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Modifying the release of leuprolide from spray dried OED microparticles

Authors
Journal
Journal of Controlled Release
0168-3659
Publisher
Elsevier
Publication Date
Volume
82
Identifiers
DOI: 10.1016/s0168-3659(02)00165-7
Keywords
  • Leuprolide
  • Controlled Release
  • Drug Delivery
  • Oligosaccharide Ester Derivatives
  • Spray Drying
Disciplines
  • Biology
  • Design
  • Medicine

Abstract

Abstract A range of oligosaccharide ester derivatives (OEDs) have been designed as drug delivery matrices for controlled release. The synthetic hormone analogue, leuprolide, was encapsulated within these matrices using hydrophobic ion pairing and solvent spray drying. The particles produced modified the release of leuprolide in vitro (dissolution in phosphate buffered saline) and in vivo (subcutaneous and pulmonary delivery in the rat). Release rate was dependent on drug loading and could be manipulated by choice of OED and by combining different OEDs in different ratios. Leuprolide encapsulated in the OEDs retained biological activity as evidenced by elevation in plasma luteinising hormone levels following subcutaneous injection of leuprolide recovered from OED particles in vitro prior to in vivo administration.

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