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. 2019 Jul;27(5):603-611.
doi: 10.1016/j.jsps.2019.02.008. Epub 2019 Mar 1.

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

Abdullah Alomrani  1   2 , Mohamed Badran  1   3 , Gamaleldin I Harisa  1   4   5 , Mohamed ALshehry  1 , Moayed Alhariri  6 , Aws Alshamsan  1   2 , Musaed Alkholief  1   2
Affiliations

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

Abdullah Alomrani et al. Saudi Pharm J. 2019 Jul.

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.

Keywords: 5-fluorouracil; Chitosomes; Colorectal cancer; Liposomes.

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Figures

Fig. 1
Fig. 1
Particle size and zeta potential of F3 and F6 (A), and images of F3, F6, and CSNPs (B).
Fig. 2
Fig. 2
Entrapment efficiency (EE%) and drug loading (DL%) of 5-FU-loaded liposomes, chitosomes, and CSNPs (Mean ± SD, n = 3).
Fig. 3
Fig. 3
Transmission electron microscopy micrographs of liposomes (F3) and chitosomes (F6).
Fig. 4
Fig. 4
Variation in particle size of 5-FU-loaded liposomes, chitosomes, and CSNPs during storage at 4 °C (Mean ± SD, n = 3).
Fig. 5
Fig. 5
In vitro release profile of 5-FU from 5-FU solution, 5-FU-loaded liposomes, chitosomes, and CSNPs in PBS (pH 7.4) at 37 ± 0.5 °C (Mean ± SD, n = 3).
Fig. 6
Fig. 6
Hemolysis test results obtained using the naked eye (6, negative control; 2, positive control; 3–9, test samples).
Fig. 7
Fig. 7
Cytotoxicity of 5-FU from 5-FU-loaded liposomes, chitosomes and CSNPs in the HT-29 cell line (Mean ± SD, n = 6).
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