School of Life Sciences, Jilin University, Changchun, China.
School of Life Sciences, Jilin University, Changchun, China.
J Pharm Sci. 2021 May;110(5):2233-2240. doi: 10.1016/j.xphs.2021.01.024. Epub 2021 Jan 29.
Ketoprofen, a non-steroidal anti-inflammatory drug, can effectively relieve pain associated with arthritis, and microRNA-124 (miR-124) can inhibit the progression of the disease. In this study, poly (cyclohexane-1,4-diylacetone dimethylene ketal) (PCADK) nanoparticles (NPs) co-loaded with ketoprofen and miR-124 were successfully prepared using an emulsified solvent evaporation method. The co-loaded NPs exhibited a mean particle diameter of 160 nm. The acid sensitivity of the NPs was determined through in vitro release experiments. An adjuvant-induced arthritis rat model of arthritis was established for evaluating the pharmacodynamics of the NPs through clinical scoring and degree of swelling. The PCADK NPs exhibited more potent pharmacodynamic effects owing to the acid-sensitive properties of the carrier materials, compared with Poly (lactic-co-glycolic acid) (PLGA) NPs. Furthermore, PCADK co-loaded NPs exhibited superior anti-inflammatory effects compared to NPs loaded with either miR-124 or ketoprofen alone. In conclusion, co-delivery of ketoprofen and miR-124 through NPs is a promising strategy for the treatment of arthritis.
酮洛芬是一种非甾体抗炎药，能有效缓解关节炎引起的疼痛，而 microRNA-124（miR-124）可以抑制疾病的进展。在这项研究中，采用乳化溶剂蒸发法成功制备了载有酮洛芬和 miR-124 的聚（环己烷-1,4-二基丙酮二亚甲基缩酮）（PCADK）纳米颗粒（NPs）。共载 NPs 的平均粒径为 160nm。通过体外释放实验确定了 NPs 的酸敏性。建立了佐剂诱导的关节炎大鼠关节炎模型，通过临床评分和肿胀程度评估 NPs 的药效学。与聚乳酸-羟基乙酸共聚物（PLGA） NPs 相比，由于载体材料的酸敏特性，PCADK NPs 表现出更强的药效。此外，PCADK 共载 NPs 与单独载 miR-124 或酮洛芬的 NPs 相比，表现出更好的抗炎效果。综上所述，通过 NPs 共递送酮洛芬和 miR-124 是治疗关节炎的一种有前途的策略。
