Thiolated pectin-doxorubicin conjugates: Synthesis, characterization and anticancer activity studies

Area of Science:

• Biomaterials Science
• Drug Delivery Systems
• Cancer Therapeutics

Background:

• Pectin, a natural polysaccharide, is being explored for drug delivery applications.
• Thiolation of pectin enhances its conjugation capabilities for drug attachment.
• Doxorubicin (DOX) is a widely used chemotherapy agent with limitations in targeted delivery.

Purpose of the Study:

• To synthesize and characterize thiolated pectin-doxorubicin (DOX) conjugates.
• To evaluate the efficiency of different conjugation methods for creating these drug conjugates.
• To assess the in vitro anticancer efficacy of the synthesized conjugates against various cancer cell lines.

Main Methods:

• Pectin cross-linking with thioglycolic acid or cystamine dihydrochloride to form thiolated pectins.
• Coupling of thiolated pectins with a DOX derivative using disulfide bond formation and disulfide bond exchange methods.
• Characterization of physicochemical properties and morphology of the conjugates.
• In vitro evaluation of anticancer activity against mouse colon carcinoma, human bone osteosarcoma, and human prostate cancer cells.

Main Results:

• The disulfide bond exchange method proved to be a more efficient synthesis route for thiolated pectin-DOX conjugates.
• DOX content was higher in conjugates synthesized using low methoxy pectin compared to high methoxy pectin.
• Thiolated pectin-DOX conjugates exhibited significantly enhanced in vitro anticancer activity against mouse colon carcinoma and human bone osteosarcoma cells compared to free DOX.

Conclusions:

• Thiolated pectin-DOX conjugates can be efficiently synthesized via disulfide bond exchange.
• The conjugates demonstrate promising in vitro anticancer efficacy, suggesting potential for targeted drug delivery.
• These novel conjugates show potential as a drug platform for colorectal cancer-targeted delivery of DOX.