Antibiofilm Effects of Macrolide Loaded Microneedle Patches: Prospects in Healing Infected Wounds,Pharmaceutical Research

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Antibiofilm Effects of Macrolide Loaded Microneedle Patches: Prospects in Healing Infected Wounds
Pharmaceutical Research ( IF 3.5 ) Pub Date : 2021-02-03 , DOI: 10.1007/s11095-021-02995-0
Muhammad Sohail Arshad ₁ , Aleema Tehreem Zahra ₁ , Saman Zafar ₁ , Hussain Zaman ₂ , Ambreen Akhtar ₂ , Muhammad Mazhar Ayaz ₃ , Israfil Kucuk ₄ , Mohammed Maniruzzaman ₅ , Ming-Wei Chang ₆ , Zeeshan Ahmad ₂

Affiliation

Aim

The aim of this study was to fabricate polymeric microneedles, loaded with macrolides (erythromycin, azithromycin), using hyaluronic acid and polyvinyl pyrollidone.

Methods

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.

Results

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.

Conclusion

It was concluded that azithromycin loaded microneedle patches can be used to treat biofilms in the infected wounds.

Graphical abstract

中文翻译：

载有大环内酯的微针贴片的抗菌膜作用：治愈感染伤口的前景

目的

本研究的目的是使用透明质酸和聚乙烯吡咯烷酮制造载有大环内酯类（红霉素、阿奇霉素）的聚合物微针。

方法

这些微针是使用真空微成型技术制造的。微针贴片的完整性通过记录它们的形态特征、耐折性、膨胀和微穿孔来研究。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了理化特性。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，以确认制剂的功效。

结果

配制的贴剂显示出可接受的耐折性 (>100) 和可穿透石蜡膜的微针 (10 × 10) 的均匀分布。差示扫描量热法结果表明大环内酯类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剂制剂（超过 30 分钟）中的释放百分比分别为 90% 和 63%。广义上，细菌生长抑制区与金黄色葡萄球菌、大肠杆菌和沙门氏菌的顺序相同。用阿奇霉素贴片治疗5天后，伤口完全愈合，皮肤结构（如毛囊和真皮）得到再生。