Retinoic acid core-shell lipoplexes for the treatment of colorectal cancer

Abstract

The use of retinoic acid restricts the application in cancer using oral and intravenous drug delivery systems due to rapid decrease in plasma concentration. Moreover, low aqueous solubility and topical irritation limits the usage of retinoic acid in clinical studies. DNA, a non-viral vector stimulates the immune system against the cancerous cell by inhibiting the growth of tumour cell. The aim of the present research work was to formulate lipid-complexed with DNA using cationic lipid in the form of lipoplexes of retinoic acid on colorectal cancer cell lines. Lipoplexes are lipid-based systems with DNA attached to the cationic branch of the liposomes for easy and faster penetration inside the cell. Lipoplexes were prepared by film-hydration method and followed by complexation with DNA in presence of retinoic acid. The lipoplexes were characterized by surface morphology, surface charge, % drug encapsulation, in-vitro release profile and stability studies. Particle size of the lipoplexes of retinoic acid was found to be in the range of 306.12 ± 1.23–526.4 ± 4.25 nm. The smaller particle size and higher zeta potential indicated better stability of the formulations due to the development of more surface resistance for aggregation. The encapsulation efficiency was found to be 79.46 ± 2.12 % due to the complex formation of lipophilic retinoic acid and the lipid nature of liposomes. The in-vitro release study of retinoic acid from lipoplex network was found to be 78.56 ± 2.58 % with the first-order controlled release pattern for 24 h. Therefore, lipoplex formulation showed a novel approach for the delivery of retinoic acid in colorectal cancer for site-specific action.