title: Application of new silicone gel to sustained release dosage form of antitumor drug.
abstract: The object of this study was to develop a sustained release implantable dosage form of a new silicone gel (PHYCON 6600R) which undergoes addition polymerization to produce a solid gel at ordinary temperature. Implantable PHYCON-drug composites were studied as a means of tumor therapy using 3',5'-diesters of 5-fluoro-2'-deoxyuridine (FUdR-Cn) as a model for antitumor drugs. Using an in vitro dissolution test, we found that the release characteristics of drugs from these preparations could be controlled by the addition of powdered L-alanine. In vivo studies of antitumor activity were carried out, using preparations containing the dodecyl ester (FUdR-C12) by measuring the lifespan of lymphoma-inoculated mice. Antitumor activity, reflected in increased lifespan, was shown to be greater following intraperitoneal administration of the PHYCON formulations (drug and L-alanine) than following injections of the drug alone. Our results suggest that sustained release implantable formulations of antitumor drugs in PHYCON might be suitable for tumor chemotherapy.
authors.affiliation: Faculty of Pharmaceutical Sciences, Hoshi University, Tokyo, Japan.
authors.forename: K
authors.initials: K
authors.lastname: Imasaka
authors.forename: H
authors.initials: H
authors.lastname: Ueda
authors.forename: T
authors.initials: T
authors.lastname: Azuma
authors.forename: T
authors.initials: T
authors.lastname: Kawaguchi
authors.forename: T
authors.initials: T
authors.lastname: Nagai
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004343:Drug Implants / Q000493:pharmacokinetics; D005467:Floxuridine / Q000008:administration & dosage* / Q000493:pharmacokinetics / Q000494:pharmacology; D005782:Gels; D008223:Lymphoma / Q000188:drug therapy / Q000473:pathology; D008297:Male; D051379:Mice; D009368:Neoplasm Transplantation; D020034:Silicone Gels; D012828:Silicones / Q000493:pharmacokinetics* / Q000494:pharmacology
chemical_list: D003692:Delayed-Action Preparations; D004343:Drug Implants; D005782:Gels; C069501:Phycon 6600; D020034:Silicone Gels; D012828:Silicones; D005467:Floxuridine