Faculty of Pharmacy, Bahauddin Zakariya University, Multan, Pakistan.
Leicester School of Pharmacy, De Montfort University, Leicester, UK.
Pharm Res. 2021 Jan;38(1):165-177. doi: 10.1007/s11095-021-02995-0. Epub 2021 Feb 3.
The aim of this study was to fabricate polymeric microneedles, loaded with macrolides (erythromycin, azithromycin), using hyaluronic acid and polyvinyl pyrollidone.
These microneedles were fabricated using a vacuum micromolding technique. The integrity of the microneedle patches was studied by recording their morphologic features, folding endurance, swelling and micro-piercing. Physicochemical characteristics were studied by differential scanning calorimetry, thermogravimetric analysis and fourier transform infrared spectroscopy. In-vitro drug release, antibiofilm and effect of microneedle patch on wound healing were also studied to confirm the efficacy of the formulations.
Formulated patches displayed acceptable folding endurance (>100) and uniform distribution of microneedles (10 × 10) that can penetrate parafilm. Differential scanning calorimetry results depict a decrease in the crystallinity of macrolides following their incorporation in to a polymer matrix. Percentage release of azithromycin and erythromycin from the polymeric patch formulations (over 30 min) was 90% and 63% respectively. Broadly, the zone of bacterial growth inhibition follows the same order for Staphylococcus aureus, Escherichia coli and Salmonella enterica. After 5 days of treatment with azithromycin patches, the wound healing was complete and skin structure (e.g. hair follicles and dermis) was regenerated.
It was concluded that azithromycin loaded microneedle patches can be used to treat biofilms in the infected wounds.
本研究旨在使用透明质酸和聚乙烯吡咯烷酮制备载有大环内酯类药物（红霉素、阿奇霉素）的聚合物微针。
采用真空微成型技术制备这些微针。通过记录微针贴片的形态特征、折叠耐力、溶胀和微穿刺来研究其完整性。通过差示扫描量热法、热重分析和傅里叶变换红外光谱研究物理化学特性。还研究了体外药物释放、抗生物膜和微针贴片对伤口愈合的影响，以确认配方的疗效。
配制的贴片显示出可接受的折叠耐力（>100）和均匀分布的微针（10×10），可以穿透聚偏二氟乙烯。差示扫描量热法结果表明，大环内酯类药物在掺入聚合物基质后结晶度降低。阿奇霉素和红霉素从聚合物贴片制剂中的释放百分比（超过 30 分钟）分别为 90%和 63%。总的来说，细菌生长抑制区对金黄色葡萄球菌、大肠杆菌和肠炎沙门氏菌的抑制效果相同。使用阿奇霉素贴片治疗 5 天后，伤口愈合完全，皮肤结构（如毛囊和真皮）得到再生。
可以得出结论，载有阿奇霉素的微针贴片可用于治疗感染伤口中的生物膜。
