Dual-drug-loaded lipid-based formulation for colon cancer therapeutics: in vitro optimization and characterization.

OBJECTIVE

The current investigation aims to fabricate, optimize and characterize dual-drug-loaded liposomes for the management of colon cancer.

SIGNIFICANCE: Lipid-based nanocarriers are versatile nanocarriers that facilitate the loading of both hydrophilic and hydrophobic therapeutic agents. The simultaneous delivery of capecitabine (CAP) and celecoxib (CEL) is anticipated to enhance anticancer efficacy against colon cancer.

METHODS

CAP-CEL-loaded liposomes (CAP-CEL-LIPs) were designed and optimized utilizing Box-Behnken Design (BBD). The optimized LIPs were characterized for particle size, polydispersity index (PDI), entrapment efficiency and morphological studies. In vitro drug release studies were conducted under both acidic and physiological conditions. Hemocompatibility was evaluated using the hemolysis assay and the stability of the LIPs was assessed over a duration of one month.

RESULTS

The optimized CAP-CEL-LIPs demonstrated a mean particle size of 130 ± 2.36 nm with a PDI of 0.162 ± 0.008, showing the homogeneous particle size distribution. The encapsulation efficiency for CAP and CEL was found to be 64.96 ± 2.81% and 92.23 ± 2.22%, respectively. SEM and TEM images revealed the spherical morphology of the developed LIPs. In vitro drug release investigations revealed a controlled release profile for both drugs under both acidic and physiological conditions. The hemolysis assay showed hemolysis rate of less than 2%, thereby confirming superior blood compatibility. Stability data indicated that LIPs remained stable for one-month. The developed CAP-CEL-LIPs showed significant cytotoxic potential with enhanced cellular uptake and apoptotic activity against colon cancer cells.

CONCLUSION

The engineered CAP-CEL-LIPs could be a promising platform for managing colon cancer.