Advanced Search
YUAN Dong-fen, SUN Min-jie, WANG Yu, PING Qi-neng. Preparation and in vitro characterization of octreotide-targeting doxorubicin liposome[J]. Journal of China Pharmaceutical University, 2011, 42(3): 223-229.
Citation: YUAN Dong-fen, SUN Min-jie, WANG Yu, PING Qi-neng. Preparation and in vitro characterization of octreotide-targeting doxorubicin liposome[J]. Journal of China Pharmaceutical University, 2011, 42(3): 223-229.

Preparation and in vitro characterization of octreotide-targeting doxorubicin liposome

  • The aim of this study was to develop the preparation method of octreotide-targeting doxorubicin liposome.First,doxorubicin plain liposome (P-L) was prepared by ethanol injection and ammonium sulfate gradient loading,and optimized by single-factor design regarding formulation and pharmaceutical process.Then octreotide-targeting liposome (Oct-L) was obtained by post-inserting Octreotide-PEG4000-HSPE into prepared liposome.Sephadex G-50 column separation and zetasizer were used to evaluate drug entrapment efficiency,size distribution and storage stability; transmission electron microscopy was used to evaluate its surface morphology and dialysis method was used to investigate the drug release profile.It was shown that octreotide-targeting liposome had a mean size of 100 nm and a drug entrapment efficiency of 100%.The liposome particle was round and only 20% of entrapped doxorubicin was released after 48h incubation in pH 7.4 PBS under 37 °C.Compared to plain doxorubicin liposome,octreotide-targeting doxorubicin liposome showed stronger cytotoxicity and higher cellular uptake on NCI H-446 expressing somatostatin receptor.Therefore,ethanol injection,ammonium sulfate gradient loading and post-insertion method can be utilized to construct doxorubicin liposome and to achieve octreotide targeting modification.
  • loading

Catalog

    Turn off MathJax
    Article Contents

    /

    DownLoad:  Full-Size Img  PowerPoint
    Return
    Return