Slow-release melarsoprol microparticles.
The present study compares two methods of preparation of microparticles of melarsoprol for the treatment of the human trypanosomiasis. Melarsoprol is poorly soluble in water and in organic media. Microparticles were formulated with modified O/W and W/O/W methods, Poly(epsilon -caprolactone) microparticles were prepared either with a suspension-in-oil-in-water (S/O/W) solvent evaporation method or by complexation of melarsoprol with methyl ss-cyclodextrin followed by a water-in-oil-in-water (W(CD)/O/W) solvent evaporation method. Results showed a poor incorporation of melarsoprol (2.89 +/- 0.20 microg mg(-1)) using the W(CD)/O/W process, while the S/O/W process allowed achieving 161 +/- 5 microg mg(-1) and seemed to be very effective for the preparation of a sustained release form of melarsoprol. Moreover S/O/W microparticles showed a slow release of the drug in 70% of phosphate buffer pH 7.4, 0.1 M and 30% of propylene glycol (about 50% in 2 h and 80% after 7 h).
Gibaud
Stéphane
S
Laboratoire de Pharmacie Clinique, UPRES EA 3452, Faculté de Pharmacie, 5, rue Albert Lebrun, 54000 Nancy, France. stephanie.gibaud@pharma.uhp-nancy.fr
Gaia
Adela
A
Astier
Alain
A
D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004339:Drug Compounding; D004655:Emulsions; D008549:Melarsoprol / Q000737:chemistry*; D010316:Particle Size; D014344:Trypanocidal Agents / Q000737:chemistry*; D014961:X-Ray Diffraction
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004655:Emulsions; D014344:Trypanocidal Agents; D008549:Melarsoprol