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 similar to 250 days. A modification of this formulation by means of a wear coating allows minimisation of the initial burst a feature rarely discussed. (C) 1998 Elsevier Science B.V.