Polyester-based microparticles of different hydrophobicity: the patterns of lipophilic drug entrapment and release

J Microencapsul. 2016 May;33(3):199-208. doi: 10.3109/02652048.2016.1144818. Epub 2016 Feb 18.

Abstract

The paper is devoted to the investigation of the effect of polyester hydrophobicity and ability for crystallisation on lipophilic drug loading and release from microparticles fabricated on the base of these polymers. Poly(l-lactic acid), poly(d, l-lactic acid) and poly (lactic acid-co-glycolic acid) were synthesised by ring-opening polymerisation using stannous octoate as catalyst, while poly(caprolactone) (PCL) and poly(ω-pentadecalactone) (PPDL) formation was catalysed by lipase. The particles were formed via single emulsion evaporation/diffusion method. The particles obtained were studied using SEM, XRD and DSC methods. The degradation of particles based on different polyesters, entrapment and release of a model hydrophobic drug (risperidone®) were thoroughly studied. The effect of particles hydrophobicity and crystallinity on these parameters was of most interest. The drug entrapment is greater for the hydrophobic polymers. Drug release was more rapid from crystalline particles (PLLA, PCL, PPDL), than from amorphous PDLLA and PLGA ones.

Keywords: Biodegradable particles; drug encapsulation; drug release; risperidone.

MeSH terms

  • Antipsychotic Agents / administration & dosage*
  • Antipsychotic Agents / chemistry
  • Crystallization
  • Delayed-Action Preparations / chemistry*
  • Dopamine Antagonists / administration & dosage*
  • Dopamine Antagonists / chemistry
  • Drug Liberation
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • Lactic Acid / chemistry
  • Macrolides / chemistry
  • Polyesters / chemistry*
  • Polyglycolic Acid / chemistry
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Risperidone / administration & dosage*
  • Risperidone / chemistry
  • U937 Cells

Substances

  • Antipsychotic Agents
  • Delayed-Action Preparations
  • Dopamine Antagonists
  • Macrolides
  • Polyesters
  • omega-pentadecalactone
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • polycaprolactone
  • Polyglycolic Acid
  • Lactic Acid
  • poly(lactide)
  • Risperidone