Nagarajan Sakthivel, Soussan Laurence, Bechelany Mikhael, Teyssier Catherine, Cavaillès Vincent, Pochat-Bohatier Céline, Miele Philippe, Kalkura Narayana, Janot Jean-Marc, Balme Sébastien
Institut Européen des Membranes, UMR 5635 CNRS ENSCM Université Montpellier, Place Eugene Bataillon, F-34095 Montpellier cedex 5, France.
J Mater Chem B. 2016 Feb 14;4(6):1134-1141. doi: 10.1039/c5tb01897h. Epub 2016 Jan 13.
The aim of this study was to synthesize stable gelatin electrospun mats (ESMs) (cross-linked by glutaraldehyde (GTA) vapors) with tunable drug release properties using pH as a stimulus. Gelatin ESMs loaded with rhodamine as a model drug were first synthesized. The in vitro release of rhodamine was characterized to understand the mechanisms of drug release and the effects of both cross-linker concentration and pH on drug release. An optimal cross-linker concentration of 5% was evidenced to provide ESMs allowing both sustainable release of drugs at pH 7 and burst release at pH 2. The release profiles were then fitted with a power law model to describe the release kinetics. The chlorhexidine antibiotic drug was finally loaded into the optimal electrospun mat and its bactericidal activity was demonstrated against Gram-negative (E. coli) and Gram-positive (S. epidermidis) bacteria by agar diffusion tests. This biocompatible material was shown to efficiently destroy bacterial biofilms and prevent bacterial growth within a short time (3 h), while maintaining its antibacterial activity up to at least 72 h. This study provides a promising material, which could treat infected sites and prevent infections, with tunable drug releasing properties using pH as a stimulus.
本研究的目的是合成具有稳定药物释放特性的明胶电纺垫(ESMs)(通过戊二醛(GTA)蒸汽交联),并以pH值作为刺激因素来调节药物释放。首先合成了负载若丹明作为模型药物的明胶ESMs。对若丹明的体外释放进行了表征,以了解药物释放机制以及交联剂浓度和pH值对药物释放的影响。结果表明,5%的最佳交联剂浓度可使ESMs在pH值为7时实现药物的持续释放,在pH值为2时实现突释。然后用幂律模型拟合释放曲线,以描述释放动力学。最后将氯己定抗生素药物负载到最佳电纺垫中,并通过琼脂扩散试验证明其对革兰氏阴性菌(大肠杆菌)和革兰氏阳性菌(表皮葡萄球菌)具有杀菌活性。这种生物相容性材料被证明能在短时间内(3小时)有效破坏细菌生物膜并防止细菌生长,同时至少在72小时内保持其抗菌活性。本研究提供了一种有前景的材料,它可以利用pH值作为刺激因素来调节药物释放特性,从而治疗感染部位并预防感染。