Application of new silicone gel to sustained release dosage form of antitumor drug.
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.
Imasaka
K
K
Faculty of Pharmaceutical Sciences, Hoshi University, Tokyo, Japan.
Ueda
H
H
Azuma
T
T
Kawaguchi
T
T
Nagai
T
T
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
D003692:Delayed-Action Preparations; D004343:Drug Implants; D005782:Gels; C069501:Phycon 6600; D020034:Silicone Gels; D012828:Silicones; D005467:Floxuridine