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1.
J Control Release ; 138(1): 32-9, 2009 Aug 19.
Artigo em Inglês | MEDLINE | ID: mdl-19401210

RESUMO

The purpose of this study is to monitor in vivo the effect of chemical penetration enhancers on the delivery of trans-retinol into human skin. Chemical penetration enhancers reversibly alter barrier properties of the SC by disruption of the membrane structures or maximising drug solubility with the skin. So far, most of permeation or penetration experiments are performed in vitro. Raman spectroscopy is uniquely placed to be able to measure biological processes in vivo and this paper shows for the first time that the effect of penetration enhancer on the delivery of trans-retinol can successfully be measured in vivo using this technique. Here, the volar forearm of volunteers was treated with four formulations. One formulation is a highly effective model delivery system identified from ex vivo experiments: trans-retinol in Propylene Glycol (PG)/ethanol, with PG being a well-known and efficient penetration enhancer. The other three formulations are based on 0.3% trans-retinol in Caprylic/Capric Acid Triglyceride (MYRITOL 318), an oil commonly used in skin creams but in two of them a specific penetration enhancer is added. One contains a lipid extractor, Triton X 100, whereas another formulation contains a lipid fluidiser, Oleic Acid. Solutions were applied once and measurements were performed up to 6 h after treatment. Remarkable differences in the delivery of trans-retinol between formulation with or without penetration enhancer can clearly be seen. Moreover, the type of penetration enhancer is also shown to influence the delivery. While using the Oleic Acid, which is a lipid fluidiser, a better delivery of trans-retinol in the skin can be detected. For the first time, the effect of penetration enhancer on the delivery of trans-retinol has been monitored, non invasively in vivo, with time.


Assuntos
Portadores de Fármacos/farmacologia , Octoxinol/farmacologia , Ácido Oleico/farmacologia , Absorção Cutânea/efeitos dos fármacos , Análise Espectral Raman/métodos , Vitamina A/administração & dosagem , Vitaminas/administração & dosagem , Administração Cutânea , Adulto , Química Farmacêutica , Humanos , Masculino , Pessoa de Meia-Idade , Propilenoglicol/farmacologia , Pele/efeitos dos fármacos , Pele/metabolismo , Vitamina A/farmacocinética , Vitaminas/farmacocinética
2.
Appl Spectrosc ; 61(8): 804-11, 2007 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-17716398

RESUMO

The purpose of this study is to monitor in vivo the delivery of trans-retinol into human skin. Delivery to real systems, such as skin, can be extremely difficult to execute and is problematic to confirm and measure. So far, methods for studying the delivery of compounds through the skin are mostly ex vivo and so inherently influence the skin and may not translate directly to the in vivo situation. Raman spectroscopy is uniquely placed to be able to measure biological processes in vivo, and this paper shows that the trans-retinol penetration into the skin can successfully be measured in vivo using this technique. This study measured the volar forearm of volunteers treated with 0.3% trans-retinol in propylene glycol (PG)/ethanol and 0.3% trans-retinol in caprylic/capric acid triglyceride (MYRITOL318), an oil found in skin creams. Solutions were applied and then confocal Raman depth profiles were obtained of the stratum corneum (SC) and into the viable epidermis (VE) up to 10 hours after treatment. Remarkable differences between a penetrating and a nonpenetrating solution can clearly be observed. Treating with trans-retinol in PG/ethanol results in trans-retinol penetrating through the SC and into the VE. Its penetration was also observed to be highly correlated with the depth of penetration of the PG, which is well known as an efficient penetration enhancer. In contrast, while treating with trans-retinol in MYRITOL318, trans-retinol hardly penetrates at all. For the first time, the penetration of trans-retinol has been monitored directly after application of solutions, in vivo without skin excision. Here, the effect of two different solutions on the delivery of trans-retinol into the skin was measured very effectively in vivo by Raman spectroscopy.


Assuntos
Pele/metabolismo , Análise Espectral Raman/métodos , Vitamina A/farmacocinética , Vitaminas/farmacocinética , Administração Cutânea , Adulto , Portadores de Fármacos/farmacocinética , Interações Medicamentosas , Antebraço , Humanos , Masculino , Pessoa de Meia-Idade , Absorção Cutânea , Análise Espectral Raman/instrumentação
3.
J Phys Chem B ; 111(11): 2813-9, 2007 Mar 22.
Artigo em Inglês | MEDLINE | ID: mdl-17402701

RESUMO

In this article, we focus on the influence of side groups on terminal alkyne creation, in aliphatic polymers submitted to swift heavy ions, under vacuum. Terminal alkyne creation was compared in polyethylene and in substituted polymers. We selected two classes of side groups: alkyl groups, which differed in their length (polypropylene and polybutene) and allyl groups, which were linear (EPDMh) or cyclic (EPDMn). Irradiated samples were analyzed using Fourier transform IR spectroscopy, in the transmission mode, at room temperature. Alkynes are created when the electronic stopping power, (dE/dx)e, exceeds a threshold value. This threshold value was moderately influenced by the presence of an alkyl side chain but was clearly reduced in the presence of C=C bonds on the side chain. Nevertheless, in all-saturated polymers, below the (dE/dx)e threshold, terminal alkyne formation is observed after a latent dose, rather independently of the side-chain length and directly related to the formation of radiation-induced double bonds prior to alkyne formation. Under S ion irradiation, the radiation chemical yield G0 value obtained in EPDMh was 4 times the value of G0 in PE. This effect is understandable only if important energy transfers, from the backbone to C=C double bonds, are considered.

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