In vitro and in vivo evaluation of progesterone implants based on new biodegradable poly(glutamic and glutamate esters) copolymers.
New biodegradable polypeptidic copolymers of glutamic acid and tert-butyloxycarbonylmethyl glutamate were evaluated as implantable drug delivery systems. Three copolymers varying in degrees of esterification, which is inversely proportional to the number of glutamic residues, were selected for their range of hydrophilicity and biodegradation rates. Progesterone-containing implants were then prepared by means of an extrusion process and both in vitro and in vivo evaluations were performed. The effects of drug loading, nature, and pH of release medium were investigated. In vitro/in vivo correlations were established for some types of implants. Finally, mathematical fitting of the data, using published models, helped to better understand the mechanisms governing release.
Lescure
F
F
Laboratoires UPSA, Rueil Malmaison, France.
Gurny
R
R
Doelker
E
E
D000818:Animals; D001672:Biocompatible Materials / Q000737:chemistry*; D001673:Biodegradation, Environmental; D004343:Drug Implants; D005069:Evaluation Studies as Topic; D006863:Hydrogen-Ion Concentration; D015233:Models, Statistical; D015394:Molecular Structure; D009842:Oligopeptides / Q000737:chemistry*; D011099:Polyglutamic Acid / Q000737:chemistry*; D011374:Progesterone / Q000008:administration & dosage*; D051381:Rats; D017207:Rats, Sprague-Dawley
D001672:Biocompatible Materials; D004343:Drug Implants; D009842:Oligopeptides; C062244:poly(tert-butyloxycarbonylmethyl)glutamate; D011099:Polyglutamic Acid; D011374:Progesterone