Polyvinyl alcohol boric acid - A promising tool for the development of sustained release drug delivery systems

Abstract

The paper deals with the design and investigation of the morphology, in vitro drug release and biocompatibility of some new formulations based on polyvinyl alcohol boric acid (PVAB) and diclofenac sodium salt (DCF), with the aim to explore the ability of PVAB to act as a matrix for controlled drug delivery systems. A series of three formulations was obtained by mixing the drug and the polymeric matrix in different mass ratios, with high drug content from 10% w/w to 30% w/w. Their structural and supramolecular characterization, performed by FTIR spectroscopy and X-ray diffraction, revealed important physical interactions between the drug and the polymeric matrix. The morphological data, obtained by X-ray diffraction, polarized optical microscopy and scanning electron microscopy revealed the presence of the drug into the PVAB polymeric matrix, as micrometric polycrystals with a mean diameter in the range 10-15 μm, depending on the drug/polymer ratio. The investigation of their surface peculiarities indicated highly hydrophilic surfaces with a water to air contact angle between 29.9 and 41.4 deg and a surface free energy of 45.6-54.2 N/m². The in vitro release kinetics was monitored by UV-VIS spectroscopy and the cytotoxic effect was investigated in vitro on fibroblasts and HeLa cells. The PVAB proved excellent cytocompatibility, a relative cell viability of the fibroblasts higher than 90% being recorded for concentrations of PVAB up to 7.5% w/v. The drug has been strongly anchored into the electron deficient PVAB matrix, fact which led to its prolonged release up to 5 days. These findings recommend PVAB as a versatile tool for the development of sustained release drug delivery systems with real chances to cross the gap from theory to applications.

Keywords: Biocompatible; Diclofenac sodium salt; Drug delivery systems; Local therapy; Sustained release.