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Yao xue xue bao = Acta pharmaceutica Sinica 2002-Jan

[Studies on the preparation of camptothecin niosomes].

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Li-biao Luan
Jia-bi Zhu
Wei-ping Yu
Kai-bin Wei

Keywords

Abstract

OBJECTIVE

To study the non-ion surfactant vehicle (niosome) entrapped-camptothecin.

METHODS

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.

RESULTS

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.

CONCLUSIONS

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.

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