Institute for Advanced Study, Shenzhen University, Shenzhen 518060, China.
State Key Laboratory of Polymer Physics and Chemistry, Joint Laboratory of Polymer Science and Materials, Beijing National Laboratory for Molecular Sciences, Institute of Chemistry, Chinese Academy of Sciences, Beijing 100190, China.
J Control Release. 2020 Apr 10;320:337-346. doi: 10.1016/j.jconrel.2020.01.020. Epub 2020 Jan 10.
Drug delivery systems based on electrospun fibers have been under development for many years. However, studies of controllable long-term drug release from electrospun membrane systems and the underlying release mechanisms have seldom been reported.
In this study, electrospun membrane drug delivery systems consisting of the antibiotic ciprofloxacin hydrochloride and FDA-approved polymers are fabricated. Different second-component polymers are introduced to change the properties of a poly(d,l-lactide-co-glycolide) (PLGA) matrix, thereby altering the drug release behavior. On the basis of observations of morphology, cumulative release profiles, and determinations of release duration, the drug release kinetics and critical characteristics influencing drug release behavior are discussed.
It is found that the drug release profiles can be divided into three stages according to the rate of drug release. Stage I is controlled by fiber swelling and diffusion according to Fick's second law. Stage II is controlled by diffusion through a fused membrane structure, which results in very slow drug release. Stage III is controlled by polymer degradation and involves release of the remaining drug.
The results of this study of release mechanisms should provide a basis for adjustments of drug release dosage and duration, thereby contributing to the development of drug delivery systems satisfying clinical requirements.
基于电纺纤维的药物输送系统已经开发了多年。然而,很少有研究报道电纺膜系统中可控的长期药物释放及其潜在的释放机制。
在这项研究中,制备了由抗生素盐酸环丙沙星和 FDA 批准的聚合物组成的电纺膜药物输送系统。引入不同的第二组分聚合物来改变聚(DL-丙交酯-共-乙交酯)(PLGA)基质的性质,从而改变药物释放行为。基于形态学观察、累积释放曲线和释放持续时间的测定,讨论了药物释放动力学和影响药物释放行为的关键特性。
发现药物释放曲线可以根据药物释放的速度分为三个阶段。第一阶段受纤维溶胀和扩散的控制,符合菲克第二定律。第二阶段受熔融膜结构的扩散控制,导致药物释放非常缓慢。第三阶段受聚合物降解的控制,并释放剩余的药物。
本研究中对释放机制的研究结果应为调整药物释放剂量和持续时间提供依据,从而有助于开发满足临床要求的药物输送系统。