Slow-release melarsoprol microparticles

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Medicinal Chemistry

Background:

• Melarsoprol is a crucial drug for treating human African trypanosomiasis.
• Melarsoprol exhibits poor solubility in both aqueous and organic solvents, complicating formulation.
• Effective microparticle formulation is needed to improve melarsoprol delivery and efficacy.

Purpose of the Study:

• To compare two distinct methods for preparing Poly(epsilon -caprolactone) microparticles loaded with melarsoprol.
• To evaluate the drug incorporation efficiency and release kinetics of the formulated melarsoprol microparticles.
• To identify an optimal method for developing sustained-release melarsoprol formulations.

Main Methods:

• Formulation of melarsoprol microparticles using modified oil-in-water (O/W) and water-in-oil-in-water (W/O/W) solvent evaporation techniques.
• Comparison of a suspension-in-oil-in-water (S/O/W) method with a water-in-oil-in-water method involving methyl beta-cyclodextrin complexation (W(CD)/O/W).
• Assessment of melarsoprol incorporation and in vitro drug release in a phosphate buffer/propylene glycol mixture.

Main Results:

• The W(CD)/O/W method resulted in poor melarsoprol incorporation (2.89 +/- 0.20 microg mg(-1)).
• The S/O/W method achieved significantly higher melarsoprol incorporation (161 +/- 5 microg mg(-1)).
• S/O/W microparticles demonstrated sustained drug release, with approximately 50% released in 2 hours and 80% after 7 hours.

Conclusions:

• The S/O/W solvent evaporation method is highly effective for preparing melarsoprol microparticles.
• This S/O/W method facilitates the development of sustained-release formulations for melarsoprol.
• The findings suggest a promising approach for improving melarsoprol delivery in trypanosomiasis treatment.