Curcumin-loaded soluplus® based ternary solid dispersions with enhanced solubility, dissolution and antibacterial,...

Area of Science:

• Pharmaceutical Sciences
• Materials Science

Background:

• Amorphous solid dispersions (ASDs) are crucial for improving drug solubility and bioavailability.
• Binary ASD systems often show limited long-term solubility, necessitating advanced formulations.

Purpose of the Study:

• To design and evaluate ternary amorphous solid dispersions (TSDs) of curcumin (CUR).
• To enhance curcumin's solubility, dissolution rate, and biological activities (anti-bacterial, antioxidant, anti-inflammatory).

Main Methods:

• Preparation of TSDs using Soluplus®, Syloid® XDP 3150, Syloid® 244, Poloxamer® 188, and HPMC E5 via solvent evaporation.
• Solubility and dissolution testing.
• Solid-state characterization using FTIR, SEM, DSC, and XRD.
• In vitro evaluation of anti-bacterial, antioxidant, and anti-inflammatory activities.

Main Results:

• The optimized ternary formulation (F3) containing 20% Soluplus® dramatically increased curcumin solubility (186 μg/ml) and dissolution (91%) by 3100 and 9-fold, respectively.
• Solid-state analyses confirmed the amorphous nature and enhanced properties of the TSDs.
• F3 demonstrated significant improvements in anti-bacterial activity against Gram-positive and Gram-negative bacteria, notably against Staphylococcus aureus (24 mm zone of inhibition).
• Antioxidant activity increased to 93% (vs. 69% for CUR), and anti-inflammatory activity showed 80% BSA inhibition (vs. 49% for CUR).

Conclusions:

• Ternary amorphous solid dispersions, particularly F3, represent a highly effective system for enhancing curcumin's solubility and dissolution.
• The developed TSDs exhibit superior anti-bacterial, antioxidant, and anti-inflammatory properties compared to pure curcumin.
• This formulation strategy holds promise for improving the delivery and efficacy of hydrophobic drugs like curcumin.