Microencapsulation of hydrophilic drug substances using biodegradable polyesters. Part II: Implants allowing controlled drug release--a feasibility study using bisphosphonates

J Microencapsul. 2004 Mar;21(2):137-49. doi: 10.1080/02652040310001637857.

Abstract

The prolonged delivery of hydrophilic drug salts from hydrophobic polymer carriers at high drug loading is an ambitious goal. Pamidronate disodium salt (APD) containing implants prepared from spray-dried microparticles were investigated using a laboratory ram extruder. An APD-containing polymer matrix consisting of an APD-chitosan implant embedded in the biodegradable polymer D,L-poly(lactide-co-glycolide acid-glucose) (PLG-GLU) was compared with a matrix system with the micronized drug distributed in the PLG-GLU. The APD-chitosan matrix system showed a triphasic release behaviour at loading levels of 6.86 and 15.54% (w/w) over 36 days under in-vitro conditions. At higher loading (31.92%), a drug burst was observed within 6 days due to the formation of pores and channels in the polymeric matrix. In contrast, implants containing the micronized drug showed a more continuous release profile over 48 days up to a loading of 31.78% (w/w). At a drug loading of 46.17% (w/w), a drug burst was observed. Using micronized drug salts and reducing the surface area available for diffusion, parenteral delivery systems for highly water-soluble drug candidates were shown to be technically feasible at high drug loadings.

MeSH terms

  • Adjuvants, Pharmaceutic
  • Anti-Inflammatory Agents
  • Biocompatible Materials
  • Biodegradation, Environmental
  • Chitin* / analogs & derivatives*
  • Chitosan
  • Diphosphonates*
  • Drug Compounding / methods*
  • Drug Implants*
  • Feasibility Studies
  • Lactic Acid
  • Microscopy, Electron, Scanning
  • Microspheres
  • Pamidronate
  • Polyesters
  • Polyglycolic Acid
  • Sucrose
  • Surface Properties

Substances

  • Adjuvants, Pharmaceutic
  • Anti-Inflammatory Agents
  • Biocompatible Materials
  • Diphosphonates
  • Drug Implants
  • Polyesters
  • polymer D,L-poly(lactide-co-glycolide acid-glucose)
  • Chitin
  • Polyglycolic Acid
  • Lactic Acid
  • Sucrose
  • Chitosan
  • Pamidronate