Co-precipitates of lumefantrine-Eudragit E PO for dissolution improvement

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Lumefantrine exhibits poor solubility and variable bioavailability, limiting its therapeutic efficacy.
• Developing strategies to enhance lumefantrine's dissolution is crucial for improving its antimalarial activity.

Purpose of the Study:

• To prepare and evaluate a lumefantrine-Eudragit E PO co-precipitate.
• To improve the dissolution rate and solubility of lumefantrine through anti-solvent precipitation.

Main Methods:

• Co-precipitates of lumefantrine and Eudragit E PO were prepared using anti-solvent precipitation at various ratios.
• The optimized co-precipitate (1:0.5 ratio) underwent solid-state characterization (SEM, FTIR, DSC, XRPD) and dissolution testing.

Main Results:

• The lumefantrine-Eudragit E PO co-precipitate demonstrated a substantial increase in lumefantrine solubility.
• SEM revealed drug dispersion within the polymer matrix; FTIR showed no drug-polymer interaction.
• DSC and XRPD indicated the conversion of lumefantrine to an amorphous form, enhancing dissolution rates compared to the pure drug.

Conclusions:

• The lumefantrine-Eudragit E PO co-precipitate effectively improves lumefantrine dissolution.
• This formulation strategy holds potential for enhancing the bioavailability of poorly soluble drugs like lumefantrine.
• Further studies on the stabilization of these co-precipitates are warranted.