Formulações nanoestruturadas contendo a associação coenzima Q10 e vitamina e acetato: desenvolvimento e avaliação de atividades biológicas

Abstract

Coenzyme Q10 is an endogenous synthesized molecule that presents antioxidant activity and acts on cellular respiration process and ATP synthesis. Besides, it presents neuroprotective effect, anti-inflammatory and hepatoprotective effects, among others. However, this molecule has high molecular weight, poor water solubility and, consequently, low bioavailability when administered by the oral route. Besides, coenzyme Q10 is photolabile, that difficults its therapeutic use. In this sense, nanocarriers constitute an interesting alternative to the delivery of this active substance. In the first step, this study aimed the development of poly- - caprolactone nanocapsules containing the association of two antioxidant compounds, coenzyme Q10 and vitamin E acetate, and the evaluation of the photodegradation of Q10 associated to nanostructures and their in vitro antitumoral effect. This nanocapsule suspensions presented suitable physicochemical characteristics for this type of drug delivery system, high encapsulation efficiency rates and drug content. It was also verified the influence of vitamin E concentration on coenzyme Q10 degradation by ultraviolet C radiation exposure, which was smaller with the increase of vitamin E concentration. Moreover, nanoencapsulated coenzyme Q10 and vitamin E reduced cell viability of tumoral cells melanoma (A375 line) and glioma (C6 line). In the second part of this work, semisolid formulations were prepared from nanocapsule suspensions by the addition of gellan gum, a natural polysaccharide. These formulations were employed in the investigation of the antiedematogenic, anti-inflammatory and antioxidant effects in a model of ear edema induced by ultraviolet radiation type B (UVB) in mice. All formulations tested, excepting the vehicle (gellan gum and water), led to a reduction of the ear edema in mice and in the activities of the enzymes myeloperoxidase (MPO; marker of neutrophil infiltration in the tissue) and -N-acetylglucosaminidase (NAGase; marker of macrophage infiltration). Besides, semisolid formulations containing nanoencapsulated coenzyme Q10 led to a decrease on oxidative stress biomarkers levels (nonproteic thiols and lipid peroxidation). Considering obtained results, developed formulations of coenzyme Q10 and vitamin E acetate are an interesting alternative to the control of tumoral cells growing, as well as to inflammatory skin wounds induced by UVB radiation.