Abstract：
BACKGROUND: Diabetic foot infection (DFI) is one of the complications of diabetes mellitus. Clindamycin (CLY) is one of the antibiotics recommended to treat DFI, but CLY given orally and intravenously still causes many side effects.
METHODS: In this study, we encapsulated CLY in a bacteria sensitive microparticle system (MP-CLY) using polycaprolactone (PCL) polymer. MP-CLY was then delivered in a separable effervescent microarray patch (MP-CLY-SEMAP), which has the ability to separate between the needle layer and separable layer due to the formation of air bubbles when interacting with interstitial fluid in the skin.
RESULTS: The characterization results of MP-CLY proved that CLY was encapsulated in large amounts as the amount of PCL polymer used increased, and there was no change in the chemical structure of CLY. In vitro release test results showed increased CLY release in media cultured with Staphylococcus aureus bacteria and showed controlled release. The characterization results of MPCLY-SEMAP showed that the developed formula has optimal mechanical and penetration capabilities and can separate in 56 ± 5.099 s. An ex vivo dermatokinetic test on a bacterially infected skin model showed an improvement of CLY dermatokinetic profile from MP-CLY SEMAP and a decrease in bacterial viability by 99.99%.
CONCLUSIONS: This research offers proof of concept demonstrating the improved dermatokinetic profile of CLY encapsulated in a bacteria sensitive MP form and delivered via MP-CLY-SEMAP. The results of this research can be developed for future research by testing MP-CLY-SEMAP in vivo in appropriate animal models.
METHODS: In this study, we encapsulated CLY in a bacteria sensitive microparticle system (MP-CLY) using polycaprolactone (PCL) polymer. MP-CLY was then delivered in a separable effervescent microarray patch (MP-CLY-SEMAP), which has the ability to separate between the needle layer and separable layer due to the formation of air bubbles when interacting with interstitial fluid in the skin.
RESULTS: The characterization results of MP-CLY proved that CLY was encapsulated in large amounts as the amount of PCL polymer used increased, and there was no change in the chemical structure of CLY. In vitro release test results showed increased CLY release in media cultured with Staphylococcus aureus bacteria and showed controlled release. The characterization results of MPCLY-SEMAP showed that the developed formula has optimal mechanical and penetration capabilities and can separate in 56 ± 5.099 s. An ex vivo dermatokinetic test on a bacterially infected skin model showed an improvement of CLY dermatokinetic profile from MP-CLY SEMAP and a decrease in bacterial viability by 99.99%.
CONCLUSIONS: This research offers proof of concept demonstrating the improved dermatokinetic profile of CLY encapsulated in a bacteria sensitive MP form and delivered via MP-CLY-SEMAP. The results of this research can be developed for future research by testing MP-CLY-SEMAP in vivo in appropriate animal models.
摘要：
背景：糖尿病足感染（DFI）是糖尿病的并发症之一。克林霉素（CLY）是推荐用于治疗DFI的抗生素之一，但是口服和静脉注射CLY仍然会引起许多副作用。
方法：在本研究中，我们使用聚己内酯（PCL）聚合物将CLY封装在细菌敏感的微粒系统（MP-CLY）中。然后在可分离的泡腾微阵列贴片（MP-CLY-SEMAP）中递送MP-CLY，当与皮肤中的间质液相互作用时,由于气泡的形成,其具有在针层和可分离层之间分离的能力。
结果：MP-CLY的表征结果证明，随着PCL聚合物用量的增加，CLY被大量包封，CLY的化学结构没有变化。体外释放测试结果表明，在金黄色葡萄球菌培养的培养基中，CLY的释放增加，并显示出受控的释放。MPCLY-SEMAP的表征结果表明，开发的配方具有最佳的机械和渗透能力，并且可以在56±5.099s内分离。在细菌感染的皮肤模型上进行的离体皮肤动力学测试显示，与MP-CLYSEMAP相比，CLY皮肤动力学曲线有所改善，细菌活力降低了99.99％。
结论：这项研究提供了概念证明，证明了以细菌敏感的MP形式封装并通过MP-CLY-SEMAP递送的CLY的改善的皮肤动力学特征。这项研究的结果可以通过在适当的动物模型中体内测试MP-CLY-SEMAP来开发用于未来的研究。
方法：在本研究中，我们使用聚己内酯（PCL）聚合物将CLY封装在细菌敏感的微粒系统（MP-CLY）中。然后在可分离的泡腾微阵列贴片（MP-CLY-SEMAP）中递送MP-CLY，当与皮肤中的间质液相互作用时,由于气泡的形成,其具有在针层和可分离层之间分离的能力。
结果：MP-CLY的表征结果证明，随着PCL聚合物用量的增加，CLY被大量包封，CLY的化学结构没有变化。体外释放测试结果表明，在金黄色葡萄球菌培养的培养基中，CLY的释放增加，并显示出受控的释放。MPCLY-SEMAP的表征结果表明，开发的配方具有最佳的机械和渗透能力，并且可以在56±5.099s内分离。在细菌感染的皮肤模型上进行的离体皮肤动力学测试显示，与MP-CLYSEMAP相比，CLY皮肤动力学曲线有所改善，细菌活力降低了99.99％。
结论：这项研究提供了概念证明，证明了以细菌敏感的MP形式封装并通过MP-CLY-SEMAP递送的CLY的改善的皮肤动力学特征。这项研究的结果可以通过在适当的动物模型中体内测试MP-CLY-SEMAP来开发用于未来的研究。
