Institute of Pharmaceutical Technology, Faculty of Pharmacy, University of Ss Cyril and Methodius, Skopje, Republic of Macedonia.
Institute of Physics, Faculty of Natural Sciences and Mathematics, University Ss Cyril and Methodius, Skopje, Republic of Macedonia.
Carbohydr Polym. 2018 Apr 15;186:260-272. doi: 10.1016/j.carbpol.2018.01.043. Epub 2018 Jan 31.
The aim of this study was to develop chitosan (CS) microparticulated mucoadhesive drug delivery system (DDS) with improved therapeutic performance and biological responce. Ionotropic gelation/spray drying process was used for preparation of doxycycline hyclate (DOXY) loaded low and medium molecular weight (LMw and MMw) CS/sodium tripolyphosphate microparticles (CS/TPP MPs), further coated with ethyl cellulose (EC) using coacervation/solvent displacement technique. The relevant physico-chemical and biopharmaceutical properties were optimized using experimental design approach. Both coated and uncoated CS/TPP MPs showed high mucoadhesive potential and did not affect the viability of the tested epithelial cell line. The MPs induced slow and gradual apoptotic response in murine macrophage cell line RAW 264.7 and the observed effect depended upon formulation type and MP concentration. Biological effect of the CS-based MPs observed in our experiments point to synergism of the biological response of the carrier with the anti-inflammatory effect of DOXY.
本研究旨在开发壳聚糖(CS)微粒型黏附药物递送系统(DDS),以提高治疗性能和生物响应。离子凝胶/喷雾干燥工艺用于制备盐酸多西环素(DOXY)负载的低和中分子量(LMw 和 MMw)CS/三聚磷酸钠微粒(CS/TPP MPs),进一步使用凝聚/溶剂置换技术用乙基纤维素(EC)进行包衣。使用实验设计方法优化了相关的物理化学和生物制药性质。包衣和未包衣的 CS/TPP MPs 均表现出高的黏膜黏附潜力,且不影响所测试的上皮细胞系的活力。MPs 在鼠巨噬细胞系 RAW 264.7 中诱导缓慢而渐进的凋亡反应,观察到的效果取决于配方类型和 MP 浓度。在我们的实验中观察到的基于 CS 的 MPs 的生物学效应表明载体的生物学响应与 DOXY 的抗炎作用具有协同作用。