Atovaquone-loaded nanocapsules: influence of the nature of the polymer on their in vitro characteristics.
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.
Cauchetier
Emmanuelle
E
Laboratoire de Pharmacotechnie, Service Pharmacie, C.H.U. Henri Mondor, 94010 Créteil, France. ecauchetier@ch-argenteuil.fr
Deniau
M
M
Fessi
H
H
Astier
A
A
Paul
M
M
D000981:Antiprotozoal Agents / Q000008:administration & dosage*; D053626:Atovaquone; D016503:Drug Delivery Systems; D004355:Drug Stability; D006863:Hydrogen-Ion Concentration; D019344:Lactic Acid / Q000008:administration & dosage*; D009285:Naphthoquinones / Q000008:administration & dosage* / Q000737:chemistry; D010316:Particle Size; D011091:Polyesters / Q000008:administration & dosage*; D011100:Polyglycolic Acid / Q000008:administration & dosage*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011108:Polymers / Q000008:administration & dosage*
D000981:Antiprotozoal Agents; D009285:Naphthoquinones; D011091:Polyesters; D011108:Polymers; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; C016240:polycaprolactone; D011100:Polyglycolic Acid; D019344:Lactic Acid; C033616:poly(lactide); D053626:Atovaquone