Nanoemulsion containing caffeine for cellulite treatment: characterization and in vitro evaluation

Abstract

The Ginoide Hydrolipodystrophy (GHLD), commonly known as cellulite, occurs in 80-90% of the female population after the puberty period and comes from a metabolic modification in the cutaneous adipose tissue. Caffeine has been used in topical formulations due to its lipolytic action. We studied a nanoemulsion (F3) containing caffeine with two surfactants (oleth-3 and oleth-20) by emulsification method by phase inversion temperature inversion (PIT). The polydispersion indices (PDI) showed the reduced deviation of 0.1. The mean droplet size was ~ 40 nm. The evaluated constant of Ostwald, in the refrigerator condition was the most favorable during the stability test. In the In Raman spectroscopy assay, the caffeine bands found in F3 were compatible with those found in the caffeine solution (1337, 652.5 and 558.2 cm-1). There was no interaction of caffeine anhydrous with other ingredients in nanoemulsion. In the in vitro safety assay the result of 1.4 ranked the F3 as slightly irritating. In the natural membrane, cutaneous permeation test (human skin) permeate concentrations did not exceed the saturation concentration of the PBS buffer (48.96 μg/3 mL). The caffeine solution and F3 permeated statistically equal, but the nanoemulsion visually and sensorially improved the caffeine precipitation.

Cellulite: Presentation and management

“…There have been efforts to produce nanoemulsion containing caffeine with addition of surfactants for overcoming this challenge. 19 According to the results of an animal study, emulsion with siloxanetriol alginate caffeine can promote the lipolytic action on fatty tissue whereas sodium benzoate addition to the preparations can inhibit efficiency of caffeine. 20 Formulation developments thus may play a role in efficacy of topical caffeine containing formulations.…”

“…However, there are limitations for use of caffeine, one of them being tendency to precipitate and result in clumps formation depending on the vehicle. There have been efforts to produce nanoemulsion containing caffeine with addition of surfactants for overcoming this challenge 19 . According to the results of an animal study, emulsion with siloxanetriol alginate caffeine can promote the lipolytic action on fatty tissue whereas sodium benzoate addition to the preparations can inhibit efficiency of caffeine 20 .…”

Celulite: uma breve revisão / Cellulite: a brief review

“…têm sido desenvolvidas para o tratamento da celulite. Entre os ativos utilizados estão as metilxantinas (cafeína, teofilina, aminofilina), retinol, fosfatidilcolina, L-carnitina, ginkgo biloba, nicotinato de metila, mentol, cânfora e silício (BALDISSERA, 2014;FREIRE et al, 2019).…”

“…A cafeína atua sobre o metabolismo dos adipócitos e promove a inibição da enzima fosfodiesterase, o que causa um aumento na disponibilidade celular de adenosina monofosfato cíclico (cAMP). Este mecanismo resulta na lise do triacilglicerol, resultando em ácido graxo e glicerol (FREIRE et al, 2019). Já os retinóides reduzam a celulite, aumentando a espessura dérmica, aumentando a angiogênese, sintetizando novos componentes do tecido conectivo e aumentando o número de fibroblastos ativos (SADICK, 2019).…”

Mucocele Do Apêndice Mucocele of the Appendix

“…Formulações cosméticas tópicas com ingredientes ativos visando o aumento do fluxo estimulador microvascular e linfático, efeitos anti-inflamatórios e efeitos lipolíticos têm sido desenvolvidas para o tratamento da celulite. Entre os ativos utilizados estão as metilxantinas (cafeína, teofilina, aminofilina), retinol, fosfatidilcolina, L-carnitina, ginkgo biloba, nicotinato de metila, mentol, cânfora e silício (BALDISSERA, 2014;FREIRE et al, 2019).…”