The use of chitosan-coated flexible liposomes as a remarkable carrier to enhance the antitumor efficacy of 5-fluorouracil against colorectal cancer

Abstract

Surface-coated nanocarriers have been extensively used to enhance the delivery of anticancer drugs and improve their therapeutic index. In this study, chitosan (CS)-coated flexible liposomes (chitosomes) containing 5-fluorouracil (5-FU) were designed and characterized for use as a novel approach to target colon cancer cells. 5-FU-loaded flexible liposomes (F1, F2, and F3) and 5-FU-loaded chitosomes (F4, F5, and F6) were prepared using film hydration and electrostatic deposition techniques, respectively. The particle size, polydispersity index (PDI), zeta potential, entrapment efficiency (EE%), morphology, and in vitro drug release ability, and cytotoxicity of the formulations were determined. The results revealed that the size of chitosomes ranged from 212 to 271 nm with a positive surface charge of 6.1 to 14.7 mV, whereas the particle size of liposomes ranged from 108 to 234 nm with negative surface charges of −2.3 to −16.3. F3 and F6 had a spherical shape with a rough surface structure. The in vitro drug release study revealed that chitosomes retard 5-FU release as opposed to the 5-FU solution and liposomes. The cytotoxicity study using a colon cancer cell line (HT-29) showed that 5-FU-loaded chitosomes were more effective in killing cancer cells in a sustained manner than liposomes and the 5-FU solution. Chitosomes were therefore successfully developed as nanocarriers of 5-FU, with potential cytotoxicity for colorectal cancer cells.

Development of rosuvastatin flexible lipid-based nanoparticles: promising nanocarriers for improving intestinal cells cytotoxicity

“…The effect of the surfactant concentration on the particle size could be attributed to the reduction of the surface tension of the media at higher surfactant concentration and so arrangement of the phospholipid in small vesicles as previously reported [5]. The decrease in the EE of the prepared vesicles that was observed at higher surfactant concentration could be attributed to the formation of micelles molecules that compete for the drug molecules with the lipid vesicles.…”

“…The in vitro release of RSV from the prepared liposomal NPs, chitosomes nano-formulation and pure drug suspension was studied as previously reported [5]. A quantity of each preparation containing 9 mg of drug was placed in a firmly sealed dialysis bag (Sigma-Aldrich Inc.) of a molecular weight cut-off 14 kDa.…”

“…Moreover, NPs coated with chitosan have been reported in the literature to enhance stability and drug loading, controlling the drug release and maximizing the efficacy. Chitosan-coated poly (lactic-co-glycolic acid) NPs, magnetic NPs coated with chitosan, chitosan-coated cobalt ferrite NPs, chitosan-coated solid lipid NPs and chitosan-coated liposomes are common examples [5,8,14,17,21,24,42].…”

Glycol Chitosan-Docosahexaenoic Acid Liposomes for Drug Delivery: Synergistic Effect of Doxorubicin-Rapamycin in Drug-Resistant Breast Cancer

“…The PDI value for particles with a 20:1 ratio decreased from 0.213 to 0.159 compared with bare liposomes. These results can be explained by the electrostatic interaction between the liposomes, which have a strong negative surface charge, and glycol chitosan that has oppositely charged surface amine groups [21] (Figure 1). The size of the particles increased exponentially at a higher GC rate, which indicates that the degree of electrostatic interaction between the liposomes and GC must be well controlled to maintain the stability of the particles.…”

Lipid-Based Drug Delivery Nanoplatforms for Colorectal Cancer Therapy

“…The resulting alteration of the surface charge can be used to monitor the efficiency of chitosan coating. In an in vitro drug release assay, A. Alomrani et al [ 65 ] revealed that chitosan-coated liposomes could more effectively reduce 5-fluorouracil leakage than conventional liposomes, and chitosan coating increased the cytotoxicity of 5-fluorouracil toward CRC cells (HT-29) in a sustained manner. These discoveries suggest that LCLs are promising DDSs with the potency of increasing the stability, safety, and efficacy of the delivered drug.…”