Hydrophobic guest mediated micellization and demicellization of rationally designed amphiphilic poly(organophosphazene) for efficient drug delivery

Abstract

Recently, biocompatible and amphiphilic poly(organophosphazene) (PPZ) has been suggested as a drug delivery carrier since it can be easily modified to achieve desired chemical properties. In this work, we newly designed a PPZ with balanced hydrophilicity and hydrophobicity by modulating the mole ratio of hydrophilic to hydrophobic substituents in the PPZ backbone to form hydrophobic drug, resveratrol (RSV), mediated micelle for efficient drug delivery. The feeding mass ratio of RSV and PPZ was optimized to be 1:10 based on loading efficiency, loading capacity, and release kinetics and micelles were self-assembled due to hydrophobic intermolecular interaction above critical micelle concentration (20 mg/l). According to the in vitro study, RSV molecules encapsulated in the core of PPZ micelles were released out by demicellization in a sustained manner, resulting in reduction of perceived cytotoxicity of RSV. Therefore, the present PPZ is considered as an efficient drug delivery carrier for encapsulation and sustained delivery of hydrophobic drug molecules with acceptable biocompatibility. 2016 by American Scientific Publishers.