Preparation of 5-fluorouracil-loaded chitosan nanoparticles and study of the sustained release in vitro and in vivo

Sun, Li; Chen, Yunna; Zhou, Yali; Guo, Dongdong; Fan, Yufan; Guo, Fangyan; Yong, Zheng; Chen, Weidong

doi:10.1016/j.ajps.2017.04.002

Cited by 142 publications

(75 citation statements)

References 19 publications

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“…Additionally, faster release of 5‐FU is observed at pH 9.0 than at pH 7.4 and 4.7. These phenomena are plausibly related to the solubility of 5‐FU, which is higher in alkaline solutions ,. This feature explains the release of 5‐FU in both segments.…”

Section: Resultsmentioning

confidence: 85%

“…The controlled release of a drug may lower its side effects and increases its therapeutic effect on tumors. The complexation of 5‐FU or its derivatives (for example tegafur) inside βCD attached to polymeric vectors, carbon materials, or iron oxide nanoparticles, were reported. The in vitro or in vivo studies revealed the therapeutic potential of the designed 5‐FU delivery platforms.…”

Section: Introductionmentioning

confidence: 99%

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Folic Acid‐Navigated and β‐Cyclodextrin‐Decorated Carbon‐Encapsulated Iron Nanoparticles as the Nanotheranostic Platform for Controlled Release of 5‐Fluorouracil

et al. 2018

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The theranostic probe based on carbon‐encapsulated iron nanoparticles (CEINs) is presented. First, the conjugates of CEINs and polyethylenimine (PEI) were obtained to modify the surface of CEINs with amino groups. It was archived either by means of direct radical addition of PEI to CEINs (CEINs‐NH‐PEI material) or the amidation‐type reaction between CEINs∼COOH and the polymer (CEINs∼CONH‐PEI material obtained). β‐Cyclodextrin (βCD) was selected as the drug delivery vector. βCD was covalently anchored to the PEI‐functionalized CEINs via the 1,1’‐carbonyldiimidazole‐mediated reaction. The synthesis included the conjugation of folic acid (FA; targeting ligand) to CEINs via the carbodiimide‐mediated amidation‐type process. The innovative method for excluding a side process of the FA@βCD complex formation during the FA conjugation to PEI, was developed. 5‐Fluorouracil (5‐FU) was chosen as the representative drug molecule. 5‐FU was anchored to the CEINs∼PEI∼βCD∼FA nanoplatforms employing the host‐guest chemistry of βCD. The success of the reactions was confirmed by infrared spectroscopy and thermogravimetry. The content of anchored organic compounds depends on the type of linkage between PEI and CEINs. Additionally, 5‐FU release profile was examined at various pH. The highest release of 5‐FU was observed at pH 9.0, whilst the lowest at pH 4.7. This work sheds a new light on application of carbon‐encapsulated iron nanoparticles in nanomedicine as the novel drug delivery theranostic systems.

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Section: Resultsmentioning

confidence: 85%

Section: Introductionmentioning

confidence: 99%

Folic Acid‐Navigated and β‐Cyclodextrin‐Decorated Carbon‐Encapsulated Iron Nanoparticles as the Nanotheranostic Platform for Controlled Release of 5‐Fluorouracil

et al. 2018

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“…16 It is found primarily in marine animals' exoskeleton, ie, lobsters, shrimps and crabs. Chitosan is immunogenic, and its antitumor, anti-inflammatory, antibacterial, antifungal, and antimicrobial activities have been observed.- 17,18 It has been reported that preparation of chitosan as nanoparticles revealed no toxicity at lower concentration (30 µg/ mL) but showed anticancer activity at higher concentrations (>100 µg/mL) against different cancer cell lines, which supports its application as a drug delivery system. 17,19 Previously, chitosan nanoparticles (CsNPs) have been conjugated with antiretroviral agents like saquinavir, a protease inhibitor, to improve anti-HIV therapy; cell targeting efficiency increased by 92% compared to the soluble drug control.…”

Section: Introductionmentioning

confidence: 94%

<p>Antiviral Activity of Chitosan Nanoparticles Encapsulating Curcumin Against Hepatitis C Virus Genotype 4a in Human Hepatoma Cell Lines</p>

