Recently, polymersomes have attracted growing attention as promising carriers in the application of cancer therapy. They are one type of architectures of polymeric self-assembles, which appear as liposome-like nanoparticles owning internal aqueous cavum and hydrophobic shell but with more tunable functionalization. However, due to high water solubility, it is always very difficult for polymersomes to load water-soluble small-molecular chemotherapeutics by simple method. In addition, the premature drug release in the blood circulation is always serious and has become a common problem for polymersomes, which would impair anticancer efficacy and aggravate side effect of chemotherapeutics. With the aim to solve these problems, herein, we designed a series of amphiphilic polyphosphazens containing 2-diethylaminoethyl 4-aminobenzoate (DEAAB) as hydrophobic side groups. Taking advantage of the interaction between polymers and drugs, we effectively improved the loading content of water-soluble doxorubicin hydrochloride (DOX HCl). More importantly, after added into polymersome solution, HAuCl<sub>4</sub> could be transferred to AuNPs and then, the new-born AuNPs would be homogeneously distributed in the shell of PNP polymersomes through coordination interaction with polymers and acted as crosslinkers to inhibit drug leakage at pH7.4. Furthermore, the polymersomes would facilitate intracellular drug release on the basis of the protonation of tertiary amino groups responsive to the relatively low pH in cancer cells. As a consequence, all these features of polyphosphazene vesicle cooperatively facilited the improvement of drug anti-cancer efficacy in vivo. Also, self-assembled polyphosphazene vesicles display great potentials as effective carriers to deliver other water-soluble bioactive substances, such as protein and gene medicines.

Self-assembled polyphosphazene vesicles as effective carriers for water-soluble chemotherapeutics

254th National Meeting (2017)

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