Solid Dispersion of Kaempferol: Formulation Development, Characterization, and Oral Bioavailability Assessment.

Area of Science:

• Pharmacology and Pharmaceutics
• Drug Delivery Systems
• Natural Product Chemistry

Background:

• Kaempferol (KPF), a flavonoid, exhibits antioxidant, anti-inflammatory, and anticancer properties.
• Poor water solubility and oral bioavailability limit KPF's therapeutic potential.
• Novel drug delivery systems are needed to improve KPF's efficacy.

Purpose of the Study:

• To enhance the water solubility, dissolution rate, and pharmacokinetic properties of Kaempferol (KPF).
• To develop and characterize solid dispersions (SDs) of KPF using Poloxamer 407.
• To evaluate the in vivo performance of KPF-loaded SDs.

Main Methods:

• Solid dispersions (SDs) of KPF were prepared using solvent and melting methods with Poloxamer 407 at a 1:5 KPF:carrier ratio.
• Formulations were characterized using FTIR, XRD, DSC, and SEM.
• In vitro dissolution studies and in vivo pharmacokinetic studies in rats were conducted.

Main Results:

• KPF-loaded SDs exhibited a ~4000-fold increase in water solubility compared to free KPF.
• SDs significantly enhanced KPF dissolution rate and extent (approx. 100% in 120 min).
• Oral administration of KPF SDs in rats resulted in a twofold increase in AUC and Cmax compared to free KPF.

Conclusions:

• Solid dispersion with Poloxamer 407 is an effective strategy to improve KPF's dissolution and oral bioavailability.
• This approach offers a promising avenue for enhancing the therapeutic utility of Kaempferol.
• Further research into KPF solid dispersions could lead to improved pharmaceutical formulations.