Phenylboronic Acid-Functionalized Hyaluronic Acid as Polysaccharide Carriers for Diol-Containing Drugs Delivery

Packaging hydrophobic drugs into polysaccharide carriers can improve their aqueous solubility, biocompatibility, tumor-specific accumulation, and therapeutic effect. In this work, phenylboronic acid (PBA) was anchored onto the chain of biocompatible polysaccharide hyaluronic acid (HA) by an amide condensation reaction, which could be used to fabricate stimuli-responsive targeted drug delivery systems. A series of pH-responsive conjugated hyaluronic acid nanoparticles composed of a hydrophobic drug core and hydrophilic hyaluronic acid shell were prepared by the boronate-crosslink of the PBA with diol-containing anticancer drugs such as capecitabine (CAPE) and aloin (Al). Satisfactory targeted drug release behavior at acidic pH, lower cytotoxicity, and higher anticancer effect were realized by using this polysaccharide carrier. It is believed that this strategy has great potential for polysaccharide modification and anticancer-associated applications. The stimuli-responsive building block phenylboronic acid was anchored onto the chain of biocompatible polysaccharide hyaluronic acid to obtain a novel pH-responsive and cell-targeting polysaccharide carrier for delivery of the diol-containing anticancer drug to cancer cells. image