Topical bioavailability of diclofenac from locally-acting, dermatological formulations
| Autor: | Annette L. Bunge, Sarah F. Cordery, Richard H. Guy, Andrea Pensado, Wing Sin Chiu, M B Delgado-Charro, M.Z. Shehab |
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| Rok vydání: | 2017 |
| Předmět: |
Drug
Diclofenac Skin Absorption media_common.quotation_subject Biological Availability Pharmaceutical Science 02 engineering and technology Pharmacology Administration Cutaneous Topical bioavailability 030226 pharmacology & pharmacy Article 03 medical and health sciences Drug Delivery Systems 0302 clinical medicine In vivo Dermato-pharmacokinetics Stratum corneum medicine Humans Skin media_common Transepidermal water loss Topical bioequivalence integumentary system Chemistry 021001 nanoscience & nanotechnology Bioavailability medicine.anatomical_structure Drug delivery 0210 nano-technology medicine.drug Subcutaneous tissue |
| Zdroj: | Cordery, S F, Pensado, A, Chiu, W S, Shehab, M Z, Bunge, A L, Delgado-Charro, M B & Guy, R H 2017, ' Topical bioavailability of diclofenac from locally-acting, dermatological formulations ', International Journal of Pharmaceutics, vol. 529, no. 1-2, pp. 55-64 . https://doi.org/10.1016/j.ijpharm.2017.06.063 |
| ISSN: | 0378-5173 |
| DOI: | 10.1016/j.ijpharm.2017.06.063 |
| Popis: | Assessment of the bioavailability of topically applied drugs designed to act within or beneath the skin is a challenging objective. A number of different, but potentially complementary, techniques are under evaluation. The objective of this work was to evaluate in vitro skin penetration and stratum corneum tape-stripping in vivo as tools with which to measure topical diclofenac bioavailability from three approved and commercialized products (two gels and one solution). Drug uptake into, and its subsequent clearance from, the stratum corneum of human volunteers was used to estimate the input rate of diclofenac into the viable skin layers. This flux was compared to that measured across excised porcine skin in conventional diffusion cells. Both techniques clearly demonstrated (a) the superiority in terms of drug delivery from the solution, and (b) that the two gels performed similarly. There was qualitative and, importantly, quantitative agreement between the in vitro and in vivo measurements of drug flux into and beyond the viable skin. Evidence is therefore presented to support an in vivo − in vitro correlation between methods to assess topical drug bioavailability. The potential value of the stratum corneum tape-stripping technique to quantify drug delivery into (epi)dermal and subcutaneous tissue beneath the barrier is demonstrated. |
| Databáze: | OpenAIRE |
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