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

机译：聚乙烯醇硼酸-开发持续释放药物递送系统的有前途的工具

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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 mu m, 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/m(2). The in vitro release kinetics was monitored by UV-VIS spectroscopy and the cytotoxic effect was investigated in 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.
机译：本文研究了一些基于聚乙烯醇硼酸（PVAB）和双氯芬酸钠（DCF）的新制剂的形态，体外药物释放和生物相容性，旨在探索PVAB发挥作用的能力。通过将药物和聚合物基质以不同的质量比混合得到一系列三种配方，其中药物含量从10％w / w到30％w / w不等。通过FTIR光谱和X射线衍射对它们进行结构和超分子表征，揭示了药物与聚合物基质之间的重要物理相互作用。通过X射线衍射，偏振光学显微镜和扫描电子显微镜获得的形态数据表明，药物存在于PVAB聚合物基体中，为平均粒径在10-15μm范围内的微晶多晶体，具体取决于药物/聚合物比。他们的表面特性的研究表明高度亲水的表面，水与空气的接触角为29.9至41.4度，表面自由能为45.6-54.2 N / m（2）。通过UV-VIS光谱监测体外释放动力学，并在体外研究对成纤维细胞和HeLa细胞的细胞毒性作用。 PVAB被证明具有出色的细胞相容性，对于浓度高达7.5％w / v的PVAB，成纤维细胞的相对细胞活力高于90％。该药物已被牢固地固定在缺乏电子的PVAB基质中，这导致其延长释放长达5天。这些发现推荐PVAB作为开发持续释放药物输送系统的多功能工具，它确实有机会跨越理论与应用之间的鸿沟。

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