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Skin Delivery (skin + delivery)

Distribution by Scientific Domains

Medical Sciences	100%

Selected Abstracts

Skin delivery of 5-fluorouracil from ultradeformable and standard liposomes in-vitro

JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 8 2001
Gamal M. M. El Maghraby
The potential use of ultradeformable and standard liposomes as skin drug delivery systems was investigated in-vitro. An improved experimental design gave a good measure for skin deposition of drug. This avoided the contamination that can occur due to incomplete washing of the donor before direct determination of the amount of drug in the skin. The design used aqueous ethanolic receptor which is believed to diffuse into skin, disrupting deposited liposomes (if any) and thus releasing both bound and free drug. The receptor fluid was refined by testing different concentrations of ethanol. The applied dose was also optimized. Using the improved design and the optimum dose, an ultradeformable formulation was compared with four traditional liposomes for skin delivery of 5-fluorouracil (5-FU). The best receptor was 50% aqueous ethanol and the optimum dose was 20 ,L. The ultradeformable formulation was superior to standard liposomes in the skin delivery of 5-FU. Of the traditional liposomes, the non-rigid preparation was the best. However, stabilization of the liposome membrane with cholesterol abolished the benefit of this non-rigid preparation. It was concluded that ultradeformable vesicles are promising agents for skin delivery of drugs. [source]

Transdermal delivery of two antioxidants from different cosmetic formulations

INTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Issue 1-2 2003
S. Richert
Synopsis The efficacy of any cosmetic product containing a functional ingredient is determined by the skin delivery of the active molecule, which is influenced by the type of the vehicle and the molecule itself. This study was designed to compare the percutaneous absorption habits of the antioxidants carcinine and lipoic acid out of various formulations by means of the porcine skin model. Initial evaluation of the in vitro porcine skin model has demonstrated its feasibility for various substances and formulations [1, 2]. Increasing legal requirements for risk assessment in the cosmetic industry have led to the development of this alternative test method. The penetration properties are determined by the OECD Guideline TG 428: Skin Absorption: in vitro Method [3, 4], which allows the use of porcine skin for penetration studies. Porcine skin is used because of its similarity to human skin in terms of its morphology and the essential permeation characteristics [5]. The mass balances for each tested formulation type of the antioxidants show individual penetration behaviours with significant differences. The presented data plainly demonstrate that the lipophilic lipoic acid has a distinct higher penetration potential than the hydrophilic carcinine. The chosen vehicle can enhance or reduce the transdermal delivery of both tested antioxidants. Modern effective cosmetic formulations will work only, if the active ingredients penetrate into the epidermis. In conclusion, the correct selection of a suitable formulation plays an important role during product development. Résumé L'efficacité d'un produit cosmétique ou de son principe actif est définie par l'absorption du principe actif par la peau. Cette action est influencée par la structure moléculaire du principe actif ainsi que par la galénique du produit. Dans cette étude, les taux d'absorption percutanée des agents anti-oxydants Carcinine et Acide Lipoïque intégrés dans différentes formulations cosmétiques ont été comparés avec le modèle de peau porcine. La phase de validation sur plusieurs années du modèle peau porcine in vitro a prouvé qu'il se prête très bien à la détermination de la pénétration percutanée de différentes substances et formulations. Des exigences légales de plus en plus sévères concernant la pratique des tests de sécurité pour les produits cosmétiques ont mené au développement de cette méthode qui remplace les essais sur animaux. La définition des qualités de pénétration se fait selon la directive OECD TG 428 : Skin Absorption : in vitro Method [3, 4] qui permet l'utilisation de la peau porcine provenant des abattoirs pour l'exécution des études de pénétration. Les bilans quantitatifs des formulations testées montrent que les agents anti-oxydants ont des comportements de pénétration différant de manière significative. Les données présentées démontrent très clairement que l'acide Lipoïque, lipophile, possède un potentiel de pénétration bien plus élevé que la Carcinine, hydrophile. La base cosmétique peut aussi réduire ou augmenter le potentiel de pénétration des agents anti-oxydant testés. En résumé, le choix correct d'un type de formulation joue un rôle très important dans le développement d'un produit cosmétique. [source]

