Targeted Liposome Garcinol Formulation for the Treatment of Colon Cancer: Pharmacological and Toxicological Evaluation

Garcinol is a secondary metabolite commonly found in Garcinia plant species that exhibits potential anticancer properties but faces challenges in delivery due to its insolubility in aqueous solutions, rapid elimination from the body, and poor bioavailability. To overcome these limitations, a targeted liposomal garcinol (TLG) formulation was developed by using the VRPMPLQ-NC16 peptide to target colon tumors. The TLG formulation demonstrated an encapsulation efficiency of 77.29% and a size of 134.4 nm. <i>In vitro</i> anticancer studies revealed the ability of the TLG formulation to induce cell cycle arrest in the G/M phase and increase reactive oxygen species in cancer cells. In a murine colon carcinoma model, the TLG formulation effectively targeted tumors, activated cell death pathways, and inhibited metastasis. The pharmacokinetic analysis revealed the sustained release of garcinol from the TLG formulation with a peak concentration (<i>C</i>_max) of 912.1 ng/mL at 2-3 h and a half-life (<i>t</i>_1/2) of 36.61 h, compared to garcinol <i>C</i>_max of 1230.06 ng/mL at 0.5 h and <i>t</i>_1/2 of 4.23 h. Furthermore, genotoxicity studies showed that TLG proved to be protective, indicating its potential as a more effective and safer colon cancer treatment.