Non-ionic surfactant based vesicular drug delivery system for topical delivery of caffeine for treatment of cellulite: design, formulation, characterization, histological anti-cellulite activity, and pharmacokinetic evaluation

Abstract

Cellulite is a common topographical alteration where skin acquires an orange peel or mattress appearance with alterations in adipose tissue and microcirculation. This work aims to develop and evaluate a topical niosomal gel formulae with good permeation to reach the subcutaneous fat layer. Several caffeine niosomal dispersions were prepared and incorporated into gel formulae using Carbopol 940 polymer, chemical penetration enhancers, and iontophoresis, then the prepared gels were applied onto the skin of rats and anticellulite activity of caffeine from the prepared gels compared to that of the commercial product Cellu Destock was evaluated by histological study of the skin and measurement of plasma level of caffeine passing through the skin using liquid chromatography (LC/MS-MS). Results of histology revealed reduction of size and thickness of fatty layer of rat skin in the following order: FVII > FXIV > Cellu Destock > FVII + Iontophoresis > FXIV + Iontophoresis. Pharmacokinetic results of caffeine in plasma revealed that C, T, and AUC decreased in the following order: FXIV > FVII > Cellu Destock. These results conclude that incorporation of caffeine niosomal dispersion into gel matrix with penetration enhancers and iontophoresis resulted in improvement in penetration of caffeine through the skin into the underlying fatty layer in treatment of cellulite.

Transdermal Delivery of Telmisartan: Formulation, in vitro, ex vivo, Iontophoretic Permeation Enhancement and Comparative Pharmacokinetic Study in Rats

“…For incorporation of the best 3 formulae into a gel, 1.5% (w/v) of carbopol 940 was soaked into the prepared formulae (10mL of 40mg/mL) overnight before gelation, and then 0.5% (w/w) of triethanolamine was added to obtain a clear gel, adjust viscosity and PH. 22 The prepared gels were characterized for appearance, viscosity, PH, in vitro drug release, and ex vivo drug permeation to select the best formula.…”

Recent advances in non-ionic surfactant vesicles (niosomes): Fabrication, characterization, pharmaceutical and cosmetic applications

“…Further, a higher plasma concentration of caffeine was observed in the niosomal group, indicating that incorporation of caffeine into a niosomal system improved penetration through the skin and into the underlying fatty layer. This presents a promising approach for the formulation of a transdermal anti-cellulite product of caffeine in a niosomal gel system with improved transdermal bioavailability (147). Similarly, a transdermal gel prepared with elastic niosomes loaded with papain has been investigated in comparison with polymeric nanoparticles.…”

Skin Targeting of an Optimized Caffeine Nanostructured Lipid Carrier With Improved Efficiency Against Chemotherapy Induced Alopecia

“…Caffeine or trimethylxanthine, is an alkaloid that acts as an adenosine receptor antagonist with anti-inflammatory and psychotropic actions. It is a weakly basic drug that has a high water solubility of 20 mg/ml, pKa of 10.4, and logP of-0.07(a hydrophilic model drug with poor skin permeability) [7]. Caffeine has revealed valuable effects on androgenic alopecia due to its influence on hair growth stimulation and hair loss prevention.…”