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5-Fluorouracil-Loaded Folic-Acid-Fabricated Chitosan Nanoparticles for Site-Targeted Drug Delivery Cargo

Ullah, Shafi, Azad, Abul Kalam, Nawaz, Asif, Shah, Kifayat Ullah, Iqbal, Muhammad, Albadrani, Ghadeer M., Al-Joufi, Fakhria A., Sayed, Amany A., Abdel-Daim, Mohamed M.·2022·Polymers
DOI 10.3390/polym14102010PMC PMC9145180
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Abstract

Nanoparticles play a vital role in cancer treatment to deliver or direct the drug to the malignant cell, avoiding the attacking of normal cells. The aim of the study is to formulate folic-acid-modified chitosan nanoparticles for colon cancer. Chitosan was successfully conjugated with folic acid to produce a folic acid–chitosan conjugate. The folate-modified chitosan was loaded with 5-FU using the ionic gelation method. The prepared nanoparticles were characterized for size, zeta potential, surface morphology, drug contents, entrapment efficiency, loading efficiency, and in vitro release study. The cytotoxicity study of the formulated nanoparticles was also investigated. The conjugation of folic acid with chitosan was confirmed by FTIR and NMR spectroscopy. The obtained nanoparticles were monodispersed nanoparticles with a suitable average size and a positive surface charge. The size and zeta potential and PDI of the CS-5FU-NPs were 208 ± 15, 26 ± 2, and +20 ± 2, respectively, and those of the FA-CS-5FU-NPs were 235 ± 12 and +20 ± 2, respectively, which are in the acceptable ranges. The drug contents’ % yield and the %EE of folate-decorated NPs were 53 ± 1.8% and 59 ± 2%, respectively. The in vitro release of the FA-CS-5FU-NPs and CS-5FU-NPs was in the range of 10.08 ± 0.45 to 96.57 ± 0.09% and 6 ± 0.31 to 91.44 ± 0.21, respectively. The cytotoxicity of the nanoparticles was enhanced in the presence of folic acid. The presence of folic acid in nanoparticles shows much higher cytotoxicity as compared to simple chitosan nanoparticles. The folate-modified nanoparticles provide a potential way to enhance the targeting of tumor cells.

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Crossref · 10.3390/polym14102010

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Figure 1 A scheme illustrating the reaction of chitosan with folic acid.
Figure 1 A scheme illustrating the reaction of chitosan with folic acid.CC BY · PubMed Central
Figure 2 FTIR spectra of (a) pure chitosan, (b) pure FA, and (c) FA–CS conjugate.
Figure 2 FTIR spectra of (a) pure chitosan, (b) pure FA, and (c) FA–CS conjugate.CC BY · PubMed Central
Figure 3 1H-NMR spectra of (A) pure chitosan, (B) pure FA, and (C) FA–CS conjugate.
Figure 3 1H-NMR spectra of (A) pure chitosan, (B) pure FA, and (C) FA–CS conjugate.CC BY · PubMed Central
Figure 4 (A) Size distribution of nanoparticles, (B) surface morphology of folic-acid-modified 5-FU-loaded chitosan NPs.
Figure 4 (A) Size distribution of nanoparticles, (B) surface morphology of folic-acid-modified 5-FU-loaded chitosan NPs.CC BY · PubMed Central
Figure 5 In vitro release study of pure 5-FU, CS-5FU-NPs, and FA-CS-5FU-NPs.
Figure 5 In vitro release study of pure 5-FU, CS-5FU-NPs, and FA-CS-5FU-NPs.CC BY · PubMed Central
Figure 6 Cytotoxicity study shows the % cell death of 5-FU, CS-5-FU-NPs, and FA-CS-5-FU-NPs.
Figure 6 Cytotoxicity study shows the % cell death of 5-FU, CS-5-FU-NPs, and FA-CS-5-FU-NPs.CC BY · PubMed Central

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Research works printed but not linked: 32

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Metadata

Authors
Ullah, S., Azad, A. K., Nawaz, A., Shah, K. U., Iqbal, M., Albadrani, G. M., Al-Joufi, F. A., Sayed, A. A., & Abdel-Daim, M. M.
Venue
Polymers
Publisher
MDPI AG
Published
2022-05-13
Volume
14
Issue
10
Pages
2010
ISSN
2073-4360
DOI
10.3390/polym14102010
PMC
PMC9145180
Cited by
94
References
0
Language
en
Licence
creativecommons.org/licenses/by/4.0/ (vor)
Funders
  • Princess Nourah bint Abdulrahman University Researchers Supporting Project (PNURSP2022R30)
  • Faculty of Pharmacy, AIMST University, Kedah, Malaysia (PNURSP2022R30)

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