Transmucosal Passage of Liposomally-Entrapped Drugs in Rat Small Intestine

Toshikiro Kimura, Kazutaka Higaki, Hitoshi Sezaki

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13 Citations (Scopus)

Abstract

Intestinal absorption of liposomally-entrapped drugs was investigated for egg yolk phosphatidylcholine-cholesterol (2:1 by molar ratio) liposomes (EggPC liposome) and distearoylphosphatidylcholine-cholesterol (2:1) liposomes (DSPC liposome). The release of carboxyfluorescein, an aqueous phase marker, induced by the presence of everted rat intestine was 40 % and 6 % in one hour from DSPC liposomes and EggPC liposomes, respectively, and it is suggested that EggPC liposomes are more stable in the intestinal lumen. The transport of a liposomally-entrapped drug was examined with fluoresceinisothiocyanate-conjugated dextran (FITC-D) as a model drug that has a small mucosal-to-serosal clearance because of its high average molecular weight (64200). The clearance of FITC-D entrapped in DSPC liposomes was largely reduced and could be accounted for by the clearance of the extraliposomal FITC-D concentration in the preparation. On the other hand, the calculated clearance of EggPC liposome-associated FITC-D was similar to or even higher than that of free FITC-D. The serosal appearance of the EggPC liposome-associated drug was inhibited by colchicine, cytochalasin B, and iodoacetate, suggesting that the liposome was incorporated into the epithelial cells by endocytosis. However, the observation that a lipid phase marker, 14C-dipalmitoylphosphatidylcholine, failed to be transported into the serosal fluid indicates the absence of the penetration by an intact liposomal form.

Original languageEnglish
Pages (from-to)221-224
Number of pages4
JournalPharmaceutical Research: An Official Journal of the American Association of Pharmaceutical Scientists
Volume1
Issue number5
DOIs
Publication statusPublished - Sep 1984
Externally publishedYes

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ASJC Scopus subject areas

  • Biotechnology
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry
  • Pharmacology (medical)

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