Suitability of skin integrity tests for dermal absorption studies in vitro

Guth, Katharina; Schäfer‐Korting, Monika; Fabian, Eric; Landsiedel, Robert; Ravenzwaay, B. van

doi:10.1016/j.tiv.2014.09.007

Cited by 95 publications

(67 citation statements)

References 31 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

Section: Preclinical Pharmacokinetic Evaluationsmentioning

confidence: 99%

“…Transepidermal water loss from the skin or electrical conductivity measurements across the skin are useful for detection of skin damage, physical injury, or pathological conditions. The toxicity of the drug or formulation in the skin also may be investigated (Ashtikar et al, 2013;Pažoureková et al, 2013;Oliveira et al, 2014;Guth et al, 2015).Pharmacokinetic evaluations of a transdermal delivery system are essential to determine the in vivo behavior of the drug administered by the skin route because in vitro studies cannot reproduce the complexity of biological systems, such as metabolism, distribution, and elimination. The contribution of skin absorption by different pathways, such as the epidermis or skin appendages, is also important and may be characterized during the preclinical pharmacokinetic studies (Godin, Touitou, 2007;Farahmand, Maibach, 2009).…”

mentioning

confidence: 99%

See 1 more Smart Citation

Evaluation of skin absorption of drugs from topical and transdermal formulations

Ruela

Perissinato

Lino

et al. 2016

Braz. J. Pharm. Sci.

207

135

View full text Add to dashboard Cite

The skin barrier function has been attributed to the stratum corneum and represents a major challenge in clinical practice pertaining to cutaneous administration of drugs. Despite this, a large number of bioactive compounds have been successfully administered via cutaneous administration because of advances in the design of topical and transdermal formulations. In vitro and in vivo evaluations of these novel drug delivery systems are necessary to characterize their quality and efficacy. This review covers the most well-known methods for assessing the cutaneous absorption of drugs as an auxiliary tool for pharmaceutical formulation scientists in the design of drug delivery systems. In vitro methods as skin permeation assays using Franz-type diffusion cells, cutaneous retention and tape-stripping methods to study the cutaneous penetration of drugs, and in vivo evaluations as pre-clinical pharmacokinetic studies in animal models are discussed. Alternative approaches to cutaneous microdialysis are also covered. Recent advances in research on skin absorption of drugs and the effect of skin absorption enhancers, as investigated using confocal laser scanning microscopy, Raman confocal microscopy, and attenuated total reflectance Fourier-transform infrared spectroscopy, are reviewed. Uniterms:Skin absorption/effects/study. Skin absorption/topical formulations. Skin absorption/ transdermal formulations. Skin absorptions/enhancers. INTRODUCTIONTopical and transdermal drug delivery systems have shown significant advantages in clinical practice for drug targeting to the action site in the body; this has reduced the systemic side effects. The administration of drugs by through the skin is also performed to achieve controlled or prolonged drug delivery, and this route can be explored as an alternative to the oral route. The oral route shows some limitations for drugs with irregular absorption in the gastrointestinal tract and low bioavailability and for drugs with increased first pass metabolism and short plasma halflife times (Barry, 2001;Wokovich et al., 2006;Prausnitz, Langer, 2009;Alexander et al., 2012).Many drug products applied to the skin surface may penetrate to some extent into the skin layers, where their effects are expected. This is the case for topical formulations for treatment of skin disorders such as acne and cutaneous inflammatory diseases that include dermatitis, erythematous lupus, and psoriasis. On the other hand, transdermal formulations release drugs that permeate through the skin and enter the systemic circulation. Transdermal therapy must ensure that significant concentrations of the drug are absorbed to reach effective plasma concentrations. Permeation of drugs is targeted in some cases to body regions close to the action site, where a regional effect is expected, e.g., in the muscles, blood vessels, and articulations. In this way, the term "cutaneous absorption" is properly used to characterize the sum of the amounts of drug that penetrate and permeate the skin (Barry, 2001;El Maghraby, Barry;Willi...

show abstract

Section: Preclinical Pharmacokinetic Evaluationsmentioning

confidence: 99%

mentioning

confidence: 99%

Evaluation of skin absorption of drugs from topical and transdermal formulations

Ruela

Perissinato

Lino

et al. 2016

Braz. J. Pharm. Sci.

