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Scientific article
English

Formation of peptide impurities in polyester matrices during implant manufacturing

Contributors

Rothen-Weinhold, Alexandra Laurence; Oudry, Nathalie; Schwach-Abdellaoui, Khadija; Frutiger-Hughes, Séverine; Hughes, Graham; Jeannerat, Damien; Burger, Ulrich; Besseghir, Kamel; Gurny, Robert

Published in

European journal of pharmaceutics and biopharmaceutics, vol. 49, no. 3, p. 253-257

Publication date

2000

Abstract

Most peptides are susceptible, in vivo, to proteolytic degradation, and it is difficult to formulate and to deliver them without loss of biological activity. In addition, it is often desirable to release them continuously and at a controlled rate over a period of weeks or months. For these reasons, a controlled release system is suitable. Poly(lactic acid) (PLA) is a biocompatible and biodegradable material that can be used for many applications, including the design of injectable controlled release systems for pharmaceutical agents. Development of these delivery systems presents challenges in the assessment of stability, specially for peptide drugs. By means of an extrusion method, long-acting poly(lactic acid) implants containing vapreotide, a somatostatin analogue, were prepared. The nature of the main degradation product obtained after implant manufacturing was elucidated. It was found that the main peptide impurity was a lactoyl lactyl–vapreotide conjugate. Because lactide are found in small quantities in most commercially available PLA, the influence of residual lactide in the polymeric matrix, on the formation of peptide impurities during manufacturing, was specially investigated. This work demonstrates that the degree of purity of the carrier is of great importance with regard to the formation of peptide impurities.

Keywords

  • Peptide
  • Polylactic acid
  • Melt-processing
  • Impurity
  • Vapreotide

UNIGE affiliation entities

Citation (ISO format)

ROTHEN-WEINHOLD, Alexandra Laurence et al. Formation of peptide impurities in polyester matrices during implant manufacturing. In: European journal of pharmaceutics and biopharmaceutics, 2000, vol. 49, n° 3, p. 253–257. doi: 10.1016/S0939-6411(00)00066-7

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Article

Identifiers

Journal ISSN

0939-6411
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Technical informations

Creation

21/06/2010 10:28:37

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21/06/2010 10:28:37

Update

14/03/2023 15:47:17

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