxanthin release from liposomes,the faster the release rate;The cytotoxicity of adriamycin hydrochloride and astaxanthin co-loaded liposomes mainly depends on drug loading and release of adriamycin hydrochloride.This study provided a new idea for the development of adriamycin hydrochloride combined liposome.更多还原