Most individual anti-cancer drugs have poor targeting ability and difficulties in controlling the drug release, which significantly limit the clinical applications. This study reports a novel dual-targeted synthesis method for encapsulating 10-hydroxycamptothecin (HCPT) into pectin-(eight-arm-polyethylene glycol)-dihydroartemisinin nanoparticles (FPPD) conjugates to form self-assembled FPPDH nanoparticles (FPPDH NPs). The prepared FPPDH NPs contained hydrophilic carriers of pectin and eight-arm-polyethylene glycol and hydrophobic anticancer drugs of dihydroartemisinin and hydroxycamptothecin, for stabilizing particle size, improving water-solubility, and achieving drug controlled release. The results indicated that the obtained dual-targeted nanoparticles possessed appropriate size (~ 100 nm), drug-loaded efficiency (~ 9.02 wt% DHA) and encapsulation efficiency (~ 13.79wt% HCPT). The time-dependent cytotoxic of the FPPDH nanoparticle were only 3.1% 4T1 cell and 1.2% MCF-1 cell survived after 72 h. FPPDH nanoparticle exhibited a higher cytotoxicity, longer blood retention time of free drug (8.0-fold DHA, 7.5-fold HCPT) and more effective cellular uptake. 4T1 tumor-bearing mice treated with the nanoparticles also showed a considerable survival advantagen comparison with the free DHA as well as the free HCPT. Moreover, it is clearly an elaborate certification that FPPDH NPs could reduce the risk of hypersensitivity reactions substantially. Therefore, FPPDH NPs as an effective anti-cancer drug have a promising potential for anti-cancer combination therapy.<br/>

Self-assembled dual-targeted pectin-conjugated multi-arm-polyethylene glycol– dihydroartemisinin nanoparticles for anticancer combination therapy

256th National Meeting (2018)

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