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本文探讨了提高MTX脂质体包裹率、影响它对热稳定性的因素,并自行设计了简便、迅速、重现性好的测定MTX脂质体的方法。结果表明:采用二次乳化蒸发法制备MTX脂质体,在控制乳化温度及有机相比例的条件下,可获得50％左右较高的包裹率。另外提示,脂质体分散溶媒的离子强度和脂质体中胆固醇的含量是影响MTX脂质体对热稳定性的重要因素。以选用50mM的磷酸盐缓冲液为分散溶媒和PC/CHOL/SA的脂质体组成,则100℃加热30分钟灭菌,所包MTX可滞留90％。且灭菌前后的脂质体经电镜观察形态无明显变化。
This article explores the factors that increase the encapsulation efficiency of MTX liposomes and affect its thermal stability, and has designed a simple, rapid and reproducible method for the determination of MTX liposomes. The results showed that the MTX liposomes prepared by the secondary emulsification evaporation method could obtain a higher encapsulation efficiency of about 50% under the condition of controlling the emulsifying temperature and the proportion of the organic phase. Additionally, it is suggested that the ionic strength of the liposome-dispersed solvent and the cholesterol content in the liposomes are important factors that affect the thermal stability of the MTX liposomes. When 50 mM phosphate buffer was used as the dispersion medium and the liposome composition of PC / CHOL / SA, it was sterilized by heating at 100 ° C. for 30 minutes, and the MTX contained therein could be retained by 90%. The liposomes before and after sterilization had no obvious morphological changes by electron microscopy.