Development and evaluation of artemether parenteral microemulsion

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Malariology

Background:

• Artemether is a crucial hydrophobic antimalarial drug.
• Effective parenteral delivery of hydrophobic drugs like artemether presents challenges.
• Marketed artemether formulations may have limitations in efficacy or stability.

Purpose of the Study:

• To develop a stable parenteral microemulsion for artemether delivery.
• To evaluate the physicochemical properties and stability of the artemether microemulsion.
• To compare the in vivo antimalarial efficacy of the developed microemulsion against a marketed formulation.

Main Methods:

• Development and characterization of a parenteral artemether microemulsion.
• Assessment of microemulsion parameters: globule size, centrifugation, freeze-thaw cycling, and sterilization effects.
• In vivo evaluation of antimalarial activity in Plasmodium berghei infected mice.
• Stability assessment of the microemulsion at 5°C for one month.

Main Results:

• The developed microemulsion exhibited a globule size of 113 nm and demonstrated excellent stability against centrifugation and freeze-thaw cycles.
• Sterilization methods did not significantly impact artemether content or globule size.
• The artemether microemulsion showed approximately 1.5-fold higher antimalarial activity and improved survival rates compared to the marketed artemether injection (Larither®).
• The microemulsion maintained good stability over a one-month period.

Conclusions:

• Parenteral artemether microemulsion is a viable and effective drug delivery system.
• The developed microemulsion offers enhanced antimalarial efficacy and stability over conventional artemether injections.
• This formulation holds promise for improved malaria treatment.