Nanoencapsulation of Aptamer-Functionalized 5-Fluorouracil Liposomes Using Alginate/Chitosan Complex As a Novel Targeting Strategy for Colon-Specific Drug Delivery Publisher



Khodarahmi M^{1, 2} ; Abbasi H^{1, 2} ; Kouchak M^{1, 3} ; Mahdavinia M^{4, 5} ; Handali S⁶ ; Rahbar N^{1, 2} Show Affiliations
Source: Journal of Drug Delivery Science and Technology Published:2022

Abstract

Two important challenges in clinical application of 5-Fluorouracil (5-FU) in the treatment of colon cancer are preventing the release or degradation of the drug in the stomach/small intestine, and its delivering the colon as the site of action. The preparation of targeted liposomes using a suitable ligand and their encapsulation may be a promising method for the targeted treatment of colon cancer. The targeted liposomes were prepared by the optimized thin film method, and anti-nucleolin aptamer (AS1411) was used as the ligand. The nanocapsules were then prepared by coating of the synthesized liposomes with alginate and chitosan solution. The chemical structure, particle size and morphology of the liposomes and the nanocapsules were examined by Fourier transform infrared spectroscopy (FT-IR), dynamic light scattering (DLS), zeta potentiometer and field emission scanning electron microscopy (FESEM). MTT cytotoxicity studies were performed in vitro on the colon cancer cell line (HT-29). The liposomes and nanocapsules prepared were spherical with approximate sizes of 120 and 170 nm, respectively. The cytotoxicity studies on HT-29 cells showed that aptamer-conjugated liposomes induced significantly more cell death than aptamer-free liposomes and free drug. The results of the drug release experiments under simulated conditions including stomach, small intestine, and colon showed the excellent efficiency of the nanocapsules in releasing their cargo only under colonic condition. © 2022