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Abstract

Objective: The Failure in chemotherapy is mainly because of the resistance of the chemotherapeutic drugs towards the neoplastic cells. The main reason behind this study was to develop a novel combination of 5-Fluorouracil (5-FU) lipid curcumin conjugates for the treatment of cancer. Methods: In this study, the lipid group stearic acid and oleic acid was conjugated with the parent drug moiety 5-Fluorouracil to acquire lipophilicity. The next step involves the conjugation of curcumin with 5-Fluorouracil lipid to form a lipid dual drug conjugate. The characterization of conjugates followed the synthesis part by using FT-IR, DSC, and LCMS. The conjugates hence obtained were further carried for formulation aspect. After the successful completion of the formulation part, in-vitro studies and MTT Assay was performed. Results: The results depict the successful synthesis of the conjugates, and its characterization was successfully done. The conjugates are formulated into Self Nanomulsifying drug delivery system (SNEDDS). The results obtained from the MTT assay also shown a significant cytotoxic effect in both the conjugation. Conclusion: The in-vitro results suggest further studies for cleavage of the drug and the lipids in the conjugate and in-vivo animal studies to demonstrate the anticancer efficacy.

Multidrug Resistance of Cancer Cells and the Vital Role of P-Glycoprotein

“…Verapamil, a calcium channel antagonist utilized as a racemic combination in the nanomolar concentration range for the treatment of cardiovascular disorders, is one of the most investigated first-generation inhibitors. Although second-, third-, and fourth-generation inhibitors that were less harmful and more effective were created, the notion was never tested in clinical settings (see Section 5) [16]. P-gp is considered a major MDR transporter with respect to its resistance to cancer chemotherapy [15].…”