Formulation, characterization and in vitro release study of 5-fluorouracil loaded chitosan nanoparticles

Samy, Moshera; El-Alim, Sameh Hosam Abd; Rabia, Abd El Gawad; Amin, Amal; Ayoub, Magdy M. H.

doi:10.1016/j.ijbiomac.2020.04.112

Cited by 61 publications

(24 citation statements)

References 58 publications

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“…In addition, the characteristic crystalline peaks of 5-FU were not seen after ERS coating on 5-FU-loaded SEMC (Figure 5e), but only the characteristic peaks of SEMC were found with low intensities (1193 and 484 cps) at 2θ (38.1 and 44.3 deg) with d-values (2.36 and 2.04) and I/I 0 values of 100 and 41, respectively in F2-ERS. The above findings are in agreement with a previous report of 5-FU-loaded PCL and PLGA-NPs [61] as well as 5-FU-loaded chitosan-NPs [62,63]. Conclusively, the absence or disappearance of the characteristic crystalline peaks of 5-FU in F2 and F2-ERS indicate the existence of 5-FU in an amorphous state in the pores and matrix of the SEMC.…”

Section: Powdered X-ray Diffraction (Pxrd)supporting

confidence: 93%

Eudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of Phoenix dactylifera L. of 5-Fluorouracil for Colon-Specific Drug Delivery

et al. 2021

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In this study, 5-fluorouracil (5-FU)-loaded pollens of Phoenix dactylifera and their coating with ERS was done and evaluated for the colon-targeted delivery of 5-FU to treat colon cancer. Sporopollenin exine microcapsules (SEMC) from the pollens of Phoenix dactylifera were extracted by the reflux method and 5-FU into SEMC was encapsulated by the vacuum-assisted loading method. 5-FU loaded SEMC was coated with Eudragit® RS-100 (ERS) by the organic solvent-evaporation technique under vacuum to avoid the discharge of 5-FU in the stomach and small intestine. Morphological and physicochemical characterization of drug-loaded SEMC (coated/uncoated) was performed by scanning electron microscopy (SEM), FTIR, XRD, and DSC. The encapsulation and drug loading were determined by the direct method, and an in vitro release study was performed in simulated gastric and intestinal fluids (SGF/SIF). The colon-specific delivery of 5-FU from the SEMC was assessed in terms of pharmacokinetics and gastrointestinal tract distribution after oral administration in rats. The successful encapsulation and loading of 5-FU into SEMC by a vacuum-assisted loading technique and its coating with ERS by a solvent-evaporation technique were achieved. SEM images of uncoated SEMC have shown porous structures, and coating with ERS reserved their morphology with a smooth surface and discrete microstructures and the 5% w/v ERS acetone solution. ERS-coated SEMC sustained the release of 5-FU until 24 h in SIF, while it was up to 12 h only from uncoated SEMC. The maximum plasma concentration (Cmax) of 5-FU from uncoated SEMC was 102.82 μg/mL after 1 h, indicating a rapid release of 5-FU in the upper gastrointestinal tract. This concentration decreased quickly with a half-life of 4 h, AUC0-t was 264.1 μg/mL.h, and MRT0-inf was 5.2 h. The Cmax of 5-FU from ERS-coated SEMC was 19.47 μg/mL at 16 h. The Cmax of 5-FU in small intestines was 406.2 μg/g at 1 h from uncoated SEMC and 1271.5 μg/g at 12 h from coated SEMC. Conclusively, a 249.9-fold higher relative bioavailability of 5-FU was achieved with the ERS-coated SEMC in colon tissues than that from uncoated SEMC.

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Section: Powdered X-ray Diffraction (Pxrd)supporting

confidence: 93%

Eudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of Phoenix dactylifera L. of 5-Fluorouracil for Colon-Specific Drug Delivery

et al. 2021

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“…The kinetic analysis of drug release from CSNP can be carried out by mathematical models such as the zero-order model, first-order model, the Higuchi model, the Hixson-Crowell cube root law, the Baker-Lonsdale time kinetics equation, and the Peppas exponential model [ 139 ]. The diffusion-controlled release kinetics were investigated using the zero-order, first-order, and Higuchi models.…”

