Solubility enhancement of lovastatin by modified locust bean gum using solid dispersion techniques

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Pharmacology

Background:

• Poor water solubility of drugs like lovastatin (LS) limits their bioavailability and therapeutic efficacy.
• Solid dispersion (SD) technology offers a promising approach to enhance the solubility of poorly soluble compounds.
• Locust bean gum (LBG) is a natural polymer with potential as a carrier in pharmaceutical formulations.

Purpose of the Study:

• To improve the solubility and dissolution rate of lovastatin (LS) using modified locust bean gum (MLBG) as a carrier via solid dispersion (SD) techniques.
• To evaluate the effect of MLBG concentration and preparation methods on LS solubility and dissolution.
• To characterize the prepared SDs and assess the in vivo efficacy of LS-loaded SDs.

Main Methods:

• Locust bean gum (LBG) was modified by heating, resulting in reduced viscosity while maintaining swelling properties.
• Solid dispersions (SDs) of lovastatin (LS) were prepared using MLBG with varying concentrations and different preparation techniques.
• Solubility, dissolution studies, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), X-ray diffraction (XRD), and in vivo HMG-CoA reductase inhibition assays were performed.

Main Results:

• Solubility of LS increased with increasing concentrations of MLBG in the solid dispersions.
• The modified solvent evaporation method proved to be the most effective for preparing LS SDs, yielding superior solubility enhancement.
• In vivo studies demonstrated a significant reduction in HMG-CoA reductase activity for LS-loaded SDs compared to plain LS, indicating enhanced bioavailability.

Conclusions:

• Modified locust bean gum (MLBG) is a suitable and effective carrier for enhancing the solubility, dissolution rate, and bioavailability of poorly water-soluble drugs like lovastatin (LS).
• The preparation method significantly influences the performance of LS solid dispersions.
• MLBG-modified solid dispersions represent a promising strategy for improving the therapeutic potential of lovastatin.