Topical bioavailability of diclofenac from locally-acting, dermatological formulations

[Display omitted] 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 penetr...

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Vydáno v:International journal of pharmaceutics Ročník 529; číslo 1-2; s. 55 - 64
Hlavní autoři: Cordery, S.F., Pensado, A., Chiu, W.S., Shehab, M.Z., Bunge, A.L., Delgado-Charro, M.B., Guy, R.H.
Médium: Journal Article
Jazyk:angličtina
Vydáno: Netherlands Elsevier B.V 30.08.2017
Témata:
Administration, Cutaneous
Biological Availability
Dermato-pharmacokinetics
Diclofenac
Diclofenac - administration & dosage
Drug Delivery Systems
Humans
Skin
Skin Absorption
Topical bioavailability
Topical bioequivalence
Q1
A
Q2
FDA
DMSO
MR,jh
Topical bioavailability
MS,n
Diclofenac
MUp,6h
P
SC
IVPT
S
Δ
ANOVA
V
Topical bioequivalence
VS,n
Dermato-pharmacokinetics
HPLC
QR
TEWL
Jinvivo
Jinvitro
MR
MCl,23h
tn
Skin
VR
ISSN:0378-5173, 1873-3476, 1873-3476
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Shrnutí:[Display omitted] 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.
Bibliografie:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0378-5173
1873-3476
1873-3476
DOI:10.1016/j.ijpharm.2017.06.063