Istanbul Technical University, Department of Chemical Engineering, Istanbul, Turkey.
Istanbul Technical University, Department of Chemical Engineering, Istanbul, Turkey.
Eur J Pharm Sci. 2022 Mar 1;170:106113. doi: 10.1016/j.ejps.2021.106113. Epub 2022 Jan 2.
In recent years, there is an increasing attention on biocompatible electrospun nanofibers for drug delivery applications since they provide high surface area, controlled and sustained drug release, and they mimic the extracellular matrix. In the present study, tetracycline hydrochloride (TCH) antibiotic loaded poly(ω-pentadecalactone-co-ε-caprolactone)/gelatin/chitosan nanofibrous membranes were fabricated as a controlled drug delivery system. Poly(ω-pentadecalactone-co-ε-caprolactone) copolymer has been enzymatically synthesized in previous studies, thus it provides an originality to the membrane. Combination of a synthetic polymer, a protein, and a polysaccharide in order to obtain a synergetic effect is another novelty of this work and there exists limited examples for such electrospun membrane. Varied amounts of TCH was electrospun together with poly(ω-pentadecalactone-co-ε-caprolactone)/gelatin/chitosan (50/40/10 vol ratio) polymer blend (fiber diameters ranged between 85.7-225.2 nm) and several characterizations (morphological and molecular structure, wettability characteristics, and thermal behavior) were applied to examine the drug incorporation. Subsequently, in vitro drug release studies were conducted and mathematical modeling was applied for the detection of transport mechanism of drug. TCH release proceeded 14 days through an initial burst release in first hour and followed by a sustained release. 1% TCH-loaded sample was shown as optimal preparation with 96.5% total drug release and 11.8% initial burst release. TCH-loaded preparations demonstrated a good antibacterial activity against Gram-positive (Staphylococcus aureus and Bacillus subtilis) bacteria and a limited effect (no inhibition zone observed below 3% TCH concentration) against Gram-negative (Escherichia coli) bacterium. Thus, TCH concentrations of ≥ 3% could be preferred to obtain a wide-spectrum effectiveness. The presented drug delivery system is suggested to be applied for treatment of skin infections as a wound dressing device.
近年来，人们越来越关注用于药物输送应用的生物相容的电纺纳米纤维，因为它们提供了高的表面积、控制和持续的药物释放，并模拟细胞外基质。在本研究中，制备了载盐酸四环素（TCH）抗生素的聚（ω-十五内酯-共-ε-己内酯）/明胶/壳聚糖纳米纤维膜作为一种控制药物释放系统。聚（ω-十五内酯-共-ε-己内酯）共聚物已在先前的研究中通过酶合成，因此为膜提供了原创性。将合成聚合物、蛋白质和多糖结合起来以获得协同效应是这项工作的另一个新颖之处，并且这样的电纺膜的例子有限。将不同量的 TCH 与聚（ω-十五内酯-共-ε-己内酯）/明胶/壳聚糖（50/40/10 体积比）聚合物共混物一起电纺（纤维直径在 85.7-225.2nm 之间），并进行了几种特性（形态和分子结构、润湿性特性和热行为）的分析，以检查药物的掺入。随后，进行了体外药物释放研究，并应用数学模型来检测药物的传输机制。TCH 释放持续了 14 天，首先在第一个小时内有一个初始突释，然后是持续释放。负载 1% TCH 的样品显示出最佳的制备效果，总药物释放率为 96.5%，初始突释率为 11.8%。负载 TCH 的制剂对革兰氏阳性（金黄色葡萄球菌和枯草芽孢杆菌）细菌表现出良好的抗菌活性，对革兰氏阴性（大肠杆菌）细菌的作用有限（低于 3% TCH 浓度观察不到抑制区）。因此，为了获得广谱效果，可以选择 TCH 浓度≥3%。建议将该药物输送系统作为一种伤口敷料装置应用于皮肤感染的治疗。
