Bioavailability Enhancement of Curcumin by PEG-Based Gastroretentive System: Development and In Vitro Evaluation

Area of Science:

• Pharmaceutical Technology
• Drug Delivery Systems
• Biopharmaceutics

Background:

• Poor bioavailability of BCS class IV drugs (poor solubility and permeability) presents a significant challenge.
• Active pharmaceutical ingredients in BCS class IV often face rapid efflux and metabolism.
• Enhancing drug absorption and overcoming these barriers is crucial for effective therapeutics.

Purpose of the Study:

• To improve the bioavailability of poorly absorbed drugs, specifically BCS class IV compounds.
• To formulate a gastroretentive self-emulsifying system using curcumin as a model drug.
• To develop an extended-release formulation with enhanced gastric retention.

Main Methods:

• Formulation of self-emulsifying systems incorporating emulsifying agents, dissolution retardants, and PEGs.
• Characterization of aqueous dispersions using dynamic light scattering and viscosity measurements.
• Assessment of gastroretention via melt foaming, microCT, PXRD, DSC, cytotoxicity assays, and transcellular transport studies.

Main Results:

• Development of a homogeneous, gastric-floating, self-emulsifying system.
• Demonstrated an advantageous cytotoxic profile in Caco-2 cells.
• Achieved increased bioavailability and extended drug release.

Conclusions:

• Successfully created a self-emulsifying gastroretentive formulation for enhanced drug bioavailability.
• The formulation exhibits effective gastric retention and extended release properties.
• Utilized a minimal amount of cost-efficient excipients for formulation development.