Section: Drug Release From Csnpsmentioning

confidence: 99%

Drug release study of the chitosan-based nanoparticles

Herdiana

Wathoni

Shamsuddin

et al. 2022

Heliyon

236

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Recently, multifunctional drug delivery systems (DDSs) have been designed to provide a comprehensive approach with multiple functionalities, including diagnostic imaging, targeted drug delivery, and controlled drug release. Chitosan-based drug nanoparticles (CSNPs) systems are employed as diagnostic imaging and delivering the drug to particular targeted sites in a regulated manner. Drug release is an important factor in ensuring high reproducibility, stability, quality control of CSNPs, and scientific-based for developing CSNPs. Several factors influence drug release from CSNPs, including composition, composition ratio, ingredient interactions, and preparation methods. Early, CSNPs were used for improving drug solubility, stability, pharmacokinetics, and pharmacotherapeutics properties. Chitosan has been developed toward a multifunctional drug delivery system by exploring positively charged properties and modifiable functional groups. Various modifications to the polymer backbone, charge, or functional groups will undoubtedly affect the drug release from CSNPs. The drug release from CSNPs has a significant influence on its therapeutic actions. Our review's objective was to summarize and discuss the relationship between the modification in CSNPs as multifunctional delivery systems and drug release properties and kinetics of the drug release model. Kinetic models help describe the release rate, leading to increased efficiency, accuracy, the safety of the dose, optimizing the drug delivery device's design, evaluating the drug release rate, and improvement of patient compatibility. In conclusion, almost all CSNPs showed bi-phasic release, initial burst release drug in a particular time followed controlled manner release in achieving the expected release, stimuli external can be applied. CSNPs are a promising technique for multifunctional drug delivery systems.

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“…This could be possibly due to using higher ratio of the cellulose and scleroglucan than chitosan. Studies by Samy et al (2020) have shown that the ratio between chitosan and cellulose was 1:1 and epichlorohydrin acted as a cross-linker [ 46 ]. This composite showed size above 100 nm, according to the SEM images.…”

Section: Resultsmentioning

confidence: 99%

5-Fluorouracil Encapsulated Chitosan-Cellulose Fiber Bionanocomposites: Synthesis, Characterization and In Vitro Analysis towards Colorectal Cancer Cells

et al. 2021

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Cellulose and chitosan with remarkable biocompatibility and sophisticated physiochemical characteristics can be a new dawn to the advanced drug nano-carriers in cancer treatment. This study aims to synthesize layer-by-layer bionanocomposites from chitosan and rice straw cellulose encapsulated 5-Fluorouracil (CS-CF/5FU BNCs) using the ionic gelation method and the sodium tripolyphosphate (TPP) cross-linker. Data from X-ray and Fourier-transform infrared spectroscopy showed successful preparation of CS-CF/5FU BNCs. Based on images of scanning electron microscopy, 48.73 ± 1.52 nm was estimated for an average size of the bionanocomposites as spherical chitosan nanoparticles mostly coated rod-shaped cellulose reinforcement. 5-Fluorouracil indicated an increase in thermal stability after its encapsulation in the bionanocomposites. The drug encapsulation efficiency was found to be 86 ± 2.75%. CS-CF/5FU BNCs triggered higher drug release in a media simulating the colorectal fluid with pH 7.4 (76.82 ± 1.29%) than the gastric fluid with pH 1.2 (42.37 ± 0.43%). In in vitro cytotoxicity assays, cellulose fibers, chitosan nanoparticles and the bionanocomposites indicated biocompatibility towards CCD112 normal cells. Most promisingly, CS-CF/5FU BNCs at 250 µg/mL concentration eliminated 56.42 ± 0.41% of HCT116 cancer cells and only 8.16 ± 2.11% of CCD112 normal cells. Therefore, this study demonstrates that CS-CF/5FU BNCs can be considered as an eco-friendly and innovative nanodrug candidate for potential colorectal cancer treatment.

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Formulation, characterization and in vitro release study of 5-fluorouracil loaded chitosan nanoparticles

Cited by 61 publications

References 58 publications

Eudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of Phoenix dactylifera L. of 5-Fluorouracil for Colon-Specific Drug Delivery

Eudragit-Coated Sporopollenin Exine Microcapsules (SEMC) of Phoenix dactylifera L. of 5-Fluorouracil for Colon-Specific Drug Delivery

Drug release study of the chitosan-based nanoparticles

5-Fluorouracil Encapsulated Chitosan-Cellulose Fiber Bionanocomposites: Synthesis, Characterization and In Vitro Analysis towards Colorectal Cancer Cells

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