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Preparation of adriamycin propanediol liposomes and its anti-tumor in vitro |
DAI Dandan1 CHEN Guanghui2 XU Ping1 |
1.Department of Pharmacy, Ningbo First Hospital, Zhejiang Province, Ningbo 315000, China;
2.Department of Pharmacy, People′s Hospital of Beilun, Zhejiang Province, Ningbo 315800, China |
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Abstract Objective To prepare a novel nano-alcoholic plastid-propylene glycol liposome, namely, adriamycin propanediol liposomes (A-PL) using adriamycin as a model drug and to investigate its anti-tumor effect in vitro. Methods A-PL glycol liposomes were prepared and their microscopic morphology, particle size and potential were observed by transmission electron microscopy, laser particle size analyzer and potentiometer. Human hepatoma cell line HepG-2 was used as the model cell line. The cytotoxicity of A-PL was examined by MTT assay. The uptake of A-PL by HepG-2 was observed by flow cytometry and inverted fluorescence microscopy. The function of P-glycoprotein (P-gp) was detected by rhodamine reagent. Results A-PL had a round appearance, good dispersion and no aggregation. The average particle size was 150 nm, the Zeta potential was -5.78 mV, and the encapsulation rate was 83.7%. The cytotoxicity of A-PL was significantly higher than that of adriamycin solution; A-PL could increase cell uptake of drugs. In addition, A-PL was easier to enter cells and had a strong affinity with the nucleus. A-PL could inhibit the overexpression of P-gp. Conclusion The A-PL prepared in this study overcomes the shortcomings of traditional liposome aggregation, has the advantages of stability and small particle size, and has good anti-tumor effect. The mechanism of action is mainly dependent on the strong endocytosis of A-PL and the inhibition of poloxamer on drug efflux pump.
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