Research On Bioadhesive Phenylboronic Acid-Rich Nanoparticles(PBNPs) For Vaginal Drug Delivery

Currently the ineffective interaction with the mucous is a major factor limiting mucoadhesive delivery system, resulting in a short partial residence time. To solve this problem, researchers have proposed some new adhesion strategies, such as thiomer and lectin modification, but the chemical stability of these two strategies is poor and both need special protection during storage and application. Therefore, explore a novel bioadhesive strategy with stable and strong adhesion properties is necessary.Phenylboronic acid and its derivatives are known to possess the ability to reversibly interact with diols, sugars, and glycoproteins. All biological membranes, especially mucosa (including the mucus on the mucosa), virtually include glycoproteins such as the highly-glycosylated mucin, providing numerous interacting sites for phenylboronic acid. These characteristics make its application in the field of mucoadhesion possible.This study was to research the potential of Phenylboronic acid (PBA) modification in mucoadhesive drug delivery system. Phenylboronic acid-rich nanoparticls (PBNPs) were prepared by two step, the physical and chemical properties, adhesive property, drug delivery and security properties were characterized. Results show that PBNPs adsorbed mucin in vitro effectively and could be easily loaded with the model drug Interferon (IFN). Drug release from PBNPs was controlled by the presence of mucin.Adhesion results in vivo showed that the residence time of PBNPs were increased significantly compared with the IR-783 solution. Neither obvious cytotoxicity nor vaginal histological changes in mice caused by PBNPs or IFN-loaded PBNPs were observed.In summary, the mucin-triggered release of proteins drugs validated the potential of this PBNPs as a promising smart mucosal drug delivery system.