Pharmacokinetic and local tissue disposition of [14C]sodium diclofenac following iontophoresis and systemic administration in rabbits

Xiaoying Hui, Angela Anigbogu, Parminder Singh, Glen Xiong, Nicholas Poblete, Puchun Liu, Howard I. Maibach

Research output: Contribution to journal › Article

24 Citations (Scopus)

Abstract

The systemic pharmacokinetics and local drug distribution of sodium diclofenac in skin and underlying tissues was studied. Iontophoresis facilitated local and systemic delivery of diclofenac sodium compared with passive diffusion. The maximum plasma concentration of sodium diclofenac was achieved within 1 h of iontophoresis, and the delivery was proportional to applied current density (371 ± 141 and 132 ± 62 μg/L at 0.5 and 0.2 mA/cm2, respectively). The in vivo delivery efficiency for diclofenac in rabbit was 0.15 mg/mA-h. The concentrations of sodium diclofenac in the skin, subcutanoeus tissue, and muscle beneath the drug application site (cathode) were significantly greater than plasma concentrations and concentrations of drug in similar tissues at the untreated sites. The results thus suggest that the cutaneous microvasculature is not always a perfect "sink" and that transdermal iontophoresis facilitated the direct penetration of diclofenac sodium to deeper tissues. No skin irritation was observed up to 0.5 mA/cm2 current density and 7 mg/mL sodium diclofenac concentration.

Original languageEnglish (US)
Pages (from-to)1269-1276
Number of pages8
JournalJournal of Pharmaceutical Sciences
Volume90
Issue number9
DOIs
StatePublished - 2001

Fingerprint

Iontophoresis
Pharmacokinetics
Diclofenac
Tissue
Rabbits
Skin
Current density
Pharmaceutical Preparations
Plasmas
Microvessels
Muscle
Electrodes
Cathodes
Muscles

Keywords

  • Iontophoresis
  • Local tissue disposition
  • Rabbit
  • Sodium diclofenac

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry
  • Chemistry(all)
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science

Cite this

Pharmacokinetic and local tissue disposition of [14C]sodium diclofenac following iontophoresis and systemic administration in rabbits. / Hui, Xiaoying; Anigbogu, Angela; Singh, Parminder; Xiong, Glen; Poblete, Nicholas; Liu, Puchun; Maibach, Howard I.

In: Journal of Pharmaceutical Sciences, Vol. 90, No. 9, 2001, p. 1269-1276.

Research output: Contribution to journal › Article

Hui, X, Anigbogu, A, Singh, P, Xiong, G, Poblete, N, Liu, P & Maibach, HI 2001, 'Pharmacokinetic and local tissue disposition of [14C]sodium diclofenac following iontophoresis and systemic administration in rabbits', Journal of Pharmaceutical Sciences, vol. 90, no. 9, pp. 1269-1276. https://doi.org/10.1002/jps.1079
Hui X, Anigbogu A, Singh P, Xiong G, Poblete N, Liu P et al. Pharmacokinetic and local tissue disposition of [14C]sodium diclofenac following iontophoresis and systemic administration in rabbits. Journal of Pharmaceutical Sciences. 2001;90(9):1269-1276. https://doi.org/10.1002/jps.1079
Hui, Xiaoying ; Anigbogu, Angela ; Singh, Parminder ; Xiong, Glen ; Poblete, Nicholas ; Liu, Puchun ; Maibach, Howard I. / Pharmacokinetic and local tissue disposition of [14C]sodium diclofenac following iontophoresis and systemic administration in rabbits. In: Journal of Pharmaceutical Sciences. 2001 ; Vol. 90, No. 9. pp. 1269-1276.
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AB - The systemic pharmacokinetics and local drug distribution of sodium diclofenac in skin and underlying tissues was studied. Iontophoresis facilitated local and systemic delivery of diclofenac sodium compared with passive diffusion. The maximum plasma concentration of sodium diclofenac was achieved within 1 h of iontophoresis, and the delivery was proportional to applied current density (371 ± 141 and 132 ± 62 μg/L at 0.5 and 0.2 mA/cm2, respectively). The in vivo delivery efficiency for diclofenac in rabbit was 0.15 mg/mA-h. The concentrations of sodium diclofenac in the skin, subcutanoeus tissue, and muscle beneath the drug application site (cathode) were significantly greater than plasma concentrations and concentrations of drug in similar tissues at the untreated sites. The results thus suggest that the cutaneous microvasculature is not always a perfect "sink" and that transdermal iontophoresis facilitated the direct penetration of diclofenac sodium to deeper tissues. No skin irritation was observed up to 0.5 mA/cm2 current density and 7 mg/mL sodium diclofenac concentration.

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