Abstract
The ionic gelation technique allows us to obtain nanoparticles able to function as carriers for hydrophobic anticancer drugs, such as 5-fluoruracil (5-FU). In this study, reticulated chitosan– docosahexaenoic acid (Chi–DHAr) nanoparticles were synthesized by using a chemical reaction between amine groups of chitosan (Chi) and carboxylic acids of docosahexaenoic acid (DHA) and the presence of a link between Chi and DHA was confirmed by FT-IR, while the size and morphology of the obtained Chi-DHAr nanoparticles was evaluated with dynamic light scattering (DLS) and scanning electron microscopy (SEM), respectively. Drug-loading content (DLC) and drug-loading efficiency (DLE) of 5-FU in Chi-DHAr nanoparticles were 33.74 ± 0.19% and 7.9 ± 0.26%, respectively, while in the non-functionalized nanoparticles (Chir + 5FU), DLC, and DLE were in the ranges of 23.73 ± 0.14%, 5.62%, and 0.23%, respectively. The in vitro release profile, performed in phosphate buffer saline (PBS, pH 7.4) at 37 °C, indicated that the synthetized Chi–DHAr nanoparticles provided a sustained release of 5-FU. Based on the obtained regression coefficient value (R2), the first order kinetic model provided the best fit for both Chir and Chi-DHAr nanoparticles. Finally, cytotoxicity studies of chitosan, 5-FU, Chir, Chir + 5-FU, Chi-DHAr, and Chi-DHAr + 5-FU nanoparticles were conducted. Overall, Chi-DHAr nanoparticles proved to be much more biocompatible than Chir nanoparticles while retaining the ability to release the drug with high efficiency, especially towards specific types of cancerous cells.
Highlights
Chitin and chitosan are the second-most abundant naturally-occurring polysaccharides, following cellulose, and they can be extracted from wastes of the fishing industry
chitosan oligosaccharide with low-molecular weight (Chi)-DHAr nanoparticles were prepared by the ionic gelation technique, while Chi-docosahexaenoic acid (DHA) conjugate was prepared by using EDC carbodiimide cross linker
The obtained conjugate was investigated by FT-IR spectroscopy and swelling studies, which confirmed the presence of a stable amide bond between the carboxyl group of DHA and the amine group of Chi while the dimensions and surfaces of nanoparticles were investigated with dynamic light scattering (DLS) and scanning electron microscopy (SEM) instruments
Summary
Chitin and chitosan are the second-most abundant naturally-occurring polysaccharides, following cellulose, and they can be extracted from wastes of the fishing industry. One of the most feasible reactions that can be carried out to achieve amphiphilic Chi involves the condensation of a fatty acid with the amino group of glucosamine monomer These chemical modifications allow the chitosan structure to become amphiphilic and for nanoparticles with a nanometric size to be obtained by using the ionic gelation technique. If 5-FU maintains high levels in serum concentrations, it is involved in severe toxic effects and, for this reason, a system for controlled release of 5-FU, such as nanoparticles, may overcome this problem This kind of drug delivery system can reduce its adverse effect and enhance its therapeutic index [10].
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