环磷酰胺脂质体(CPL)重建型的制备、重建后CPL的特性及抑瘤作用的研究

本文建立了一个对环磷酰胺(cyclophosphamide以下简称CP)具有较高包封率、制备过程中CP水解程度最小、其重建型(冻干态)能长期贮存的CPL制备新工艺—SLV(sonication—lyo philization—vesicle)法。制备过程中CP的损失量为4.34%。CP的包封率达50%以上。MPVⅢ—TAS显微分光图象仪对重建的CPL(CPRL)的粒度测定表明,平均粒径为0.689μm。CPRL的LD₅₀以及对S₁₈₀,EAC,LL三个瘤株的抑瘤结果显示,CPRL降低了CP的毒性、提高了其抑瘤活性。

THE PREPARATION OF LIPOSOME ENTRAPMENT OF CYC LOPHOSPHAMIDE(CPL) IN ITS RECONSTITUTED FORM AND THE PROPERTIES AND ANTITUMOR ACTIVITIES OF RECONSTITUTED CPL

In this study, a new procedure of preparing CPL is established. It is the SLV (sonication-lyophilization-vesicle) method. It is capable of entrapping a large proportion of water-soluble materials and make it minimal for cyclophosphamide (CP) to hydrolyze. CPL can be stored for a long time in the reconstituted form (lyophilized state). The loss of CP during preparation of CPL by SLV method is 4.34%. The encapsulation efficiency of CP is over 50%. The particle size distribution of reconstituted CPL (CPRL) was determined by MPV Ⅲ-TAS. The average particle size is 0.689 μm. The results of LD₅₀ and antitumor activities of CPRL on S₁₈₀, LL, EAC show that CPRL has higher antitumor activity and lower toxicity.