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

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A Correction to this article was published on 28 April 2021

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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®, 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.

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Funding

This work was funded by Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP, São Paulo, Brazil) (FAPESP Refs. No. 2016/08884-3 (Project PneumoPhageColor) and 2016/12234-4 (Project TransAppIL)). Funding for Victor M. Balcão through a BPE grant from FAPESP (São Paulo, Brazil) (Ref. No. 2018/05522-9, Project PsaPhageKill) is hereby gratefully acknowledged. This work also received support from CNPq, National Council for Scientific and Technological Development Brazil, in the form of Research Productivity (PQ) fellowships granted to Victor M. Balcão (Refs. No. 306113/2014-7 and 308208/2017-0).

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Authors and Affiliations

  1. PhageLab - Laboratory of Biofilms and Bacteriophages, University of Sorocaba, Sorocaba, SP, 18023-000, Brazil

    Audrey N. Hernandes, Rodrigo Boscariol, Victor M. Balcão & Marta M. D. C. Vila

  2. Department of Biology and CESAM, University of Aveiro, Campus Universitário de Santiago, P-3810-193, Aveiro, Portugal

    Victor M. Balcão

Authors
  1. Audrey N. Hernandes
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  2. Rodrigo Boscariol
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  3. Victor M. Balcão
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  4. Marta M. D. C. Vila
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Contributions

All authors participated in the conception and design of the experiments and analyzed the resulting data; A.N.H and R.B. performed the experiments; V.M.B. and M.M.D.C.V. wrote the paper. M.M.D.C.V. supervised the work and contributed with reagents and analysis tools. V.M.B. performed the image analysis and revised the paper. All authors have read and agreed to the published version of the manuscript.

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Correspondence to Victor M. Balcão or Marta M. D. C. Vila.

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The original online version of this article was revised: An English translation error occurred with the word usage of “cellulitis” in the title and throughout the article. The correct usage is “cellulite”.

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Hernandes, A.N., Boscariol, R., Balcão, V.M. et al. Transdermal Permeation of Caffeine Aided by Ionic Liquids: Potential for Enhanced Treatment of Cellulite. AAPS PharmSciTech 22, 121 (2021). https://doi.org/10.1208/s12249-021-01956-5

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