Effects of lipid nanocarriers on the performance of topical vehicles in vivo

JOURNAL OF COSMETIC DERMATOLOGY, Issue 2 2009
Mojgan Moddaresi PharmD
Summary Background/aims, Nanocarrier systems have been extensively studied for their suitability in personal care formulations. Theoretically, they could enhance skin delivery of active compounds, thereby improving in vivo efficacy of the products. As such the aim of this study was to evaluate the effect of a lipid nanocarrier (LNC) system loaded with tocopheryl acetate (TA) on the hydration, biomechanical properties, and antioxidant capacity of human skin, when used in two different vehicles, and compare it with a non-LNC formulation. Methods, TA-loaded lipid nanocarriers (TA-LNCs) were produced by the phase inversion method, using physiological lipids and purified by ultra-centrifugation. They were incorporated into a hydrophilic gel and foam, and their performance compared with a saturated TA solution in silicon oil. Skin hydration and biomechanical properties were measured by means of a corneometer and a cutometer, respectively, while a high-resolution spectrophotometer was used to assess skin redness after stimulation by methyl nicotinate in a micro-inflammatory test. Both short-term (3 h) and long-term trials (4 weeks) were performed. Results, The results confirmed that the LNCs enhanced skin hydration in both studies, while skin viscoelastic parameters remained practically unchanged during the 4-week study. The antioxidant assessment failed to show significant difference between the test sites. Conclusions, TA-loaded LNCs exhibited the ability to enhance skin hydration, while their effect on skin biomechanical properties and on antioxidant efficacy could not be statistically proved. [source]

Tocopheryl acetate disposition in porcine and human skin when administered using lipid nanocarriers

JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 6 2010
Mojgan Moddaresi
Abstract Objectives Assessing the delivery of a drug into the skin when it has been formulated within a nanocarrier is a complex process that does not conform to the conventions of traditional semi-solid formulations. The aim of this study was to gain a fundamental understanding of drug disposition in both human and porcine skin when applied using a lipidic nanocarrier. Methods A model system was generated by loading tocopheryl acetate into a well-characterised solid lipid nanoparticle and formulating this system as a traditional aqueous hyaluronic acid gel. Franz diffusion cells fitted with a silicone or nylon membrane were used to assess drug and particle transport independently whilst human and pig skin were employed to determine skin delivery. Key findings The tocopheryl acetate, when loaded into the solid lipid nanoparticles, did not release from the particle. However, 1.65 ± 0.90% of an infinite dose of tocopheryl acetate penetrated into the stratum corneum of pig skin when delivered using a nanoparticle-containing gel. Conclusions These results suggest that hydration of the stratum corneum in pig skin could lead to the opening of hydrophilic pores big enough for 50 nm-sized particles to pass into the superficial layers of the skin, a phenomenon that was not repeated in human skin. [source]

Skin hydration and possible shunt route penetration in controlled estradiol delivery from ultradeformable and standard liposomes

JOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 10 2001
Gamal M. M. El Maghraby
Human skin delivery of estradiol from ultradeformable and traditional liposomes was explored, comparing occlusive and open application, with the aim of examining the role of skin hydration. Partially hydrated epidermis was used for open hydration, but fully hydrated membranes were used for occluded studies. In addition, we developed a novel technique to investigate the role of shunt route penetration in skin delivery of liposomal estradiol. This compared delivery through epidermis with that through a stratum corneum (SC)/epidermis sandwich from the same skin with the additional SC forming the top layer of the sandwich. This design was based on the fact that orifices of shunts only occupy 0.1% of skin surface area and thus for SC/epidermis sandwiches there will be a negligible chance for shunts to superimpose. The top SC thus blocks most shunts available on the bottom membrane. If shunts play a major role then the delivery through sandwiches should be much reduced compared with that through epidermis, taking into consideration the expected reduction owing to increased membrane thickness. After open application, both ultradeformable and traditional liposomes improved estradiol skin delivery, with the ultradeformable liposomes being superior. Occlusion reduced the delivering efficiency of both vesicle types, supporting the theory that a hydration gradient provides the driving force. Shunt route penetration was found to play only a very minor role in liposomal delivery. In conclusion, full hydration of skin reduces estradiol delivery from liposomes and the shunt route is not the main pathway for this delivery. [source]