Preservative Activity and in Vivo Percutaneous Penetration of Butylparaben Entrapped in Liposomes

Hideo Komatsu, Kazutaka Higaki, Hirokazu Okamoto, Kazuko Miyagawa, Mitsuru Hashida, Hitoshi Sezaki

Research output: Contribution to journalArticle

21 Citations (Scopus)

Abstract

Butylparaben (BP) was added to liposomes prepared by the hydration method from egg phosphatidylcholine (egg PC), cholesterol, and dicetylphosphate in a molar ratio of 4:2: 1 for the purpose of antimicrobial preservation. Most of the BP was entrapped in liposomes near the polar surface of the lipid bilayers, and rapid equilibrium was observed in its distribution between liposomes and the outer aqueous phase. The antimicrobial activities of liposomes containing BP were studied qualitatively against eight kinds of microorganisms. Although the liposome suspension without BP (empty liposomes) had no effect on the microorganisms, liposome suspensions with BP showed antimicrobial activities. The preservative effect was roughly proportional to the free concentration (not the total concentration) of BP. Percutaneous penetration of liposomes containing BP after topical application was studied in vivo in guinea pigs by autoradiography. 14C-BP in liposomes was observed to penetrate into the body, but no difference was found in its distribution pattern in comparison with that after administration as an ointment. On the other hand, 14C-dipalmitoylphosphatidylcholine, a marker of egg PC, remained on the skin surface and was scarcely detected in the body, suggesting that the percutaneous penetration of liposomes themselves did not occur.

Original languageEnglish
Pages (from-to)3415-3422
Number of pages8
JournalChemical and Pharmaceutical Bulletin
Volume34
Issue number8
DOIs
Publication statusPublished - 1986
Externally publishedYes

Fingerprint

Liposomes
Phosphatidylcholines
Microorganisms
Ovum
Suspensions
butylparaben
1,2-Dipalmitoylphosphatidylcholine
Lipid bilayers
Lipid Bilayers
Ointments
Autoradiography
Hydration
Skin
Guinea Pigs
Cholesterol

Keywords

  • autoradiography
  • butylparaben
  • dipalmitoylphosphatidylcholine
  • liposome
  • percutaneous penetration
  • preservative activity

ASJC Scopus subject areas

  • Chemistry(all)
  • Drug Discovery

Cite this

Preservative Activity and in Vivo Percutaneous Penetration of Butylparaben Entrapped in Liposomes. / Komatsu, Hideo; Higaki, Kazutaka; Okamoto, Hirokazu; Miyagawa, Kazuko; Hashida, Mitsuru; Sezaki, Hitoshi.

In: Chemical and Pharmaceutical Bulletin, Vol. 34, No. 8, 1986, p. 3415-3422.

Research output: Contribution to journalArticle

Komatsu, Hideo ; Higaki, Kazutaka ; Okamoto, Hirokazu ; Miyagawa, Kazuko ; Hashida, Mitsuru ; Sezaki, Hitoshi. / Preservative Activity and in Vivo Percutaneous Penetration of Butylparaben Entrapped in Liposomes. In: Chemical and Pharmaceutical Bulletin. 1986 ; Vol. 34, No. 8. pp. 3415-3422.
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