Formulation and investigation of 5-FU nanoparticles with factorial design-based studies

Bozkır, Asuman; Saka, Ongun Mehmet

doi:10.1016/j.farmac.2005.06.016

Cited by 68 publications

(33 citation statements)

References 17 publications

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“…Several methods are described in the literature for the determination of 5-FU in samples of biological matrices using gas chromatography/mass spectrometry (GC/MS) (Anderson et al, 1997), spectrometry (Badea et al, 2002), high performance liquid chromatography (HPLC) (Escoriaza et al, 1999), hydrophilic interaction liquid chromatography-APCI-mass spectrometry (Pisano et al, 2005) or liquid chromatography tandem mass spectrometry (LC-MS/MS) (Licea-Perez, Wang, Bowen, 2009;Liu et al, 2010). The analytical determination of 5-FU in pharmaceutical dosage forms such as nanoparticles has been performed by several authors using spectrophotometry (Bozkir, Saka, 2005;Liu et al, 2006;Zhu et al, 2009;Lai, Guo, 2011;Li et al, 2011;Rejinold et al, 2011a;Rejinold et al, 2011b;Zhang et al, 2011), but few studies report the use of HPLC methods for this determination. Arbós, Campanero and Irache (2002) described an HPLC method for the quantitation of 5-fluorouridine in nanoparticles and verified the possible degradation of 5-FU, but the investigators used a C8 column.…”

Section: Introductionmentioning

confidence: 99%

Development and validation of an HPLC method for the determination of fluorouracil in polymeric nanoparticles

Mattos

Khalil

Mainardes

2013

Braz. J. Pharm. Sci.

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The objective of this work was to develop and validate a rapid high performance liquid chromatography (HPLC) method for the quantitative analysis of fluorouracil (5-FU) in polymeric nanoparticles. Chromatographic analyses were performed on an RP C18 column with a mobile phase consisting of acetonitrile and water (10:90, v/v) at a flow rate of 1 mL/min. The 5-FU was detected and quantitated using a photodiode array detector at a wavelength of 265 nm. The method was shown to be specific and linear in the range of 0.1-10 μg/mL (r = 0.9997). The precision (intra-and inter-day) was demonstrated because the maximum relative standard deviation was 3.51%. The method is robust relative to changes in flow rate, column and temperature. The limits of detection and quantitation were 10.86 and 32.78 ng/mL, respectively. The method fulfilled the requirements for reliability and feasibility for application to the quantitative analysis of 5-FU in polymeric nanoparticles.Uniterms: Fluorouracil/determination. Nanoparticles. High performance liquid chromatography/ quantitative analysis/method validation.O objetivo deste trabalho foi desenvolver e validar um método rápido de cromatografia líquida de alta eficiência (CLAE) para análise quantitativa de fluorouracila (5-FU) em nanopartículas poliméricas. Corridas cromatográficas foram realizadas sob uma coluna RP C18 com uma fase móvel consistindo de acetonitrila e água (10:90, v/v) a um fluxo de 1 mL/min. O 5-FU foi detectado e quantificado através de um detector de fotodiodos em um comprimento de onda de 265 nm. O método demonstrou ser específico e linear na faixa de 0,1-10 μg/mL (r =0.9997). As precisões (intra e inter dia) revelaram um desvio padrão relativo máximo de 3,51%. O método é robusto considerando mudanças realizadas no fluxo da fase móvel, temperatura e marca da coluna. Os limites de detecção e quantificação foram de 10,86 e 32,78 ng/mL, respectivamente. O método cumpriu os requisitos para ser considerado confiável e viável para aplicação na análise quantitativa de 5-FU em nanopartículas poliméricas.Unitermos: Fluorouracila/determinação. Nanopartículas. Cromatografia líquida de alta eficiências/ análise quantitativa/validação de método.

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Section: Introductionmentioning

confidence: 99%

Development and validation of an HPLC method for the determination of fluorouracil in polymeric nanoparticles

Mattos

Khalil

Mainardes

2013

Braz. J. Pharm. Sci.

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“…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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“…Non ophthalmic nanoparticles of 5-FU using polymers such as poly(butylcyanoacrylate), 2) poly(lactic acid), poly-(lactide-co-glycolide) 3) and chitosan [4][5][6] have been reported, but investigators have not explored the application of 5-FU loaded nanoparticles (DNPs) for the treatment of ocular application.…”

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confidence: 99%

Chitosan Nanoparticles of 5-Fluorouracil for Ophthalmic Delivery: Characterization, in-Vitro and in-Vivo Study

et al. 2011

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5-FU is a pyrimidine analogue commonly used to treat many epithelial cancers. It acts by interacting with S phase cells (those actively synthesizing DNA). Therefore, it is suitable to treat squamous cell carcinoma because squamous tumours are composed of rapidly proliferating abnormal epithelial cells. It has limited side effects on the normal ocular surface epithelium.1) 5-FU is an inexpensive drug, easily handled by medical personnel and patients, and is stable in aqueous solution for at least 3 weeks. It does not need to be stored in a refrigerator. Topical solution of this drug is always prepared extemporaneously. The acute and chronic side effects of mitomycin C (MMC) are definitely much more frequent and serious than those induced by 5-FU, as referred to by clinicians using MMC for pigmented conjunctival lesions. 1)Currently 1% of 5-FU solution is used by the ophthalmologist which is a high concentration for ophthalmic application. Bioavailability at anterior segment of eye is obtained less than 5% of applied eye dose because of drainage and lacrimation and low retention exposure to the absorption surface.Non ophthalmic nanoparticles of 5-FU using polymers such as poly(butylcyanoacrylate), 2) poly(lactic acid), poly-(lactide-co-glycolide)3) and chitosan [4][5][6] have been reported, but investigators have not explored the application of 5-FU loaded nanoparticles (DNPs) for the treatment of ocular application.Ocular therapy by 5-FU can be improved and its toxicity diminished by facilitating the specific accumulation in the tumor infected regions with prolonged exposure of the cells to this agent. In this sense, the association of anticancer drugs to delivery systems has been an interesting approach for selectively delivering these agents and, at the same time, reducing their toxicity. Another benefit of 5-FU loaded nanoparticles in the targeted tissues could be an improvement in its pharmacokinetics profile.Polymeric nanoparticulate systems have been evaluated as ocular drug delivery to enhance the absorption of therapeutic drugs to improve bioavailability, reduce side effects, and sustain intraocular drug levels.7) In addition, chitosan (CH) is suitable for fabrication of nanogel/nanoparticles of 5-FU because it is positively charged, making it able to adhere to the negatively charged ocular surface and is soluble in diverse acids and able to interact with polyanions to form complex and nanogel. The cornea and conjunctiva have negative charge so the mucoadhesive polymer might interact intimately with these structures and increase the concentration and residence time of the associated drug at the disease site. Among the mucoadhesive polymers, chitosan exhibits several favourable properties, such as biodegradability, nontoxicity, biocompatibility, and mucoadhesiveness. In fact, an ionic interaction between the positively charged amino groups of CH and negatively charged sialic acid residues in mucus has been proposed as the mucoadhesion mechanism. This unique combination of properties makes it a novel versat...

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Formulation and investigation of 5-FU nanoparticles with factorial design-based studies

Cited by 68 publications

References 17 publications

Development and validation of an HPLC method for the determination of fluorouracil in polymeric nanoparticles

Development and validation of an HPLC method for the determination of fluorouracil in polymeric nanoparticles

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

Chitosan Nanoparticles of 5-Fluorouracil for Ophthalmic Delivery: Characterization, in-Vitro and in-Vivo Study

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