Oral delivery and fate of poly(lactic acid) microsphere-encapsulated interferon in rats

J. E. Eyles, H. O. Alpar, B. R. Conway, M. Keswick

Research output: Contribution to journalArticle

18 Citations (Scopus)

Abstract

In the light of previous findings which suggest that particulate material can be absorbed and thence systemically disseminated from the gastrointestinal tract, we have investigated the oral uptake and distribution of soluble and microsphere-encapsulated radiolabelled interferon-γ. For trace-loaded (0.01% w/w interferon) microspheres, a quite different distribution of radioactivity was observed in-vivo 15 and 240 min after oral administration in comparison with the control group which received equivalent doses of unencapsulated interferon-γ. Thyroid gland activity in control animals killed at these times was significantly higher than that detected in those rodents receiving trace amounts of microencapsulated interferon-γ (P ≤ 0.05). For poly(L-lactide) particles with higher interferon loadings (0.97% w/w interferon-γ) the distinction between the two experimental groups was less significant. During incubation in-vitro, the trace-loaded particles released a significantly lower percentage of interferon-γ in comparison with 0 97% w/w loaded microspheres (P ≤ 1). Bio-distribution data from rats treated orally with trace amounts of unencapsulated and microencapsulated interferon-γ leads us to the tentative conclusion that microencapsulation of proteins markedly affects oral uptake, and possibly post-absorption pharmacokinetic parameters also.

Original languageEnglish
Pages (from-to)669-674
Number of pages6
JournalJournal of Pharmacy and Pharmacology
Volume49
Issue number7
DOIs
Publication statusPublished - 1 Jul 1997
Externally publishedYes

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Microspheres
Interferons
Drug Compounding
poly(lactic acid)
Radioactivity
Oral Administration
Gastrointestinal Tract
Rodentia
Thyroid Gland
Pharmacokinetics
Control Groups
Proteins

Cite this

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abstract = "In the light of previous findings which suggest that particulate material can be absorbed and thence systemically disseminated from the gastrointestinal tract, we have investigated the oral uptake and distribution of soluble and microsphere-encapsulated radiolabelled interferon-γ. For trace-loaded (0.01{\%} w/w interferon) microspheres, a quite different distribution of radioactivity was observed in-vivo 15 and 240 min after oral administration in comparison with the control group which received equivalent doses of unencapsulated interferon-γ. Thyroid gland activity in control animals killed at these times was significantly higher than that detected in those rodents receiving trace amounts of microencapsulated interferon-γ (P ≤ 0.05). For poly(L-lactide) particles with higher interferon loadings (0.97{\%} w/w interferon-γ) the distinction between the two experimental groups was less significant. During incubation in-vitro, the trace-loaded particles released a significantly lower percentage of interferon-γ in comparison with 0 97{\%} w/w loaded microspheres (P ≤ 1). Bio-distribution data from rats treated orally with trace amounts of unencapsulated and microencapsulated interferon-γ leads us to the tentative conclusion that microencapsulation of proteins markedly affects oral uptake, and possibly post-absorption pharmacokinetic parameters also.",
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Oral delivery and fate of poly(lactic acid) microsphere-encapsulated interferon in rats. / Eyles, J. E.; Alpar, H. O.; Conway, B. R.; Keswick, M.

In: Journal of Pharmacy and Pharmacology, Vol. 49, No. 7, 01.07.1997, p. 669-674.

Research output: Contribution to journalArticle

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