Preparation and characterization of Simvastatin solid dispersion using skimmed milk

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems

Background:

• Simvastatin exhibits poor aqueous solubility, leading to low oral bioavailability (5%).
• This presents a significant challenge for developing effective oral dosage forms.

Purpose of the Study:

• To enhance the aqueous solubility and oral bioavailability of Simvastatin.
• To develop a novel solid dispersion formulation using skimmed milk as a carrier.

Main Methods:

• Solid dispersions of Simvastatin were prepared using lyophilization with skimmed milk.
• Formulations were characterized using differential scanning calorimetry, X-ray diffraction, and scanning electron microscopy.
• In vitro drug release and in vivo lipid-lowering potential were evaluated.

Main Results:

• The optimal Simvastatin:skimmed milk ratio (1:9) significantly increased solubility (approx. 30-fold) and in vitro drug release (86.69% vs. 25.19%).
• Solid dispersion converted crystalline Simvastatin to an amorphous form, confirmed by analytical studies.
• The reformulated drug demonstrated a 3-fold increase in lipid-lowering potential in a hyperlipidemia model.

Conclusions:

• Solid dispersion using skimmed milk is a promising strategy to improve Simvastatin's oral delivery.
• This approach effectively enhances solubility, dissolution, and therapeutic efficacy.