Formulation and statistical optimization of novel double-incorporated PLA-PLGA microparticles within an alginate-pectinate platform for the delivery of nicotine

J Microencapsul. 2006 Mar;23(2):153-67. doi: 10.1080/02652040500435139.

Abstract

The application of nicotine in the research phase of Alzheimer's disease (AD) treatment has shown promise. The present study was aimed at understanding the incorporation of nicotine into poly-lactic acid (PLA) and poly(D,L-lactic-co-glycolic) acid (PLGA) microparticles which were then re-incorporated into a cross-linked zinc-alginate-pectinate polyspheric multi-particulate system to be employed as a possible brain implant for the treatment of AD. The Box-Behnken design was employed to prepare 15 PLA-PLGA formulations, which were tested for their drug incorporation efficiency and release potential and subsequently optimized using multiple regression and an artificial neural network generalized feed-forward model. Based on the rapid burst effect from the microparticles, further incorporation was conducted in a zinc-alginate-pectinate system using ionotropic gelation. Although double incorporation continued to provide a burst effect, this was followed by a lag period for 7 days and a second phase of drug release.

MeSH terms

  • Alginates / chemistry*
  • Alginates / ultrastructure
  • Algorithms
  • Cross-Linking Reagents
  • Delayed-Action Preparations
  • Drug Carriers
  • Drug Compounding
  • Drug Delivery Systems*
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / chemistry
  • Lactic Acid / chemistry*
  • Microspheres
  • Nicotine / administration & dosage*
  • Nicotine / metabolism
  • Particle Size
  • Polyglycolic Acid / chemistry*
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polymers / chemistry*
  • Regression Analysis

Substances

  • Alginates
  • Cross-Linking Reagents
  • Delayed-Action Preparations
  • Drug Carriers
  • Hexuronic Acids
  • Polymers
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • Nicotine
  • Glucuronic Acid