Gómez-Segura Lídia, Parra Alexander, Calpena-Campmany Ana Cristina, Gimeno Álvaro, Gómez de Aranda Immaculada, Boix-Montañes Antonio
Department of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08028 Barcelona, Spain.
Department of Medicine and Animal Health, Autonomous University of Barcelona, 08193 Bellatera, Spain.
Nanomaterials (Basel). 2020 Feb 18;10(2):355. doi: 10.3390/nano10020355.
(1) Background: Carprofen (CP), 2-(6-chlorocarbazole) propionic acid, is used as an anti-inflammatory, analgesic and anti-pyretic agent and it belongs to the family of non-steroidal anti-inflammatory drugs (NSAIDs). CP has some adverse reactions in systemic administration; for this reason, topical administration with CP nanoparticles (CP-NPs) can be an optimal alternative. The main objective of this work is the investigation of ex vivo permeation of CP through different types of porcine mucous membranes (buccal, sublingual and vaginal) and ophthalmic tissues (cornea, sclera and conjunctiva) to compare the influence of CP-NPs formulation over a CP solution (CP-Solution). (2) Methods: The ex vivo permeation profiles were evaluated using Franz diffusion cells. Furthermore, in vivo studies were performed to verify that the formulations did not affect the cell structure and to establish the amount retained () in the tissues. (3) Results: Permeation of CP-NPs is more effective in terms of drug retention in almost all tissues (with the exception of sclera and sublingual). In vivo studies show that neither of the two formulations affects tissue structure, so both formulations are safe. (4) Conclusions: It was concluded that CP-NPs may be a useful tool for the topical treatment of local inflammation in veterinary and human medicine.
(1) 背景：卡洛芬（CP），即2-(6-氯咔唑)丙酸，用作抗炎、镇痛和解热剂，属于非甾体抗炎药（NSAIDs）家族。CP全身给药会产生一些不良反应；因此，用CP纳米颗粒（CP-NPs）局部给药可能是一种最佳选择。本研究的主要目的是研究CP通过不同类型的猪粘膜（颊粘膜、舌下粘膜和阴道粘膜）和眼组织（角膜、巩膜和结膜）的体外渗透情况，以比较CP-NPs制剂与CP溶液（CP-Solution）的影响。(2) 方法：使用Franz扩散池评估体外渗透曲线。此外，进行体内研究以验证制剂不会影响细胞结构，并确定组织中保留的量（）。(3) 结果：就几乎所有组织（巩膜和舌下组织除外）中的药物保留而言，CP-NPs的渗透更有效。体内研究表明，两种制剂均不影响组织结构，因此两种制剂都是安全的。(4) 结论：得出的结论是，CP-NPs可能是兽医和人类医学中局部炎症局部治疗的有用工具。
