| Summary: | Targeted drug delivery to tumor cells may be possible using nanoparticles containing human therapeutic drugs. The present study was carried out to develop cisplatin (CP) and 5-fluorouracil (FA) encapsulated chitosan nanoparticles (CSNPs), crosslinked with sodium tripolyphosphate (TPP) by an ionic gelation method and in vitro release, promoting antibacterial and anticancer activities. The prepared CSNPs, before and after CP and FA encapsulation, have been studied using various characterization techniques such as FTIR, XRD, SEM, and TEM-SAED patterning. The composites were well-dispersed, with an average particle size diameter of about 395.3 ± 14.3 nm, 126.7 ± 2.6 nm, and 82.5 ± 2.3 nm, respectively. In vitro release studies indicated a controlled and sustained release of CP and FA from the CSNPs, with the release amounts of 72.9 ± 3.6% and 94.8 ± 2.9%. The antimicrobial activity of the CSNPs-FA (91.37 ± 4.37% and 89.28 ± 3.19%) showed a significantly better effect against <i>E. coli</i> and <i>S. aureus</i> than that shown by the CSNPs-CP (63.41 ± 3.84% and 57.62 ± 4.28%). The HCT-116 cell lines were selected for in vitro cell cytotoxicity and live/dead assay to evaluate the preliminary anticancer efficacy of the CSNPs-CP and CSNPs-FA towards successfully inhibiting the growth of cancer cells.
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