Formulation and Evaluation of Relugolix-Loaded Nanocochleates for Targeted Cancer Treatment

Abstract

This study presents the formulation and evaluation of Relugolix-loaded nanocochleates as a targeted drug delivery system for cancer treatment. Relugolix, a BCS Class IV anticancer drug, was characterized for its physicochemical properties and solubility, demonstrating optimal solubility in ethanol. Utilizing the thin film hydration method, liposomes were developed and subsequently optimized. The optimized formulation exhibited a drug content of 97.56% and an entrapment efficiency of 95.78%. In vitro diffusion studies revealed a sustained release profile, with 96.87% of the drug released over 12 hours, indicating effective drug retention. The incorporation of nanocochleates further improved stability and drug delivery, with characterization techniques such as X-ray diffraction (XRD) and differential scanning calorimetry (DSC) confirming the crystalline nature of the formulation. Cytotoxicity assays conducted on PC-3 cancer cell lines demonstrated significant growth inhibition, highlighting the therapeutic potential of the Relugolix-loaded nanocochleate system. Stability studies confirmed minimal changes in drug content and entrapment efficiency over time, suggesting a robust formulation suitable for therapeutic applications. This research underscores the promise of nanocochleates in enhancing the efficacy of Relugolix for targeted cancer therapy, necessitating further investigation in vivo.