Curcumin-loaded hydroxypropyl-β-cyclodextrin inclusion complex with enhanced dissolution and oral bioavailability for...

Area of Science:

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

Background:

• Curcumin, a turmeric extract, shows promise for neurological disorders but suffers from poor bioavailability.
• Low solubility, light/heat sensitivity, and poor absorption limit curcumin's clinical use, especially for epilepsy treatment.
• Existing limitations hinder the full therapeutic potential of curcumin in central nervous system diseases.

Purpose of the Study:

• To develop a curcumin hydroxypropyl-β-cyclodextrin inclusion complex (CUR-HP-β-CD) to enhance curcumin's bioavailability.
• To improve brain distribution and therapeutic efficacy of curcumin for potential epilepsy treatment.
• To establish a reproducible method for creating an enhanced curcumin formulation.

Main Methods:

• Curcumin hydroxypropyl-β-cyclodextrin inclusion complex (CUR-HP-β-CD) was synthesized using the solvent evaporation method.
• Solubility studies were conducted in water, HCl (pH 1.2), and PBS (pH 6.8).
• In vivo efficacy was evaluated using pentylenetetrazol (PTZ)-induced zebrafish and mouse models of epilepsy.

Main Results:

• CUR-HP-β-CD exhibited significantly increased solubility (63.5x in H2O, 60.1x in pH 1.2 HCl, 52.9x in pH 6.8 PBS) compared to curcumin.
• Bioavailability was improved 2.8-fold, with brain concentrations increasing by 38.7-fold.
• CUR-HP-β-CD demonstrated superior therapeutic effects in PTZ-induced epilepsy models.

Conclusions:

• The developed CUR-HP-β-CD effectively enhances curcumin's bioavailability and brain delivery.
• This formulation shows significant potential for improved epilepsy treatment.
• The study presents a viable strategy for overcoming curcumin's limitations in clinical applications.