Abstract��OBJECTIVE To construct a tumor-targeting and pH-sensitive lipoprotein-mimic nanocarrier containing paclitaxel(BSA-LC/DOPE-PTX)for effective antitumor therapy. METHODSIn vitro drug release study was conducted using dialysis method. The stability of BSA-LC/DOPE-PTX was studied by testing the aggregation of BSA-LC/DOPE-PTX in 50% human plasma. The cytotoxicity of drug-loaded nanocarrier against MCF-7 cells was evaluated by standard MTT assay. The subcellular localization and intracellular drug release behavior of BSA-LC/DOPE were evaluated by LSCM. RESULTSIn vitro drug release study demonstrated that paclitaxel(PTX)was released from BSA-LC/DOPE in a pH-dependent manner. The stability study showed that there was no significant change, suggesting that the coupling BSA could increase the stability in plasma. The cellular inhibition of BSA-LC/DOPE-PTX with BSA targeting agents was greater than that of LC/DOPE-PTX. BSA-LC/DOPE facilitated the capacity of endosomal escape, and rapidly released the loaded agents into the cytoplasm under acid conditions in lysosomes. CONCLUSION BSA-LC/DOPE, as biocompatible, tumor-targeting and pH-sensitive lipoprotein-mimic nanocarrier, is a promising system for effective intracellular delivery of PTX to tumors with optimal anti-tumor efficacy.
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