Controlled Release of 5-FU from Chi–DHA Nanoparticles Synthetized with Ionic Gelation Technique: Evaluation of Release Profile Kinetics and Cytotoxicity Effect

Abstract

<jats:p>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.</jats:p>

Polysaccharide-Based Hydrogels and Their Application as Drug Delivery Systems in Cancer Treatment: A Review

“…CHI’s cationic groups’ reaction with the polyanion of sodium triphosphate (TPP) also represents an ionic gelation approach: when TPP is dissolved into a CHI solution, the polyanion binds to a positive amino group by electrostatic interaction. This represents the starting point of the gelation process that will lead to the formation of CHI nanoparticles [ 38 ].…”

Large-Scale Preparation of Peanut-Bran-Derived Carbon Dots and Their Promoting Effect on Italian Lettuce

“…They have broad application prospects in biological fields such as bioimaging, biosensing, photocatalysis, and gene delivery. − Since the discovery of fluorescent CDs during the purification of single-walled carbon nanotubes in 2004, different methods for preparing CDs including laser ablation, electrochemical, hydrothermal/solvothermal, and microwave-assisted methods have been developed. Using a carbonization method to prepare CDs also has been reported. − In the past few decades, abundant CD materials have been developed for agriculture applications, for example, monitoring crop health, promoting crop growth, improving the efficiency of fertilizers and pesticides, , controlling diseases and pests, environmental stress, and many other fields. − Compared with other metal-based nanomaterials, carbon-based nanomaterials have lower environmental toxicity and higher biocompatibility due to their nontoxic carbon backbone. − However, in the current research, the synthesis of CDs is small scale, and methods for the mass production of CDs have rarely been reported.…”