Polypeptides with excellent biocompatibility and biodegradability are one of the most appealing and versatile building materials for the development of anticancer nanomedicines. Here, we have designed and prepared vitamin E-oligo(methyl diglycol L-glutamate) as a biocompatible and functional surfactant for facile preparation of active tumor-targeting PLGA nanoparticles. The <i>in vivo</i> studies showed that hyaluronic acid coated PLGA nanoparticulate docetaxel effectively targeted and suppressed orthotopic human lung cancer. In a further study, by combining reductively cleavable peptide surfactant and covalent hyaluronic acid coating, we have developed robust, responsive and targeted PLGA anticancer nanomedicines, which completely inhibited growth of orthotopic human A549-Luc lung tumor in mice, leading to a significantly improved survival rate and reduced adverse effect as compared to free docetaxel. In addition, we have also constructed pH-responsive chimaeric pepsomes based on designed asymmetric poly(ethylene glycol)-b-poly(L-leucine)-b-poly(L-glutamic acid) triblock copolymer that shows efficient loading and active intracellular delivery of doxorubicin hydrochloride.

Functional polypeptides toward design of multifunctional anticancer nanomedicines

254th National Meeting (2017)

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