In vivo tumor-suppressing efficacy and cell internalization of doxorubicin loaded in liposomes bearing folate

In vivo tumor-suppressing efficacy and in vitro cell internalization of doxorubicin (DOX) loaded in liposome bearing folate were investigated using tumor-induced nude mice and a cancer cell. The size of liposomes was 105 nm–240 nm in diameter and they were multi-lamellar vesicles. Neither the attachment of folate nor the loading of DOX had an effect on the size and the structure. However, the attachment of folate led to decrease in the surface potentials. The specific loading of DOX in folate-free liposomes and folate-decorated liposomes was 0.0041 (w/w) and 0.0043 (w/w), respectively. During 24 h release experiment, the amount of DOX released from folate-decorated liposomes was more than that of DOX from folate-free liposomes. The tumor growth-suppressing effect was greater in the order of folate-decorated liposomes containing DOX > folate-free liposomes containing DOX > free DOX. Moreover, the histological examination on TEM also revealed folate-decorated liposomes were more efficacious in suppressing tumor growth. Confocal laser scanning microscopy and flow cytometric analysis showed that DOX loaded in folate-decorated liposomes was internalized into human mouth epidermal carcinoma more efficiently than DOX loaded in folate-free liposomes and free DOX.

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