PhageLab - Laboratory of Biofilms and Bacteriophages, University of Sorocaba, Sorocaba, SP, 18023-000, Brazil.
Department of Biology and CESAM, University of Aveiro, Campus Universitário de Santiago, P-3810-193, Aveiro, Portugal.
AAPS PharmSciTech. 2021 Apr 1;22(3):121. doi: 10.1208/s12249-021-01956-5.
Ginoid hydrolipodystrophy (HDLG) or "cellulite" involves alteration of the cutaneous relief and occurs in 80-90% of the female population. Several topical treatments are available with the use of substances capable of stimulating lipolysis, such as caffeine. However, the effectiveness of topical therapy is related to the processes of release and permeation of the active in skin cells. In this sense, ionic liquids, such as choline geranate, are considered to facilitate topical permeation agents. In this way, the aim of this research was to develop and evaluation of the effectiveness of a cosmetic product for topical treatment of cellulite with caffeine in association with choline geranate. The choline geranate was synthesized by the reaction between geranic acid and choline hydroxide [1: 2]. The gel was prepared using 2% Carpobol 940®, 5% caffeine, and 1% choline geranate. Preliminary and accelerated stability tests were performed by checking pH, spreadability, and organoleptic characteristics. The transdermal permeation capacity of caffeine in vitro was evaluated by the Franz cell permeation assay, and the gel cytotoxicity by the MTS method. To prove the efficacy in the treatment of cellulite, a pilot type 1 clinical trial was carried out. The formulation was considered stable and the product maintained your characteristics during 180 days of storage. The product showed moderate cytotoxicity and high skin permeation capacity. In the clinical trial, it showed results superior to the caffeine gel without ionic liquid. The developed gel favored the cutaneous permeation of caffeine, showing a promising product in the treatment of cellulite.
吉诺型水脂营养不良（HDLG）或“蜂窝组织炎”涉及皮肤起伏的改变，发生在 80-90%的女性人群中。有几种局部治疗方法可使用能够刺激脂肪分解的物质，如咖啡因。然而，局部治疗的效果与活性物质在皮肤细胞中的释放和渗透过程有关。在这方面，离子液体，如胆碱格尔酸盐，被认为可以促进局部渗透剂。因此，本研究的目的是开发和评估含有咖啡因和胆碱格尔酸盐的局部治疗蜂窝组织炎的化妆品的有效性。胆碱格尔酸盐是通过香叶酸和胆碱氢氧化物[1:2]反应合成的。凝胶是用 2%卡波姆 940、5%咖啡因和 1%胆碱格尔酸盐制备的。通过检查 pH 值、铺展性和感官特性进行了初步和加速稳定性测试。通过 Franz 细胞渗透测定法评估了咖啡因的体外透皮渗透能力，并通过 MTS 法评估了凝胶的细胞毒性。为了证明在治疗蜂窝组织炎方面的疗效，进行了 1 型临床试验。制剂被认为是稳定的，产品在储存 180 天内保持其特性。该产品显示出中度细胞毒性和高皮肤渗透能力。在临床试验中，它显示出优于不含离子液体的咖啡因凝胶的结果。开发的凝胶有利于咖啡因的皮肤渗透，在治疗蜂窝组织炎方面是一种有前途的产品。
