Release of 5-fluorouracil from intramuscular w/o/w multiple emulsions.
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 1-14C-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.
Omotosho
J A
JA
Department of Pharmacy, School of Pharmacy and Pharmacology, University of Strathclyde, Glasgow.
Whateley
T L
TL
Florence
A T
AT
D000818:Animals; D004655:Emulsions; D005472:Fluorouracil / Q000008:administration & dosage / Q000032:analysis / Q000493:pharmacokinetics*; D007273:Injections, Intramuscular; D008297:Male; D009132:Muscles / Q000378:metabolism; D009821:Oils; D051381:Rats; D011919:Rats, Inbred Strains; D014867:Water
D004655:Emulsions; D009821:Oils; D014867:Water; D005472:Fluorouracil