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Release of 5‐fluorouracil from intramuscular w/o/w multiple emulsions
Author(s) -
Omotosho J. A.,
Whateley T. L.,
Florence A. T.
Publication year - 1989
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2510100305
Subject(s) - emulsion , chemistry , aqueous solution , intramuscular injection , aqueous two phase system , chromatography , drug , pulmonary surfactant , in vivo , hexadecane , pharmacokinetics , pharmacology , biochemistry , organic chemistry , medicine , anesthesia , biology , microbiology and biotechnology
Comparative in vivo studies of aqueous solution, multiple w/o/w, and w/o emulsions showed that formulating 5‐fluorouracil in emulsion systems significantly sustained the release of the drug from intramuscular injection sites in the rat. Intramuscular injection of the drug in both w/o and w/o/w emulsion systems produced sustained blood concentrations with a later blood level peak than observed following intramuscular injection of aqueous solutions of the drug. The multiple w/o/w emulsion exhibited a more rapid release of drug from the injection site than the w/o emulsion because of partitioning of the drug to the external aqueous phase during secondary emulsification. The fate of the oil phase following intramuscular injection of a water/hexadecane/water multiple emulsion spiked with 1‐ 14 C‐hexadecane has been studied in rats as a function of stabilizer concentrations. Increasing the lipophilic surfactant (Span 80) concentration facilitated the clearance of the oily vehicle from the injection site, by mechanisms which remain to be elucidated.