Loutfy¹,

Elberry²,

Farroh³

et al. 2020

IJN

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Purpose: Current direct-acting antiviral agents for treatment of hepatitis C virus genotype 4a (HCV-4a) have been reported to cause adverse effects, and therefore less toxic antivirals are needed. This study investigated the role of curcumin chitosan (CuCs) nanocomposite as a potential anti-HCV-4a agent in human hepatoma cells Huh7. Methods: Docking of curcumin and CuCs nanocomposite and binding energy calculations were carried out. Chitosan nanoparticles (CsNPs) and CuCs nanocomposite were prepared with an ionic gelation method and characterized with TEM, zeta size and potential, and HPLC to calculate encapsulation efficiency. Cytotoxicity studies were performed on Huh7 cells using MTT assay and confirmed with cellular and molecular assays. Anti-HCV-4a activity was determined using real-time PCR and Western blot. Results: The strength of binding interactions between protein ligand complexes gave scores with NS3 protease, NS5A polymerase, and NS5B polymerase of -124.91, -159.02, and -129.16, for curcumin respectively, and -68.51, -54.52, and -157.63 for CuCs nanocomposite, respectively. CuCs nanocomposite was prepared at sizes 29-39.5 nm and charges of 33 mV. HPLC detected 4% of curcumin encapsulated into CsNPs. IC50 was 8 µg/mL for curcumin and 25 µg/ mL for the nanocomposite on Huh7 but was 25.8 µg/mL and 34 µg/mL on WISH cells. CsNPs had no cytotoxic effect on tested cell lines. Apoptotic genes' expression revealed the caspasedependent pathway mechanism. CsNPs and CuCs nanocomposite demonstrated 100% inhibition of viral entry and replication, which was confirmed with HCV core protein expression. Conclusion: CuCs nanocomposite inhibited HCV-4a entry and replication compared to curcumin alone, suggesting its potential role as an effective therapeutic agent. Plain Language SummaryHepatitis C virus genotype 4a (HCV-4a) is a major public health problem, especially among the Egyptian population. There are more than 70 million individuals infected worldwide. It is the leading cause of chronic liver diseases, cirrhosis, and hepatocellular carcinoma. Newly emerged anti-HCV viral agents have recently become available on the market but with serious complications, high cost, and possible development of resistance. This has encouraged scientists to search for alternative, safer antiviral approaches. Nanoparticles offer unique physical properties that have associated benefits for antimicrobial activity or as drug carrier that can improve antiviral therapy. The significance of our research is in establishment of a natural nanoparticle drug carrier system that we screened with computer simulation studies and in cells against HCV-4a replication into human hepatoblastoma cell

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“…The recommended chemotherapeutic drug of choice for this purpose is 5-Fluorouracil (5-FU) though other antineoplastic drugs are also available. 5-FU is the first line drug used in the treatment of cancer 2 . Because of its inefficacy in the therapy, due to the poor selectivity and the other side effects such as mucositis, myelosuppression, emesis, nausea, and hand-foot syndrome the formulation of this drug is constantly facing various challenges.…”

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confidence: 99%

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2019

IJPSR

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Objective: The Failure in chemotherapy is mainly because of the resistance of the chemotherapeutic drugs towards the neoplastic cells. The main reason behind this study was to develop a novel combination of 5-Fluorouracil (5-FU) lipid curcumin conjugates for the treatment of cancer. Methods: In this study, the lipid group stearic acid and oleic acid was conjugated with the parent drug moiety 5-Fluorouracil to acquire lipophilicity. The next step involves the conjugation of curcumin with 5-Fluorouracil lipid to form a lipid dual drug conjugate. The characterization of conjugates followed the synthesis part by using FT-IR, DSC, and LCMS. The conjugates hence obtained were further carried for formulation aspect. After the successful completion of the formulation part, in-vitro studies and MTT Assay was performed. Results: The results depict the successful synthesis of the conjugates, and its characterization was successfully done. The conjugates are formulated into Self Nanomulsifying drug delivery system (SNEDDS). The results obtained from the MTT assay also shown a significant cytotoxic effect in both the conjugation. Conclusion: The in-vitro results suggest further studies for cleavage of the drug and the lipids in the conjugate and in-vivo animal studies to demonstrate the anticancer efficacy.

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Preparation of 5-fluorouracil-loaded chitosan nanoparticles and study of the sustained release in vitro and in vivo

Cited by 142 publications

References 19 publications

Folic Acid‐Navigated and β‐Cyclodextrin‐Decorated Carbon‐Encapsulated Iron Nanoparticles as the Nanotheranostic Platform for Controlled Release of 5‐Fluorouracil

Folic Acid‐Navigated and β‐Cyclodextrin‐Decorated Carbon‐Encapsulated Iron Nanoparticles as the Nanotheranostic Platform for Controlled Release of 5‐Fluorouracil

<p>Antiviral Activity of Chitosan Nanoparticles Encapsulating Curcumin Against Hepatitis C Virus Genotype 4a in Human Hepatoma Cell Lines</p>

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