Controlled release study of 5-fluorouracil-loaded chitosan/polyethylene glycol microparticles

Lin, Chuen−Chang; Fu, Chun-Hsien

doi:10.1080/10717540902987625

Cited by 11 publications

(7 citation statements)

References 10 publications

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“…It has gained much importance because of its chemical and biological properties, including its particle size, viscosity, density, degree of deacetylation, biodegradable and biocompatible characteristics, and lower toxicity 9, 10. Chitosan is widely used as in sponge and wound‐dressing materials,11 artificial kidney membranes,12 antacids and antiulcer agents,13 cosmetics,14 contact lenses,15 solid‐state batteries,16 photography,17 and drug‐delivery devices in the form of microspheres,18–21 nanoparticles,22, 23 beads,24 tablets,25 and membranes 26…”

Section: Introductionmentioning

confidence: 99%

Preparation and characterization of crosslinked chitosan microspheres for the colonic delivery of 5‐fluorouracil

Bhat

Keshavayya

Kulkarni³

et al. 2012

J of Applied Polymer Sci

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In this work, we attempted to develop a simple and inexpensive colon specific pulsatile drug‐delivery system using chitosan microspheres loaded with 5‐fluorouracil (5‐FU) using an enteric‐coated soft gelatin capsule. Chemical crosslinking by glutaraldehyde and interactions between the polymer and the drug were determined by Fourier transform infrared spectral study. Scanning electron microscopy of the microspheres revealed spherical shapes with smooth surfaces. Differential scanning calorimetry studies confirmed the molecular dispersion of the drug in the polymer matrix. Three different formulations (i.e., F1, F2, and F3) were prepared by the variation of the amount of 5‐FU. Encapsulation efficiencies of 5.5, 10.8, and 17.9% for drug loadings of 10, 20, and 50%, respectively, were obtained. In vitro release studies were conducted at pH 1.2 and pH 7.4 (to simulate actual gastrointestinal fluid and gastrointestinal tract conditions, respectively). The results indicate that chitosan microspheres released 5‐FU in both acidic (60%) and basic pH (40%) conditions, whereas the capsule (filled with chitosan microspheres) showed only 8–10% release in acidic media and nearly 90% in basic media within 12 h. The newly designed pulsatile capsule device could be used for targeting 5‐FU to the colon. © 2012 Wiley Periodicals, Inc. J Appl Polym Sci, 2012

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Section: Introductionmentioning

confidence: 99%

Preparation and characterization of crosslinked chitosan microspheres for the colonic delivery of 5‐fluorouracil

Bhat

Keshavayya

Kulkarni³

et al. 2012

J of Applied Polymer Sci

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“…5 In addition, a lot of polymeric nanoparticles, such as poly (Nisopropylacrylamide-co-acrylic acid), poly-(2-hydroxyethyl methacrylate), and chitosan/polyethylene glycol, were also used as carriers of 5-fluorouracil. [6][7][8][9] However, the degradation of synthetic polymers has been shown to cause unwanted toxic effects. 10 Among the drug delivery systems, inorganic materials, such as layered double hydroxides (LDHs), have attracted attention in recent years because LDHs have many advantages, including good biocompatibility, nontoxicity, and adjustable controlledrelease property.…”

Section: Introductionmentioning

confidence: 99%

“…Huang demonstrated a proof-of-concept approach for producing genipin−gelatin microcapsules, and it can enhance the effect of controlled release of 5-fluorouracil . In addition, a lot of polymeric nanoparticles, such as poly ( N -isopropylacrylamide- co -acrylic acid), poly-(2-hydroxyethyl methacrylate), and chitosan/polyethylene glycol, were also used as carriers of 5-fluorouracil. − However, the degradation of synthetic polymers has been shown to cause unwanted toxic effects…”

Section: Introductionmentioning

confidence: 99%

Preparation of 5-Fluorouracil/β-Cyclodextrin Complex Intercalated in Layered Double Hydroxide and the Controlled Drug Release Properties

Jin¹,

Liu²,

Sun³

et al. 2010

Ind. Eng. Chem. Res.

115

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Hydrophobic anticancer drug 5-fluorouracil (5-FU) has been included in the carboxymethyl modified β-cyclodextrin (CMCD), and the inclusion complex (5-FU/CMCD) was further intercalated into galleries of a zinc aluminum layered double hydroxide (ZnAl−LDH) by the ion-exchange method. Powder X-ray diffraction (XRD), Fourier transform infrared (FT-IR), and UV−vis spectroscopy indicate a successful intercalation of 5-FU/CMCD into the LDH gallery. The release behavior of 5-FU from drug/CMCD−LDH composite at different pH values was studied. It was found that 5-FU was released faster in pH 7.2 than in the acidic mediums (pH 4.8), and the released amount was higher. The introduction of CMCD into the LDH matrix could prolong the drug release time in comparison to that from LDH without CMCD, which can be attributed to the inclusion of 5-FU by the CMCD cavity. Studies on mathematical modeling of drug release show that the release of 5-FU from the drug/CMCD−LDH composite follows the Korsmeyer−Peppas equation very well at different pH values. The drug/CMCD inclusion complex intercalated LDH composite in this work provides a supramolecular formulation for controlled release behavior, which can be potentially applied for nonionic and hydrophobic drugs.

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“…Helaly et al [1] studied the slow release of 5-FU from the natural polymeric composite. Lin et al [14] performed the controlled release of 5-FU loaded chitosan/polyethylene glycol microparticles. Huang et al [15] studied the preparation of chondroitin sulfate/chitosan complex microcapsules and their application to the controlled release of 5-FU.…”

Section: Introductionmentioning

confidence: 99%

Starch‐Based Membranes for Controlled Release of 5‐Fluorouracil In Vitro

2021

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Starch is a natural polymer that is among the sustainable materials and has the characteristics of being a green material in harmony with nature. In this study, a potential transdermal release system was evaluated by investigating 5-fluorouracil (5-FU) transfer through starch/poly(vinyl alcohol) (PVA) membranes in vitro. The effects of membrane thickness, starch/PVA blending ratio, pH, and temperature on the release of 5-FU from the membranes were studied. At the end of the study, it was deduced that decrease in pH reduces the released amount of 5-FU from starch/PVA membranes and 5-FU transfer from membranes could be controlled within a fairly constant range. The diffusion coefficient was determined as 4.84�10 À 3 , 4.49 �10 À 3 and 2.54�10 À 3 cm 2 s À 1 for the pH of 7.4, 5.5, and 3.5, respectively. The activation energy for the permeation 5-FU from starch/PVA membrane (60/40, v/v) was found to be 9.72 kJ mol À 1 .

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Controlled release study of 5-fluorouracil-loaded chitosan/polyethylene glycol microparticles

Cited by 11 publications

References 10 publications

Preparation and characterization of crosslinked chitosan microspheres for the colonic delivery of 5‐fluorouracil

Preparation and characterization of crosslinked chitosan microspheres for the colonic delivery of 5‐fluorouracil

Preparation of 5-Fluorouracil/β-Cyclodextrin Complex Intercalated in Layered Double Hydroxide and the Controlled Drug Release Properties

Starch‐Based Membranes for Controlled Release of 5‐Fluorouracil In Vitro

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