Luan Li-biao, Zhu Jia-bi, Yu Wei-ping, Wei Kai-bin
Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China.
Yao Xue Xue Bao. 2002 Jan;37(1):59-62.
To study the non-ion surfactant vehicle (niosome) entrapped-camptothecin.
The niosome loaded with camptothecin was prepared from Span and cholesterol using aqueous dispersion of film. The vehicles were visualised by transmission electron microscopy and sized by laser particle analyzer on a Malvern Mastersizer. An HPLC analysis method of the camptothecin was established by fluorescence detection. The entrapment efficiency of the niosomes containing camptothecin was determinated after the ultracentrifugation of the niosome. The antitumor activities of the vehicles on S180 sarcoma in mouse were studied.
The given niosomes were the suspension finely dispersed in aqueous solution. They were spherical vehicles with the single lamellar bilayers similar to phospholipid vehicles. The mean sizes of the vehicles were (565 +/- 6) nm. The recovery of the HPLC analysis method was 100.3% with 0.4% RSD. The entrapment efficiency of the camptothecin encapsulated by the niosome was 61%. The inhibition (%) of the niosome loaded with camptothecin on S180 sarcoma in mouse were 76.1% (P < 0.05). After the given dose the weight of the mouse of the niosome groups were 92.7% (P > 0.05) and 134.7% of blank control groups and compatothecin solution groups, respectively.
The camptothecin niosomes were spherical in shape and similar to phospholipid vehicles with singlelamellar bilayers. Their size distributions were narrow. Their entrapment efficiency were higher. Its antitumor activity was better than camptothecin.
研究非离子表面活性剂载体(脂质体)包裹的喜树碱。
采用薄膜水分散法,由司盘和胆固醇制备负载喜树碱的脂质体。通过透射电子显微镜观察载体,并使用马尔文粒度分析仪对其进行粒径分析。建立了采用荧光检测的喜树碱高效液相色谱分析方法。对脂质体进行超速离心后,测定含喜树碱脂质体的包封率。研究了该载体对小鼠S180肉瘤的抗肿瘤活性。
所制脂质体为均匀分散于水溶液中的混悬液。它们是具有类似于磷脂载体的单层双分子层的球形载体。载体的平均粒径为(565±6)nm。高效液相色谱分析方法的回收率为100.3%,相对标准偏差为0.4%。脂质体包裹喜树碱的包封率为61%。负载喜树碱的脂质体对小鼠S180肉瘤的抑制率为76.1%(P<0.05)。给药后,脂质体组小鼠体重分别为空白对照组和喜树碱溶液组的92.7%(P>0.05)和134.7%。
喜树碱脂质体呈球形,类似于具有单层双分子层的磷脂载体。其粒径分布窄。其包封率较高。其抗肿瘤活性优于喜树碱。