Transdermal Permeation of Caffeine Aided by Ionic Liquids: Potential for Enhanced Treatment of Cellulitis

Author(s)

Hernandes, Audrey N. ^[1] ; Boscariol, Rodrigo ^[1] ; Balcao, Victor M. ^{[2, 3, 1]} ; Vila, Marta M. D. C. ^[1]

Affiliation

^[1] Univ Sorocaba, PhageLab Lab Biofilms & Bacteriophages, BR-18023000 Sorocaba, SP - Brazil

^[2] Univ Aveiro, Dept Biol, Campus Univ Santiago, P-3810193 Aveiro - Portugal

^[3] Univ Aveiro, CESAM, Campus Univ Santiago, P-3810193 Aveiro - Portugal

• Document type: Journal article
• Source: AAPS PHARMSCITECH; v. 22, n. 3 APR 1 2021.
• Web of Science Citations: 0

Abstract

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 (R), 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. (AU)

• FAPESP's process: 18/05522-9 - PsaPhageKill - isolation, characterisation and use of lytic bacteriophages against Pseudomonas syringae PV. actinidiae to fight the cancer of kiwifruit: an efficient and ecofriendly alternative
• Grantee: Vitor Manuel Cardoso Figueiredo Balcão
• Support Opportunities: Scholarships abroad - Research
• FAPESP's process: 16/12234-4 - TransAppIL - Transdermal delivery of structurally and functionally stabilized protein entities applying ionic liquids.
• Grantee: Marta Maria Duarte Carvalho Vila
• Support Opportunities: Regular Research Grants
• FAPESP's process: 16/08884-3 - PneumoPhageColor - development of a colorimetric biodetection kit for Pseudomonas aeruginosa based on phage particles
• Grantee: Vitor Manuel Cardoso Figueiredo Balcão
• Support Opportunities: Regular Research Grants