[New antimalarial sustained-release formulations based on bioresorbable polymers: therapeutic evaluation using the...

Area of Science:

• Pharmaceutical Sciences
• Biomaterials Science
• Infectious Disease Research

Context:

• Chemotherapy is crucial for malaria control.
• Need for long-acting antimalarial formulations to improve patient compliance and avoid high drug concentrations.
• Existing treatments often require frequent administration, posing compliance challenges.

Purpose:

• To evaluate the therapeutic efficacy of implantable bioresorbable reservoir-forms for long-term malaria treatment.
• To assess pyrimethamine-loaded microspheres and rods as potential drug delivery systems.
• To determine the suitability of different polymers (polycaprolactone, polylactide) for sustained drug release.

Summary:

• Implantable subdermic rods made of polycaprolactone and polylactide (PLA 50 and PLA 100) loaded with pyrimethamine demonstrated long-term efficacy.
• Microspheres of polycaprolactone and polylactide 100 were unsuitable for sustained malaria treatment.
• Rods containing 19-40% pyrimethamine provided protection for at least three months in a Plasmodium berghei mouse model.

Impact:

• Successful development of long-acting malaria treatment formulations.
• Potential to significantly improve patient compliance in malaria control programs.
• Reduced risk of adverse effects associated with high plasmatic peaks from conventional drug administration.