207

135

View full text Add to dashboard Cite

show abstract

“…Porcine ear skin was used since its stratum corneum is very similar to that of human stratum corneum [31]. The thickness of the skin was determined as being 1.6 ± 0.4 mm.…”

Section: Biocompatibility Of Photothermally Activable Pegdma-rgo Hydrmentioning

confidence: 99%

Photothermally triggered on-demand insulin release from reduced graphene oxide modified hydrogels

Teodorescu

Quéniat

et al. 2017

Journal of Controlled Release

View full text Add to dashboard Cite

tothermally triggered on-demand insulin release from reduced graphene oxide modified hydrogels. Journal of Controlled Release, Elsevier, 2017Elsevier, , 246, pp.164-173. 10.1016Elsevier, /j.jconrel.2016 Abstract.On-demand delivery of therapeutics plays an essential role in simplifying and improving patient care. The high loading capacity of reduced graphene oxide (rGO) for drugs has made this matrix of particular interest for its hybridization with therapeutics. In this work, we describe the formulation of rGO impregnated poly(ethylene glycol) dimethacrylate based hydrogels (PEGDMA-rGO) and their efficient loading with insulin. Near-infrared (NIR) light induced heating of the PEGDMA-rGO hydrogels allows for highly efficient insulin release. Most importantly, we validate that the NIR irradiation of the hydrogel has no effect on the biological and metabolic activities of the released insulin. The ease of insulin loading/reloading makes this photothermally triggered release strategy of interest for diabetic patients. Additionally, the rGO-based protein releasing platform fabricated here can be expanded towards 'on demand' release of various other therapeutically relevant biomolecules. The table of contents entry: Poly(ethylene glycol) based hydrogels impregnated with rGO allow efficient loading and 'on demand' photothermal release of insulin while preserving its biological and metabolic activity.

show abstract

“…The prepared skin was wrapped in aluminum foil and stored in a deep freezer at −30°C for further use. (32,33) Prior usage methylene blue dye test was performed to assess the skin integrity (34). Ex vivo skin permeation studies were conducted on Franz diffusion cells (PermeGear, Inc., Hellertown, PA, USA).…”

Section: Ex Vivo Permeation Studiesmentioning

confidence: 99%

Benzyl Benzoate-Loaded Microemulsion for Topical Applications: Enhanced Dermatokinetic Profile and Better Delivery Promises

et al. 2015

View full text Add to dashboard Cite

Abstract. Benzyl benzoate (BB) is one of the oldest drugs used for the treatment of scabies and is recommended as the "first-line intervention" for the cost-effective treatment of the disease. Though a promising candidate, its application is reported to be associated with irritation of the skin and eye, resulting in poor patient compliance. Hence, the present study aims to develop BB-loaded topical microemulsion for the safer and effective delivery of BB. Pseudo-ternary phase diagrams with BB as the oily phase itself, along with Tween 80 as surfactant, and mixture of phospholipid and ethanol as the cosurfactant along with aqueous solution as the external phase were constructed and various compositions were formulated. The optimized formulation was characterized for particle-size, zeta-potential, drugcontent, globule-morphology pH, and refractive-index, whereas evaluated for skin permeation, retention, compliance, and dermatokinetics. The nanosized formulation offered threefold higher drug permeation vis-a-vis plain drug solution across LACA mice abdominal skin. The drug retention of the selected formulation was nearly twice of that from the marketed product, assuring depot formulation and sustained release. The skin histopathology revealed the non-irritant nature of the formulation, as no changes in the normal skin histology were observed. The dermatokinetic studies confirmed better permeation and enhanced skin bioavailability of BB to epidermis as well as dermis vis-à-vis the conventional product. The results indicate that the developed lipid-based microemulsion hydrogel can alleviate the concerns associated with BB and can provide a better and safer delivery option in substantial amounts to various skin layers.

show abstract

Suitability of skin integrity tests for dermal absorption studies in vitro

Cited by 95 publications

References 31 publications

Evaluation of skin absorption of drugs from topical and transdermal formulations

Evaluation of skin absorption of drugs from topical and transdermal formulations

Photothermally triggered on-demand insulin release from reduced graphene oxide modified hydrogels

Benzyl Benzoate-Loaded Microemulsion for Topical Applications: Enhanced Dermatokinetic Profile and Better Delivery Promises

Contact Info

Product

Resources

About