Gel network comprising UV crosslinked PLGA-b-PEG-MA nanoparticles for ibuprofen topical delivery
Gel network comprising UV crosslinked PLGA-b-PEG-MA nanoparticles for ibuprofen topical delivery
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DOI：
10.1080/10837450.2019.1643880
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发表时间：
2019-08-06
影响因子：
3.4
通讯作者：
Ulubayram, Kezban
中科院分区：
文献类型：
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作者：
Eroglu, Ipek;Gultekinoglu, Merve;Ulubayram, Kezban
依那普利是一种非甾体抗炎药，用于治疗风湿性关节炎和骨关节炎。在本研究中，我们制备了局部凝胶网络，以增强布洛芬的渗透，维持控释和增加患者的依从性。采用乳液形成/溶剂扩散法制备布洛芬纳米粒。然后将纳米颗粒与甲基丙烯酸氨基乙酯缀合，得到PLGA-b-PEG-MA结构的负载布洛芬的纳米颗粒。通过经由UV曝光交联纳米颗粒来开发负载布洛芬的凝胶网络。通过表征粒度、zeta电位、形态学、包封效率、体外释放、细胞毒性和体外伤口愈合的增强来评估局部应用的适用性。纳米颗粒的平均直径测量为230 +/-20nm。制备了具有更高粒度（2800 +/-350 nm）和ζ电位（39.8 +/-9.2 mV）的凝胶网络制剂，这取决于共聚物结构内甲基丙烯酸酯的共轭，并且具有73.6 +/-2.8%的包封效率。布洛芬的体外释药持续时间超过7小时。凝胶网络以剂量依赖性方式改善胶原合成、I型胶原mRNA表达和纤维化。基于此，我们可以得出结论，PLGA-b-PEG凝胶网络可能是一个有前途的系统，局部递送布洛芬在类风湿关节炎患者。
Ibuprofen is a non-steroidal anti-inflammatory drug for the treatment of Rheumatoid Arthritis and osteoarthritis. In this study, we prepared topical gel network for enhancement of ibuprofen penetration, maintenance of controlled release and increased patient compliance. Nanoparticles containing ibuprofen were prepared by means of emulsion formation/solvent diffusion method using synthesized copolymer. Nanoparticles were then conjugated with aminoethylmethacrylate, resulting in ibuprofen-loaded nanoparticles in PLGA-b-PEG-MA structure. Ibuprofen-loaded gel networks were developed by crosslinking nanoparticles via UV exposure. Suitability for topical application has been assessed through characterization of particle size, zeta potential, morphology, encapsulation efficiency, in vitro release, cytotoxicity and enhancement of in vitro wound healing. The mean diameter of nanoparticles was measured as 230 +/- 20 nm. Gel network formulations with higher particle size (2800 +/- 350 nm) and zeta potential (39.8 +/- 9.2 mV), depending on conjugation of methacrylate within copolymeric structure, and having encapsulation efficacy of 73.6 +/- 2.8% were prepared. The in vitro release of ibuprofen was sustained for more than 7 hours. Gel network improved collagen synthesis, type I collagen mRNA expression and fibrosis in dose dependent manner. Based on this, we can conclude that PLGA-b-PEG gel network might be a promising systems for the local delivery of ibuprofen in RA patients.