Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia.
Department of Biotechnology and Pharmaceutical Engineering, University of Novi Sad, Novi Sad, Serbia.
Pharm Dev Technol. 2020 Mar;25(3):332-339. doi: 10.1080/10837450.2019.1701495. Epub 2019 Dec 12.
The physical chitosan hydrogel, obtained by ionic gelation in lactic acid solution, was combined with biocompatible oil-in-water microemulsion with ibuprofen, to prepare composite hydrogels with 0.25-1% of the polymer and 5% of the drug. The electrical conductivity measurement, photon correlation spectroscopy (PCS), and rheological analysis showed that the composite hydrogels comprise oil nanodroplets (16.21-22.56 nm) embedded within pseudoplastic chitosan hydrogel. ibuprofen release was sustained for 12 h and followed zero-order kinetics. pH values of the composite hydrogels were in the range of 4.80-5.27, thus physiologically acceptable. The formulation containing 0.5% chitosan enabled the maximum drug release rate of 239.25 μghcm as well as cohesiveness (154.958 ± 0.731 gs) higher than hardness (13.546 ± 0.065 g) and adhesiveness (-12.042 ± 1.161 gs), so textural properties were suitable for application along skin surface, without spillage, and for easy removal. This is the first study in which the composite chitosan hydrogels with ibuprofen were formulated by combining the chitosan hydrogel prepared without harmful chemical crosslinkers and low viscosity oil-in-water microemulsion, and the preclinical characterization of their biopharmaceutical aspect and textural characterization, that is of key importance in improving the patient's compliance, were performed.
物理性壳聚糖水凝胶是通过在乳酸溶液中离子凝胶化得到的,与生物相容性的油包水乳状液(含布洛芬)结合,制备出含有 0.25-1%聚合物和 5%药物的复合水凝胶。电导率测量、光子相关光谱(PCS)和流变分析表明,复合水凝胶由嵌入假塑性壳聚糖水凝胶中的油纳米液滴(16.21-22.56nm)组成。布洛芬的释放持续了 12 小时,符合零级动力学。复合水凝胶的 pH 值在 4.80-5.27 之间,因此具有生理可接受性。含有 0.5%壳聚糖的配方使药物释放率达到 239.25μghcm 的最大值,以及比硬度(13.546±0.065g)更高的内聚性(154.958±0.731gs)和粘着性(-12.042±1.161gs),因此质地特性适合应用于皮肤表面,不会溢出,易于去除。这是首次将无有害化学交联剂和低粘度油包水乳状液制备的壳聚糖水凝胶与布洛芬复合,对其生物制药方面和质地特性进行临床前特征描述的研究,这对于提高患者的顺应性至关重要。