Abrego Guadalupe, Alvarado Helen, Souto Eliana B, Guevara Bessy, Bellowa Lyda Halbaut, Garduño Maria Luisa, Garcia María Luisa, Calpena Ana C
Department of Physical Chemistry, Faculty of Pharmacy, University of Barcelona, Av. Joan XXIII s/n, 08028 Barcelona, Spain; Department of Biopharmacy and Pharmacology, Faculty of Pharmacy, University of Barcelona, Av. Joan XXIII s/n, 08028 Barcelona, Spain.
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Coimbra (FFUC), Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal; Center for Neuroscience and Cell Biology & Institute for Biomedical Imaging and Life Sciences (CNC-IBILI), University of Coimbra, Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal.
Int J Pharm. 2016 Mar 30;501(1-2):350-61. doi: 10.1016/j.ijpharm.2016.01.071. Epub 2016 Feb 1.
Pranoprofen (PF)-loaded nanoparticles (PF-F1NPs and PF-F2NPs) have been formulated into blank hydrogels (HG_PF-F1NPs and HG_PF-F1NPs) or into hydrogels composed of 3% azone (HG_PF-F1NPs-Azone and HG_PF-F2NPs-Azone), as innovative strategy to improve the biopharmaceutical profile of the selected non-steroidal anti-inflammatory drug (Pranoprofen, PF) for topical application. The purpose of this approach has been to increase the contact of PF with the skin, improve its retention in deeper layers, thus enhancing its anti-inflammatory and analgesic effects. The physicochemical characterization of the developed hydrogels showed a non-Newtonian behaviour, typical of semi-solid formulations for skin administration, with sustained release profile. The results obtained from ex vivo skin human permeation and in vivo anti-inflammatory efficacy studies suggest that topical application of HG_PF-F2NPs has been more effective in the treatment of oedema on the skin' surface in comparison to other hydrogels. No signs of skin irritancy have been detected for all the semi-solid formulations containing 0% or 3% azone.
载有普拉洛芬（PF）的纳米颗粒（PF - F1NP和PF - F2NP）已被制成空白水凝胶（HG_PF - F1NP和HG_PF - F1NP）或由3%氮酮组成的水凝胶（HG_PF - F1NP - 氮酮和HG_PF - F2NP - 氮酮），作为一种创新策略，以改善所选非甾体抗炎药（普拉洛芬，PF）的生物药剂学特性用于局部应用。这种方法的目的是增加PF与皮肤的接触，改善其在更深层的滞留，从而增强其抗炎和镇痛作用。所开发水凝胶的物理化学特性显示出非牛顿行为，这是皮肤给药半固体制剂的典型特征，具有缓释特性。体外皮肤人体渗透和体内抗炎功效研究获得的结果表明，与其他水凝胶相比，HG_PF - F2NP局部应用在治疗皮肤表面水肿方面更有效。对于所有含有0%或3%氮酮的半固体制剂，均未检测到皮肤刺激性迹象。
