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1.
Mater Sci Eng C Mater Biol Appl ; 108: 110412, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31923989

RESUMO

Phytochemicals are priceless sources of bioactive compounds with multiple health benefices. The main objective of the current investigation was to develop nanostructured herbal formulations conditioned as appropriate hydrogel (HG) conferring an enhanced transdermal absorption of bioactive compounds from selective extracts and vegetable oils. The direct impact of research is represented by the identification of prototype products which manifest an improved therapeutic response, by means of cumulative antioxidant, anti-inflammatory and anti-acne actions, without causing any side health effects. The combinatorial effect of Carrot Extract (CE) and Marigold Extract (ME) - Nanostructured Lipid Carriers (NLC) based on rosehip oil or black cumin oils was accompanied by a high biocompatibility and a significant ability to capture both short- and long-life free radicals. HG-NLC-ME-CE has been shown to be an efficient carrier with a differentiated potential for in vitro release of the two active principles, e.g. it delayed the release of carotenoids while the hydrophilic active (azelaic acid, AA) was faster released. The HG-NLC efficacy in skin inflammation treatment (demonstrated by in vitro and in vivo tests) revealed a reduced expression of inflammatory cytokines (IL-1ß and TNF-α), more pronounced in the case of TNF-α. Moreover, a superior in vivo anti-inflammatory effect of HG-based NLC-CE/ME-AA as compared to that obtained for a commercial product was detected, i.e. after 3 h of HG-NLC treatment, a significant reduction of rat paw edema was quantified. In pre-clinical studies, the quantification of the hydration and elasticity effects in the viable epidermis provided the evidence of the high potential of developed prototypes, suitable for implementation in the market area. The degree of skin hydration and skin elasticity were remarkable enhanced after topical application of developed prototypes, a hydration effect up to 74% being determined and a skin elasticity reaching 90%. The knowledge acquired from this investigation could be utilized by the cosmetic industry to design novel topical products with improved quality and health benefices, endowed with antioxidant, anti-inflammatory and anti-acne actions and with desired hydration and elasticity profiles, in order to achieve better therapeutic efficacy and no drug toxicity.


Assuntos
Cosméticos/química , Cosméticos/farmacologia , Lipídeos/química , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Óleos de Plantas/química , Óleos de Plantas/farmacologia , Animais , Linhagem Celular , Ensaio de Imunoadsorção Enzimática , Humanos , Hidrogéis/química , Luminescência , Masculino , Nanoestruturas/química , Ratos , Pele/efeitos dos fármacos
2.
Mater Sci Eng C Mater Biol Appl ; 64: 249-259, 2016 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-27127051

RESUMO

The growing scientific interest in exploitation of vegetable bioactives has raised a number of questions regarding their imminent presence in pharmaceutical formulations. This study intends to demonstrate that a dual combination between vegetable oil (e.g. thistle oil, safflower oil, sea buckthorn oil) and a carrot extract represents an optimal approach to formulate safe carrier systems that manifest cell regeneration effect and promising antioxidant and anti-inflammatory activity. Inclusion of both natural actives into lipid carriers imparted a strong negative charge on the nanocarrier surface (up to -45mV) and displayed average sizes of 70nm to 140nm. The entrapment efficiency of carrot extract into nanostructured carriers ranged between 78.3 and 88.3%. The in vitro release study has demonstrated that the entrapment of the extract represents a viable way for an equilibrated release of carotenoids. Besides the excellent antioxidant properties (e.g. scavenging up to 98% of the free oxygen radicals), the results of cellular integrity (e.g. cell viability of 133%) recommend these nanocarriers based on dual carrot extract-bioactive oil as a promising trend for the treatment of certain disorders in which oxidative stress plays a prominent role. In addition, the lipid nanocarriers based on safflower oil and sea buckthorn oil demonstrated an anti-inflammatory effect on LPS induced THP-1 macrophages, by inhibiting the secretion of two pro-inflammatory cytokines, IL-6 and TNF-α.


Assuntos
Anti-Inflamatórios , Antioxidantes , Daucus carota/química , Portadores de Fármacos , Hippophae/química , Nanoestruturas/química , Extratos Vegetais , Óleo de Cártamo , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacocinética , Anti-Inflamatórios/farmacologia , Antioxidantes/química , Antioxidantes/farmacocinética , Antioxidantes/farmacologia , Linhagem Celular Tumoral , Portadores de Fármacos/química , Portadores de Fármacos/farmacocinética , Portadores de Fármacos/farmacologia , Humanos , Camundongos , Tamanho da Partícula , Extratos Vegetais/química , Extratos Vegetais/farmacocinética , Extratos Vegetais/farmacologia , Óleo de Cártamo/química , Óleo de Cártamo/farmacocinética , Óleo de Cártamo/farmacologia
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