Influence of drug content, type of semi-solid vehicle and rheological properties on the skin penetration of the model drug fludrocortisone acetate

Nagelreiter, C.; Raffeiner, S; Geyerhofer, C; Klang, Victoria; Valenta, Claudia

doi:10.1016/j.ijpharm.2013.03.042

Cited by 34 publications

(16 citation statements)

References 27 publications

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“…The W/O type vehicle was found to be the superior to other vehicles (Nagelreiter et al, 2013). Hathout et al (2010) reported on the optimization of microemulsion composition for transdermal delivery of testosterone using the dermatomed dorsal porcine skin.…”

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

179

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

179

135

View full text Add to dashboard Cite

show abstract

“…Vehicle composition has been shown to influence the release properties of the incorporated drug and the penetration ability across/into the skin and may also improve the skin condition 3,4,33 . To examine the effect of the vehicle on the release of liposomally entrapped diclofenac sodium, different types of liposomes were incorporated into the following vehicles: the hydrogel, the cream base (O/W emulsion) and DMS base.…”

Section: Liposomes-in-vehicle Formulationsmentioning

confidence: 99%

Elastic liposomes-in-vehicle formulations destined for skin therapy: the synergy between type of liposomes and vehicle

Palac

Hurler

Škalko‐Basnet

et al. 2014

Drug Development and Industrial Pharmacy

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Objective: The present study is focused on optimization of elastic liposomes-in-vehicle formulations in respect to drug release and formulation properties. By combining penetration potential of elastic liposomes containing high ratio of entrapped drug and physicochemical properties of vehicles, both affecting the release and texture properties, optimal formulation could be achieved. Materials and methods:Deformable, propylene glycol-containing or conventional liposomes with hydrophilic model drug (diclofenac sodium) were incorporated into the following vehicles appropriate for skin application: a hydrogel, a cream base and derma membrane structure base cream (DMS base). Each formulation was assessed for in vitro drug release and mechanical properties. Results and discussion:The composition and type of both liposomes and the vehicle affected the rate and amount of the released drug. The cream base exhibited the slowest release, followed by the hydrogel and DMS base. Similar release profiles were achieved with both types of elastic vesicles (deformable and propylene glycol liposomes); the slowest release was observed for conventional liposomes, regardless of the vehicle used. The drug release profiles from different liposomes-in-vehicle formulations were in agreement with the physicochemical properties of the formulations. All of the liposomes were found to be compatible with the hydrogel preserving its original textures, whereas a significant decrease in all texture parameters was observed for liposomes-in-DMS base, regardless of liposome type. Conclusion:Propylene glycol liposomes-in-hydrogel is considered as the optimal formulation for improving skin delivery of hydrophilic drug. Further investigations involving in vivo animal studies are necessary to confirm its applicability in skin therapy. INTRODUCTIONEffective (trans)dermal drug delivery depends on both the selection of an appropriate drug and the properties of the delivery system (vehicle). Vehicles exert pronounced effects on the epidermis, affecting hydration, lubrication, drying, skin smoothness, occlusion and protection.In addition, the physicochemical properties of vehicles influence the pharmacokinetic properties of the incorporated drug by controlling its release from the vehicle and affecting penetration through the stratum corneum, permeation through the layers of skin and absorption into the blood. Preparation and characterization of liposomesDeformable, propylene glycol and conventional liposomes were prepared by the film 6The mean diameters, size distributions (polydispersity) and zeta potentials of the liposomes were determined by photon correlation spectroscopy (Zetasizer 3000HS, MalvernInstruments, Malvern, UK) 20,21 . Membrane elasticity of extruded liposomes was evaluated by home-made device at an external pressure of 5 bar using 100-nm membranes. Detailed procedure with equation for calculation of the deformability degree (E) has been previously described in details 14,19 . Separation of the unentrapped drug was performed usin...

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“…When tape stripping was started, care was taken to register whether or not the strips adhered to the skin. The first strip which adhered to the skin as observed by the experimenter was carefully noted and all strips preceding this one were termed "pre-strips" (Nagelreiter et al, 2013). Immense care was taken not to allow the non-adhering strips to shift on the ears due to the lipid contents of the formulations and 20 sequential tape strips were removed, noting when the first strip adhered to the skin.…”

Section: Protocol B -Excess Of Formulation Left Onmentioning

confidence: 99%

“…The method used is based on previously reported works (Cisternino et al, 2003;Höller and Valenta, 2007;Nagelreiter et al, 2014Nagelreiter et al, , 2013. The mobile phase consisted of acetonitrile:water in the ratio 40:60 (v/v), degassed prior to use, employed with a flow rate of 0.8 ml/min and an oven temperature of 50 C. Detection wavelength was set to 240 nm, retention time was approximately 7 min.…”

Section: Fludrocortisone Acetate (Fa)mentioning

confidence: 99%