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采用微乳液法制备了可包载脂溶性和水溶性药物的羧甲基壳聚糖十八烷基季铵盐(OQCMC)乙醇脂质体,研究了OQCMC乙醇高分子脂质体的相图、粒径和电位、对药物的包封及释放能力及共载水溶性和脂溶性荧光染料后的细胞内递送能力.结果表明:OQCMC上长链季铵盐分子的取代度和共乳化剂乙醇的加入量对相图中微乳区域的面积影响不大;微乳液法可制备包载水溶性长春新碱(VCR)、脂溶性消炎痛(IMC)或二者共载的OQCMC载药微球,微球粒径为(52.40±0.55)nm,分布均匀;微乳液体系对VCR的最大载药率为22.7%,对IMC的最大载药率为20.1%,二者共载时,VCR的最大载药率为12.2%,IMC的最大载药率为10.0%;载药微球对药物具有缓控释功能.OQCMC乙醇高聚物脂质体可有效地包载荧光染料异硫氰酸荧光素FITC(水溶性)和尼罗红(脂溶性),并将二者递送到卵巢癌HO8901细胞内.
The liposomes of lipidic and water-soluble drug-loaded octadecyl quaternary ammonium salt (OQCMC) were prepared by microemulsion method. The phase diagram of OQCMC ethanolic polymer liposomes was studied. Particle size and potential, drug encapsulation and release ability and intracellular delivery ability of water-soluble and fat-soluble fluorescent dye.The results showed that the degree of substitution of long chain quaternary ammonium salt molecule and the co-emulsifier ethanol The microemulsion method can be used to prepare VQ, liposoluble indomethacin (IMC) or OQCMC drug loaded microspheres co-loaded with the microemulsion, The diameter of microspheres was (52.40 ± 0.55) nm, and the distribution was uniform. The maximum loading rate of VCR in microemulsion system was 22.7% and the maximum loading rate of IMC was 20.1% The drug-loading rate was 12.2% and the maximum drug loading rate of IMC was 10.0%. The drug-loaded microspheres had a controlled release function for the drug.OQCMC ethanol-polymer liposomes could effectively encapsulate the fluorescent dye fluorescein isothiocyanate FITC (Water-soluble) and Nile red (liposoluble), and both were delivered to ovarian cancer HO8901 cells.