Atovaquone-loaded nanocapsules: influence of the nature of the polymer on their in vitro characteristics

Int J Pharm. 2003 Jan 2;250(1):273-81. doi: 10.1016/s0378-5173(02)00556-2.

Abstract

Nanocapsules with atovaquone concentration of 1,000 micrograms/ml were prepared according to the interfacial deposition technique using different polymers: poly- epsilon -caprolactone (PECL), poly(lactic acid) (PLA) and poly(lactic-co-glycolic acid) (PLAGA). The following characteristics of nanoparticles were determined: percentage of encapsulation of atovaquone, percentage of encapsulation of benzyl benzoate (BB), nanoparticle size, nanoparticle wall thickness, suspension pH, and in vitro stability. The different formulations showed similar characteristics: maximal percentage of encapsulation (100%), particle size of approximately 230 nm, neutral pH and wall thickness of approximately 20 nm. The type of polymer used was the main factor influencing stability, in decreasing order: PECL>PLA>PLAGA. No release of atovaquone or benzylbenzoate was noted with PECL nanoparticles over 4 months. Release of atovaquone (25.9%) was found with PLA nanoparticles at 4 months. Release of both atovaquone (18.9%) and benzylbenzoate (54.2%) was noted with PLAGA nanoparticles from the third month, indicating a disruption of the nanoparticle membrane.

MeSH terms

  • Antiprotozoal Agents / administration & dosage*
  • Atovaquone
  • Drug Delivery Systems*
  • Drug Stability
  • Hydrogen-Ion Concentration
  • Lactic Acid / administration & dosage*
  • Naphthoquinones / administration & dosage*
  • Naphthoquinones / chemistry
  • Particle Size
  • Polyesters / administration & dosage*
  • Polyglycolic Acid / administration & dosage*
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • Polymers / administration & dosage*

Substances

  • Antiprotozoal Agents
  • Naphthoquinones
  • Polyesters
  • Polymers
  • Polylactic Acid-Polyglycolic Acid Copolymer
  • polycaprolactone
  • Polyglycolic Acid
  • Lactic Acid
  • poly(lactide)
  • Atovaquone