Penetration enhancer containing vesicles as carriers for dermal delivery of tretinoin

Manconi, Maria; Sinico, Chiara; Caddeo, Carla; Vila, A.O.; Valenti, Donatella; Fadda, Anna Maria

doi:10.1016/j.ijpharm.2011.03.068

Cited by 113 publications

(59 citation statements)

References 26 publications

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“…However, the diversity in the thickness of newborn pig skin regarding the age of animal ranging from only one day old pig (1.2 kg) (Manconi et al, 2011b;Mura et al, 2009) to 40 days old animal (20 kg) needs to be taken into the consideration (Wang et al, 2014).…”

Section: Porcine Skinmentioning

confidence: 99%

In vitro skin models as a tool in optimization of drug formulation

Flaten

Palac²,

Engesland

et al. 2015

European Journal of Pharmaceutical Sciences

182

135

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Abstract(Trans)dermal drug therapy is gaining increasing importance in the modern drug development. To fully utilize the potential of this route, it is important to optimize the delivery of active ingredient/drug into/through the skin. The optimal carrier/vehicle can enhance the desired outcome of the therapy therefore the optimization of skin formulations is often included in the early stages of the product development. A rational approach in designing and optimizing skin formulations requires well-defined skin models, able to identify and evaluate the intrinsic properties of the formulation. Most of the current optimization relies on the use of suitable ex vivo animal/human models.However, increasing restrictions in use and handling of animals and human skin stimulated the search for suitable artificial skin models. This review attempts to provide an unbiased overview of the most commonly used models, with emphasis on their limitations and advantages. The choice of the most applicable in vitro model for the particular purpose should be based on the interplay between the availability, easiness of the use, cost and the respective limitations.

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Section: Porcine Skinmentioning

confidence: 99%

In vitro skin models as a tool in optimization of drug formulation

Flaten

Palac²,

Engesland

et al. 2015

European Journal of Pharmaceutical Sciences

182

135

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“…The PEV formulations were obtained by adding propylene glycol (PG-PEVs) or ethylene glycol (EG-PEVs) to the water phase (10% v/v). The ability of the glycols to improve vesicle performances and stability has been previously probed using synthetic drugs (e.g., diclofenac and tretinoin), natural active molecules (e.g., quercetin and phycocyanin), and also a phytocomplex extracted from Fraxinus angustifolia [16][17][18][19][20][21].…”

Section: Introductionmentioning

confidence: 99%

Faceted phospholipid vesicles tailored for the delivery of Santolina insularis essential oil to the skin

Castangia

Manca

Caddeo

et al. 2015

Colloids and Surfaces B: Biointerfaces

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The aim of this work was to formulate Santolina insularis essential oil-loaded nanocarriers, namely Penetration Enhancer containing Vesicles (PEVs), evaluate the physico-chemical features and stability, and gain insights into their ability to deliver the oil to the skin.Santolina insularis essential oil was obtained by steam distillation, and was predominantly composed of terpenes, the most abundant being β-phellandrene (22.6%), myrcene (11.4%) and curcumenes (12.1%). Vesicles were prepared using phosphatidylcholine, and ethylene or 2 propylene glycol were added to the water phase (10% v/v) to improve vesicle performances as delivery systems. Vesicles were deeply characterized by light scattering, cryogenic transmission electron microscopy and small/wide-angle X-ray scattering, the results showing polyhedral, faceted, unilamellar vesicles of ~115 nm in size. The presence of the glycols improved vesicle stability under accelerated ageing conditions, without changes in size or migration phenomena (e.g., sedimentation and creaming). Confocal laser scanning microscopy images of pig skin treated with Santolina insularis formulations displayed a penetration ability of PEVs greater than that of control liposomes. Moreover, all formulations showed a marked in vitro biocompatibility in human keratinocytes.These findings suggest that the nanoformulation may be of value in enhancing the delivery of Santolina insularis essential oil to the skin, where it can exert its biological activities.

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“…A novel class of lipossomes to promote dermal delivery of TRE was developed and authors observed, as the highest percentage of penetration in porcine skin after 8 hours, no more than 12% (Manconi et al, 2011).…”

Section: Discussionmentioning

confidence: 99%

Tretinoin-based formulations - influence of concentration and vehicles on skin penetration

Bagatin

Wagemaker

Júnior³

et al. 2015

Braz. J. Pharm. Sci.

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3 Pharmacist, External colaborator, Private PharmacyTretinoin is used in the management of acne and it is part of a gold standard treatment for photoaging. It has also been reported as an agent for superficial chemical peeling in highly concentrated formulations with few considerations about skin penetration. The aim of this study was to evaluate the influence of drug concentration and vehicles currently used on skin penetration of tretinoin. In vitro permeation tests were carried out using Franz diffusion cells fitted with porcine ear skin and 10% aqueous methanol in the receptor compartment. Formulations studied, cream or hydroalcoholic dispersion, containing 0.25%, 1% and 5% of tretinoin were placed in the donor compartment for six hours. Tretinoin concentration in skin layers was measured by high performance liquid chromatography. The largest amount of tretinoin from both vehicles was detected in stratum corneum with significant differences among the three concentrations. The hydroalcoholic dispersion was the best vehicle. Significant amounts of tretinoin were found even in deep layers of epidermis. The formulation with 0.25% tretinoin showed better results when considered the amount of tretinoin on skin in terms of percentage. Finally, skin penetration of tretinoin was influenced by vehicle and concentration of this drug used in formulation.Uniterms: Tretinoin/skin penetration/in vitro study. Chemical peeling. Topical formulations/analysis.A tretinoína é usada no tratamento de acne e é considerada como padrão de ouro para o tratamento do fotoenvelhecimento. Em altas concentrações, é relatada como um agente para peeling químico superficial, com poucas considerações sobre a penetração na pele. O objetivo deste estudo foi avaliar a influência da concentração do fármaco e os veículos comumente usados na penetração cutânea da tretinoína. Testes in vitro de penetração foram realizados com células de difusão de Franz equipados com pele da orelha de porco e 10% de solução aquosa de metanol no compartimento receptor. As formulações estudadas, creme ou dispersão hidroalcoólica, contendo 0,25%, 1% e 5% de tretinoína foram colocadas no compartimento doador, durante seis horas. A concentração da tretinoína foi medida por cromatografia líquida de alta eficiência. A maior quantidade de tretinoína foi detectada no estrato córneo com diferenças significativas entre as três concentrações. A dispersão hidroalcoólica foi o melhor veículo. Quantidades significativas de tretinoína foram encontradas nas camadas profundas da epiderme. A formulação com 0,25% de tretinoína mostrou melhores resultados em termos de porcentagem penetrada na pele. Por fim, a penetração de tretinoína na pele foi influenciada pelo veículo e pela concentração desta utilizada na formulação.Unitermos: Tretinoína/penetração na pele/estudo in vitro. Peeling químico. Formulações tópicas/análise.

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Penetration enhancer containing vesicles as carriers for dermal delivery of tretinoin

Cited by 113 publications

References 26 publications

In vitro skin models as a tool in optimization of drug formulation

In vitro skin models as a tool in optimization of drug formulation

Faceted phospholipid vesicles tailored for the delivery of Santolina insularis essential oil to the skin

Tretinoin-based formulations - influence of concentration and vehicles on skin penetration

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