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阿普米拉斯微乳剂作为局部炎症的局部治疗：设计、表征及疗效评估。

Apremilast Microemulsion as Topical Therapy for Local Inflammation: Design, Characterization and Efficacy Evaluation.

作者信息

Sarango-Granda Paulo, Silva-Abreu Marcelle, Calpena Ana Cristina, Halbaut Lyda, Fábrega María-José, Rodríguez-Lagunas María J, Díaz-Garrido Natalia, Badia Josefa, Espinoza Lupe Carolina

机构信息

Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028 Barcelona, Spain.

Institute of Nanoscience and Nanotechnology (IN2UB), University of Barcelona, 08028 Barcelona, Spain.

出版信息

Pharmaceuticals (Basel). 2020 Dec 21;13(12):484. doi: 10.3390/ph13120484.

DOI:10.3390/ph13120484
PMID:33371334
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7767333/
Abstract

Apremilast (APR) is a selective phosphodiesterase 4 inhibitor administered orally in the treatment of moderate-to-severe plaque psoriasis and active psoriatic arthritis. The low solubility and permeability of this drug hinder its dermal administration. The purpose of this study was to design and characterize an apremilast-loaded microemulsion (APR-ME) as topical therapy for local skin inflammation. Its composition was determined using pseudo-ternary diagrams. Physical, chemical and biopharmaceutical characterization were performed. Stability of this formulation was studied for 90 days. Tolerability of APR-ME was evaluated in healthy volunteers while its anti-inflammatory potential was studied using in vitro and in vivo models. A homogeneous formulation with Newtonian behavior and droplets of nanometric size and spherical shape was obtained. APR-ME released the incorporated drug following a first-order kinetic and facilitated drug retention into the skin, ensuring a local effect. Anti-inflammatory potential was observed for its ability to decrease the production of IL-6 and IL-8 in the in vitro model. This effect was confirmed in the in vivo model histologically by reduction in infiltration of inflammatory cells and immunologically by decrease of inflammatory cytokines IL-8, IL-17A and TNFα. Consequently, these results suggest that this formulation could be used as an attractive topical treatment for skin inflammation.

摘要

阿普米司特（APR）是一种选择性磷酸二酯酶4抑制剂，口服用于治疗中度至重度斑块状银屑病和活动性银屑病关节炎。该药物的低溶解度和低渗透性阻碍了其经皮给药。本研究的目的是设计并表征一种载有阿普米司特的微乳剂（APR-ME），用于局部皮肤炎症的局部治疗。使用伪三元相图确定其组成。进行了物理、化学和生物药剂学表征。对该制剂的稳定性进行了90天的研究。在健康志愿者中评估了APR-ME的耐受性，同时使用体外和体内模型研究了其抗炎潜力。获得了一种具有牛顿流体行为、纳米尺寸且呈球形的均匀制剂。APR-ME按照一级动力学释放所载药物，并促进药物在皮肤中的滞留，确保局部效应。在体外模型中观察到其具有抗炎潜力，能够降低IL-6和IL-8的产生。在体内模型中，通过组织学上炎症细胞浸润的减少以及免疫学上炎症细胞因子IL-8、IL-17A和TNFα的降低，证实了这种效果。因此，这些结果表明该制剂可作为一种有吸引力的皮肤炎症局部治疗药物。

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