Friuli Valeria, Pisani Silvia, Conti Bice, Bruni Giovanna, Maggi Lauretta
Department of Drug Sciences, University of Pavia, Via Taramelli 12, 27100 Pavia, Italy.
Department of Otolaryngology, Fondazione IRCCS Policlinico San Matteo, 27100 Pavia, Italy.
Polymers (Basel). 2022 May 23;14(10):2127. doi: 10.3390/polym14102127.
A challenge in the pharmaceutical sector is the development of controlled release dosage forms for oral administration of poorly soluble drugs, in particular, drugs characterized by pH-dependent solubility through the gastrointestinal tract, which itself shows wide variability in terms of environmental pHs. The best approach is to increase the dissolution rate of the drugs at the different pHs and only then modify its release behavior from the pharmaceutical form. This work aims to demonstrate the ability of properly designed polymeric nanofibers in enhancing the release rate of model drugs with different pH-dependent solubility in the different physiological pHs of the gastrointestinal tract. Polymeric nanofibers loaded with meloxicam and carvedilol were prepared using the electrospinning technique and were then included in properly designed tablet formulations to obtain fast or sustained release dosage forms. The nanofibers and the tablets were characterized for their morphological, physico-chemical and dissolution properties. The tablets are able to deliver the dose according to the expected release behavior, and zero-order, first-order, Higuchi, Korsmeyer-Peppas and Hixon-Crowell kinetics models were used to analyze the prevailing release mechanism of the tablets. This study shows that the electrospun fibers can be advantageously included in oral dosage forms to improve their release performances.
制药领域面临的一项挑战是开发用于口服难溶性药物的控释剂型，尤其是那些在胃肠道中具有pH依赖性溶解度的药物，而胃肠道的环境pH值本身就存在很大差异。最佳方法是提高药物在不同pH值下的溶解速率，然后再改变其从药物剂型中的释放行为。这项工作旨在证明经过适当设计的聚合物纳米纤维能够提高在胃肠道不同生理pH值下具有不同pH依赖性溶解度的模型药物的释放速率。采用静电纺丝技术制备了负载美洛昔康和卡维地洛的聚合物纳米纤维，然后将其纳入经过适当设计的片剂配方中，以获得速释或缓释剂型。对纳米纤维和片剂的形态、物理化学和溶解性能进行了表征。这些片剂能够按照预期的释放行为给药，并使用零级、一级、Higuchi、Korsmeyer-Peppas和Hixon-Crowell动力学模型来分析片剂的主要释放机制。这项研究表明，电纺纤维可以有利地包含在口服剂型中，以改善其释放性能。
