具有温敏释放特性的钙黄绿素复合磷脂脂质体的处方优化

Optimization of the Prescription of Calcein-Loaded Novel Temperature-Sensitive Liposomes

目的优化复合磷脂温敏脂质体的处方组成。方法采用薄膜水化法制备不同磷脂组成二棕榈酰磷脂酰胆碱-溶血磷脂-二硬脂酰乙醇胺-聚乙二醇2000(DPPC-MSPC-DSPE-PEG2000)=86:10:4;F(20%氢化大豆磷脂+80%二棕榈酰磷脂酰胆碱)-溶血磷脂-(二硬脂酰乙醇胺-聚乙二醇2000)=92:4:4的钙黄绿素温敏脂质体,并利用钙黄绿素的荧光自淬灭特性,比较两者在各自相变温度(T_m)以及37℃(正常体温)下的释放行为。结果与经典温敏脂质体相比,基于复合磷脂技术制备的温敏脂质体在溶血磷脂用量减少了60%的条件下,仍可以实现良好的温敏释放性能,且其在37℃时对药物的包封更加稳定。结论用复合磷脂技术有助于增强温敏释放效果。

OBJECTIVE To optimize the prescription of the novel temperature-sensitive liposomes（NTSL）. METHODS Cal- cein-loaded temperature-sensitive liposomes with different phospholipid composition （DPPC-MSPC-DSPE-PEG200 = 86： 10：4 and N （20% HSPC ＋ 80% DPPC）-MSPC-DSPE-PEG200 = 92： 4： 4） were prepared by the thin film -hydration method. Based on the fluores- cence self-quenching off characteristics of calcein, the release behavior of the above liposomes was compared when exposed to 37 ~C （normal temperature） as well as their respective phase transition temperature （ Tm ）. RESULTS Compared with the traditional tem- perature-sensitive liposomes（ TTSL）, the NTSL showed more favorable temperature-sensitive release performance and more stable en- capsulation ability to calcein, even with the amount of lysophospholipids was reduced by 60 percent. CONCLUSION The application of NTSL helps to enhance the effect of temperature-sensitive release.