Delivery of nalbuphine and its prodrugs across skin by passive diffusion and iontophoresis

K. C. Sung, Jia You Fang, Oliver Yoa-Pu Hu

Research output: Contribution to journalArticle

53 Citations (Scopus)

Abstract

The in vitro transport of nalbuphine (NA) and its prodrugs across various skins was investigated in order to assess the effects of prodrug lipophilicity on passive as well as iontophoretic permeation. The passive diffusion of NA and its prodrugs increased with the drug lipophilicity. Iontophoresis significantly increased the transport of NA and its prodrugs; the enhancement ratio was highest for NA and decreased as the drug lipophilicity increased. Measurements using intact and stratum corneum (SC)-stripped skins showed that the SC was the major skin diffusion barrier for the passive permeation of NA and nalbuphine pivalate (NAP). The iontophoretic permeation of NA and NAP across intact and SC-stripped skins indicated that the SC layer was not rate-limiting for the permeation of NA, but remained the rate-limiting barrier for transdermal permeation of NAP. Permeation studies using SC-stripped and delipidized skins suggested that the intercellular pathway was the predominant route for the passive permeation of NA and NAP as well as the iontophoretic permeation of NAP across the SC. The relative rates of passive and iontophoretic permeation across Wistar rat skins demonstrated that a significant amount of NA may permeate skin via the appendageal routes, whereas NAP permeated predominantly through the lipid matrix. Copyright (C) 2000 Elsevier Science B.V.

Original languageEnglish
Pages (from-to)1-8
Number of pages8
JournalJournal of Controlled Release
Volume67
Issue number1
DOIs
Publication statusPublished - Jun 15 2000
Externally publishedYes

Fingerprint

Nalbuphine
Iontophoresis
Prodrugs
Cornea
Skin
Pharmaceutical Preparations
nalbuphine pivalate
Wistar Rats

Keywords

  • Iontophoresis
  • Nalbuphine
  • Nalbuphine prodrug
  • Transdermal delivery

ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Delivery of nalbuphine and its prodrugs across skin by passive diffusion and iontophoresis. / Sung, K. C.; Fang, Jia You; Yoa-Pu Hu, Oliver.

In: Journal of Controlled Release, Vol. 67, No. 1, 15.06.2000, p. 1-8.

Research output: Contribution to journalArticle

Sung, K. C. ; Fang, Jia You ; Yoa-Pu Hu, Oliver. / Delivery of nalbuphine and its prodrugs across skin by passive diffusion and iontophoresis. In: Journal of Controlled Release. 2000 ; Vol. 67, No. 1. pp. 1-8.
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