丹参酮脂质体的药物渗漏和微粒聚结特性研究

Studies on Drug Leakage and Aggregation Behavior of Tanshinone Liposomes

考察了聚乙烯吡咯烷酮 (PVP)以及冻融处理对丹参酮脂质体的药物渗漏和微粒聚结特性的影响。结果表明 ,丹参酮脂质体在 4°C下贮存 3、6 .5个月后 ,未发现丹参酮有明显渗漏 ,处方中的 PVP和冻融处理对丹参酮的渗漏影响不明显 ;但 PVP可提高丹参酮脂质体微粒的聚结活化能 ,并使脂质体 ζ电位有所增大 ;脂质体混悬液在 4°C下贮存 3个月 ,不含 PVP的样品粒度明显增大 ,并出现分层现象 ,而含有 PVP的样品 ,其粒度变化甚微 ,混悬液均匀 ;

The effects of PVP in formulation and freeze thawing steps on drug leakage and aggregation of tanshinone liposomes were investigated. Results showed that little drug leakage was found after the liposomes being stored for 3 or 6.5 month at 4 °C , and the leakage phenomenon was nearly not affected by freeze thawing steps or PVP in the liposomes dispersion. Aggregation active energy and zeta potential of liposomes were increased by adding PVP. When the liposomes dispersions were stored for 3 months at 4 °C , the particle size of vesicles without PVP greatly increased, while nearly no change in particle size was found in liposomes with PVP, and the dispersion kept uniform. The aggregation active energy of liposomes was also increased by freeze thawing steps.