Development and evaluation in vivo of a long-term delivery system for vapreotide, a somatostatin analogue.
In recent years peptides and proteins have received much attention as candidate drugs. For many peptides, particularly hormones, it is desirable to release the drug continuously at a controlled rate over a period of weeks or even months. Polylactic acid and poly (lactic-co-glycolic) acid are well known biocompatible biodegradable materials with wide applications including the design of controlled-release systems for pharmaceutical agents. Polylactic acid implants containing vapreotide were prepared by an extrusion method and drug release was evaluated in vivo in rats using an RIA method The development of an injectable, biodegradable depot formulation of a somatostatin analogue (vapreotide) is described which ensures satisfactory peptide blood level in rats over approximately 250 days. A modification of this formulation by means of a wear coating allows minimisation of the initial burst a feature rarely discussed.
University of Geneva, School of Pharmacy, Geneva, Switzerland.
A
A
Rothen-Weinhold
K
K
Besseghir
Y
Y
De Zelicourt
R
R
Gurny
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage*; D016503:Drug Delivery Systems; D019344:Lactic Acid / Q000008:administration & dosage; D008297:Male; D008970:Molecular Weight; D011100:Polyglycolic Acid / Q000008:administration & dosage; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000008:administration & dosage; D051381:Rats; D017207:Rats, Sprague-Dawley; D013004:Somatostatin / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics
D000970:Antineoplastic Agents; D011108:Polymers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; C051458:vapreotide; D019344:Lactic Acid; D013004:Somatostatin