Tabletted polylactide microspheres prepared by a w/o emulsion-spray drying method

J Microencapsul. 2000 Nov-Dec;17(6):711-20. doi: 10.1080/02652040050161701.

Abstract

An emulsification-spray drying technique is used to prepare poly(D,L-lactic acid) (PDLLA) microparticles loaded with a water soluble, non-steroidal anti-inflammatory drug (NSAID), sodium naproxen (NaNPX). The method involves the preparation of a w/o emulsion in which the water soluble drug is dissolved in the aqueous dispersed phase, while the polymer is dissolved in the organic continuous phase. As a comparison, microparticles were prepared by spraying a suspension of the drug into an organic solution of the polymer. The spray-dried particles were characterized using SEM, DSC, XRD and in vitro release tests. The spray-dried product was then compressed (direct compression) to obtain controlled release matrix tablets. All microparticles release NaNPX within 30 min. The matrix tablets release the drug in 8-10 h; the matrix tablets characterized by the presence of surfactant (due to the emulsion used to obtain the microparticles) have the highest release rate.

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
  • Biocompatible Materials
  • Capsules
  • Delayed-Action Preparations
  • Drug Compounding
  • Emulsions
  • Humans
  • In Vitro Techniques
  • Microscopy, Electron, Scanning
  • Microspheres*
  • Naproxen / administration & dosage
  • Naproxen / pharmacokinetics
  • Polyesters*
  • Tablets

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Biocompatible Materials
  • Capsules
  • Delayed-Action Preparations
  • Emulsions
  • Polyesters
  • Tablets
  • poly(lactide)
  • Naproxen