Thymoquinone Pectin Beads Produced via Electrospray: Enhancing Oral Targeted Delivery for Colorectal Cancer Therapy

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Oncology

Background:

• Thymoquinone (TQ) has potent anticancer properties but suffers from poor solubility and bioavailability.
• Developing effective oral delivery systems is crucial to enhance TQ's therapeutic efficacy for colon cancer.

Purpose of the Study:

• To develop and optimize an oral drug delivery system for thymoquinone (TQ) using pectin beads (TQ-PBs).
• To investigate the controlled release of TQ from TQ-PBs and its targeted delivery to the colon.
• To evaluate the anticancer efficacy of TQ-PBs against colon cancer cells.

Main Methods:

• Thymoquinone pectin beads (TQ-PBs) were synthesized using an adjustable electrospray technique combined with ionic gelation.
• Beads were characterized for size, sphericity, encapsulation efficiency, water uptake, erosion, and surface morphology.
• In vitro release studies in simulated gastric, intestinal, and colonic fluids were performed.
• Cytotoxicity of TQ-PBs against HT-29 colon cancer cells was evaluated.

Main Results:

• Optimized TQ-PBs exhibited favorable characteristics: 2.05 mm size, 0.96 sphericity, and 90.32% encapsulation efficiency.
• Controlled TQ release was observed, with minimal release in simulated gastric fluid and accelerated release in simulated colonic fluid.
• TQ-PBs demonstrated significant cytotoxicity against HT-29 cells with an IC50 of 80.59 μg/mL.

Conclusions:

• Adjustable electrospray technique enables precise control over TQ-PBs for targeted colon cancer delivery.
• TQ-PBs show potential as an effective oral drug delivery system for colorectal cancer therapy.
• The developed system enhances TQ bioavailability and anticancer activity, addressing limitations of conventional TQ formulations.