Fabrication of biodegradable spheroidal microparticles for drug delivery applications

J Control Release. 2009 Sep 15;138(3):235-42. doi: 10.1016/j.jconrel.2009.05.020. Epub 2009 May 22.

Abstract

Particle shape, in addition to size, is becoming increasingly recognized as important in the design of drug carriers for in vivo use. However, few methods exist for fabricating non-spherical particles from biodegradable polymers. This work describes for the first time the fabrication of biodegradable spheroidal microparticles using the simple oil-in-water emulsion solvent evaporation technique (O/W ESE). Unloaded and paclitaxel-loaded spheroids were fabricated from poly(lactic-co-glycolic acid) (PLGA), and the shape and size of fabricated spheroids were manipulated by controlling fabrication process parameters including stir speed, aqueous and oil phase viscosity, aqueous phase pH, and the polymer molecular weight and end group. The presented data show that high aqueous phase viscosity, basic aqueous phase pH and hydrophilic polymer side chains and end groups are all conditions that favor the formation of spheroidal particles. The described technique is advantageous over methods currently described in the literature in its simplicity in setup, high particle yield and adaptability to a wide range of biodegradable polymers and therapeutics.

Publication types

  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Antineoplastic Agents, Phytogenic / administration & dosage
  • Drug Delivery Systems / methods*
  • Emulsions / chemistry
  • Glycolates / chemistry*
  • Hydrogen-Ion Concentration
  • Lactic Acid
  • Paclitaxel / administration & dosage
  • Particle Size
  • Polyglycolic Acid
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyvinyl Alcohol / chemistry*
  • Surface Properties
  • Viscosity

Substances

  • Antineoplastic Agents, Phytogenic
  • Emulsions
  • Glycolates
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polyglycolic Acid
  • Lactic Acid
  • Polyvinyl Alcohol
  • Paclitaxel