Pharmacokinetic characteristics and anticancer effects of 5-Fluorouracil loaded nanoparticles

Li, Su; Wang, Anxun; Jiang, Wenqi; Guan, Zhi‐Zhong

doi:10.1186/1471-2407-8-103

Cited by 98 publications

(90 citation statements)

References 31 publications

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“…The nanoparticles were successfully prepared with considerably good encapsulation efficiency 25 and high yield. From the TEM images ( Figure 1) and size distribution graph (Figure 2), it was shown that particles with spherical size and uniform size distribution were obtained.…”

Section: -Fluorouracil Nanoparticlesmentioning

confidence: 99%

“…Studies have shown that nanoparticles carrying anticancer agents show prolonged drug retention in the tumors, which diminishes tumor growth and thereby increases the life-span of tumor-bearing animals. [22][23][24] Although studies are in progress to increase the bioavailability of 5-FU with nanoparticle carrier systems, 25,26 data showing biological efficacy of PLGA nanoparticles as a carrier for 5-FU have hardly been reported. Moreover, dependence of these nanoparticles on the combination of PLGA used has not been investigated so far.…”

Section: Introductionmentioning

confidence: 99%

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Biological evaluation of 5-fluorouracil nanoparticles for cancer chemotherapy and its dependence on the carrier, PLGA

K¹,

Jagadeeshan²,

Nair³

et al. 2011

IJN

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Nanoscaled devices have great potential for drug delivery applications due to their small size. In the present study, we report for the first time the preparation and evaluation of antitumor efficacy of 5-fluorouracil (5-FU)-entrapped poly (D, L-lactic-co-glycolic acid) (PLGA) nanoparticles with dependence on the lactide/glycolide combination of PLGA. 5-FU-loaded PLGA nanoparticles with two different monomer combinations, 50-50 and 90-10 were synthesized using a modified double emulsion method, and their biological evaluation was done in glioma (U87MG) and breast adenocarcinoma (MCF7) cell lines. 5-FU-entrapped PLGA 50-50 nanoparticles showed smaller size with a high encapsulation efficiency of 66%, which was equivalent to that of PLGA 90-10 nanoparticles. Physicochemical characterization of nanoparticles using differential scanning calorimetry and X-ray diffraction suggested the presence of 5-FU in molecular dispersion form. In vitro release studies showed the prolonged and sustained release of 5-FU from nanoparticles with both the PLGA combinations, where PLGA 50-50 nanoparticles showed faster release. Nanoparticles with PLGA 50-50 combination exhibited better cytotoxicity than free drug in a dose- and time-dependent manner against both the tumor cell lines. The enhanced efficiency of PLGA 50-50 nanoparticles to induce apoptosis was indicated by acridine orange/ethidium bromide staining. Cell cycle perturbations studied using flow cytometer showed better S-phase arrest by nanoparticles in comparison with free 5-FU. All the results indicate that PLGA 50-50 nanoparticles possess better antitumor efficacy than PLGA 90-10 nanoparticles and free 5-FU. Since, studies have shown that long-term exposure of ailing tissues to moderate drug concentrations is more favorable than regular administration of higher concentration of the drug; our results clearly indicate the potential of 5-FU-loaded PLGA nanoparticles with dependence on carrier combination as controlled release formulation to multiplex the therapeutic effect of cancer chemotherapy.

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Section: -Fluorouracil Nanoparticlesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Biological evaluation of 5-fluorouracil nanoparticles for cancer chemotherapy and its dependence on the carrier, PLGA

K¹,

Jagadeeshan²,

Nair³

et al. 2011

IJN

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show abstract

“…Dialysis simplicity has been exploited for tracking 5-FU release from poly(lactic-coglycolic acid), chitosan, pullulan-sulfonamide, and poly(γ-benzyl-L-glutamate) nanoparticles (13)(14)(15)(16)(17)(18). Some researchers used Franz cell dissolution apparatus or paddle apparatus (USP XXIII) to analyze the in vitro 5-FU release from polymeric nanoparticles (19,20).…”

Section: Introductionmentioning

confidence: 99%

5-Fluorouracil-Loaded BSA Nanoparticles: Formulation Optimization and In Vitro Release Study

2008

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Abstract. Over the past few decades, there has been considerable interest in developing protein nanoparticles as drug delivery devices. The underlying rationale is their exceptional characteristics, namely biodegradability and nonantigenicity. Herein, phase separation method was used to prepare 5-fluorouracil-loaded bovine serum albumin (BSA) nanoparticles. Drug release was tracked by continuous flow dialysis technique. Effect of process variables on loading efficiency of 5-fluorouracil was investigated and optimized through Taguchi's M16 design with the amount of entrapped drug as response. Optimum condition was found to be 2 mg/mL of 5-fluorouracil, 3.7 mL of added ethanol, 176 µL of glutaraldehyde, drug-protein incubation time of 30 min, and pH of 8.4 for 200 mg of BSA in 2 mL drug solution. pH had the most noticeable effect on the amount of entrapped drug, but glutaraldehyde had the least. Mean diameter and zeta potential of fabricated nanoparticles under these conditions were 210 nm and −31.7 mV, respectively. Drug-loaded BSA nanoparticles suspension maintained constant release of drug for 20 h under experimental conditions, so this colloidal drug carrier is capable of releasing drug in a sustained manner.

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“…As we known, fluorouracil interferes with DNA synthesis by blocking thymidylates, an enzyme involved in the conversion of deoxyuridylic acid to thymidylic acid (Li et al, 2008). Docetaxel can impair the dynamic of microtubules, promote their polymerization, and arrest the cells in mitosis by binding to the β subunit of tubulin (Hernandez-Vargas et al, 2007).…”

Section: Discussionmentioning

confidence: 99%

Overexpression of Cyclin L2 Inhibits Growth and Enhances Chemosensitivity in Human Gastric Cancer Cells

Ding

Deng

et al. 2012

Asian Pacific Journal of Cancer Prevention

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Pharmacokinetic characteristics and anticancer effects of 5-Fluorouracil loaded nanoparticles

Cited by 98 publications

References 31 publications

Biological evaluation of 5-fluorouracil nanoparticles for cancer chemotherapy and its dependence on the carrier, PLGA

Biological evaluation of 5-fluorouracil nanoparticles for cancer chemotherapy and its dependence on the carrier, PLGA

5-Fluorouracil-Loaded BSA Nanoparticles: Formulation Optimization and In Vitro Release Study

Overexpression of Cyclin L2 Inhibits Growth and Enhances Chemosensitivity in Human Gastric Cancer Cells

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