Formulation and characterization of Paclitaxel, 5-FU and Paclitaxel + 5-FU microspheres

Gupte, Anshul; Ciftci, Kadriye

doi:10.1016/j.ijpharm.2004.02.023

Cited by 56 publications

(34 citation statements)

References 21 publications

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“…The concentration range of free 5-FU was selected based on preliminary experiments, in which increasing concentrations of 5-drug from 0.01 µM to 1 mM were tested in culture. Those drug concentrations were in accordance with data reported in the literature [33][34][35]. The administration of 5-FU 10 μM in solution produced a decrease of the percentage of viability in MCF7 cells, which was between 91 ± 8% and 43 ± 3% after 3 days of incubation.…”

Section: Cell Culture Studiessupporting

confidence: 91%

In Vitro and In Vivo Evaluation of a Folate-Targeted Copolymeric Submicrohydrogel Based on N-Isopropylacrylamide as 5-Fluorouracil Delivery System

et al. 2011

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Folate-targeted poly[(p-nitrophenyl acrylate)-co-(N-isopropylacrylamide)] nanohydrogel (F-SubMG) was loaded with 5-fluorouracil (5-FU) to obtain low (16.3 ± 1.9 μg 5-FU/mg F-SubMG) and high (46.8 ± 3.8 μg 5-FU/mg F-SubMG) load 5-FU-loaded F-SubMGs. The complete in vitro drug release took place in 8 h. The cytotoxicity of unloaded F-SubMGs in MCF7 and HeLa cells was low; although it increased for high F-SubMG concentration. The administration of 10 μM 5-FU by 5-FU-loaded F-SubMGs was effective on both cellular types. Cell uptake of F-SubMGs took place in both cell types, but it was higher in HeLa cells because they are folate receptor positive. After subcutaneous administration (28 mg 5-FU/kg b.w.) in Wistar rats, F-SubMGs were detected at the site of injection under the skin. Histological studies indicated that the OPEN ACCESSPolymers 2011, 3 1108 F-SubMGs were surrounded by connective tissue, without any signs of rejections, even 60 days after injection. Pharmacokinetic study showed an increase in MRT (mean residence time) of 5-FU when the drug was administered by drug-loaded F-SubMGs.

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Section: Cell Culture Studiessupporting

confidence: 91%

In Vitro and In Vivo Evaluation of a Folate-Targeted Copolymeric Submicrohydrogel Based on N-Isopropylacrylamide as 5-Fluorouracil Delivery System

et al. 2011

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“…Diversos trabalhos comprovaram o aumento da efi cácia e a redução da toxicidade de substâncias bioativas de origem natural ou sintética, administrados em lipossomas (Ratner, 2002), sistemas nanoparticulados (Feng et al, 2004;Berkland et al, 2002) ou micropartículas (Gupte;Ciftci, 2004;Ribeiro-Costa et al, 2004). Relatos recentes demonstram a atividade antitumoral do taxol (Gupte;Ciftci, 2004) e do ácido úsnico (Cladonia substellata) em microesferas (Ribeiro-Costa et al, 2004), da lectina de Cratylia mollis encapsulada em lipossomas (Andrade et al, 2004), de xantonas (Teixeira et al, 2005), da doxorrubicina em nanopartículas (Barraud et al, 2005) e 5-fl uorouracil em lipossomas (Jin et al, 2005), atividade antiparasitária do praziquantel em lipossomas (Mourão et al, 2005), atividade antibiótica da vancomicina em micropartículas (Le Ray et al, 2005) e anfotericina B em lipossomas (Bellocchio et al, 2005), atividade hipoglicemiante da insulina em micropartículas (Kim et al, 2005) e anti-estrógenos em lipossomas e nanopartículas para tratamento do câncer de mama (Maillard et al, 2005;Memisoglu-Bilensoy et al, 2005).…”

Section: Toxicidade E Viabilização Da Biodisponibilização Da Dctnunclassified

Uma revisão das atividades biológicas da trans-desidrocrotonina, um produto natural obtido de Croton cajucara

Costa¹,

Magalhães²,

Gomes³

et al. 2007

Rev. bras. farmacogn.

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RESUMO:Croton cajucara Beth (Euphorbiaceae) uma espécie medicinal nativa da região Amazônica do Brasil, onde é vulgarmente conhecida como 'sacaca', representa um recurso terapêutico efi caz no tratamento e cura de várias doenças. O metabólito majoritário transdesidrocrotonina (DCTN), isolado das cascas do caule desta planta, encontra-se correlacionado com grande parte das propriedades medicinais da sacaca. Este artigo de revisão, descreve os resultados fi toquímicos e farmacológicos que foram realizados com o diterpeno do tipo clerodano DCTN, bem como seus derivados semi-sintéticos. Adicionalmente, apresenta perspectivas para a biodisponibilização deste protótipo de fármaco em nanosistemas. Unitermos:Croton cajucara, trans-desidrocrotonina, DCTN, fi toquímica, atividade biológica, nanobiotecnologia.ABSTRACT: "A review of the biologic activities of trans-dehydrocrotonin, a natural product obtained from Croton cajucara". Croton cajucara Beth (Euphorbiaceae) is a plant found in the Amazonian Region of North Brazil, where it is popularly known as sacaca. The major secondary metabolite, trans-dehydrocrotonin (DCTN) a clerodane-type diterpene, isolated from the stem bark is a chief bioactive compound of Croton cajucara. This review describes results of extensive pharmacological studies of DCTN, as well as its semi-synthetic derivatives, and also presents insights into the use of DCTN as a therapeutic agent and some potential advantages of its incorporation in drug delivery systems.

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“…It is a fluorinated analog of pyrmidine base uracil, which is metabolized intracellulary to its active form, fluorodeoxyuridine monophophate (FdUMP). The active form inhibits DNA synthesis by inhibiting the normal production of thymidine (Gupte & Ciftci, 2004).…”

Section: Introductionmentioning

confidence: 99%

Preparation of ferric ion crosslinked acrylamide grafted poly (vinyl alcohol)/sodium alginate microspheres and application in controlled release of anticancer drug 5-fluorouracil

Şanlı

Olukman

2013

Drug Delivery

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Ionically crosslinked microspheres of acrylamide (AAm) grafted poly (vinyl alcohol) (PVA)/ sodium alginate (NaAlg) were prepared by crosslinking with FeCl 3 and 5-fluorouracil (5-FU), which is an anticancer drug and was successfully encapsulated into the microspheres. The graft copolymer (PVA-g-PAAm) was characterized by using Fourier transform infrared spectroscopy (FTIR) and elemental analysis. The prepared microspheres were characterized by FTIR and scanning electron microscopy (SEM). Microspheres were also characterized by particle diameter, equilibrium swelling values and release profiles. The release studies were carried out at three pH values 1.2, 6.8 and 7.4, respectively, each for 2 h. The effects of preparation conditions as PVA-g-PAAm/NaAlg ratio, drug/polymer ratio, crosslinker concentration and exposure time to FeCl 3 on the release of 5-FU were investigated for 6 h at 37 C. The highest 5-FU release was found to be as 99.57% (w/w) at the end of 6 h for PVA-g-PAAm/NaAlg ratio of 1:4 (w/w), drug/ polymer ratio of 1:8 (w/w), crosslinker concentration of 0.05 M and exposure time of 10 min. The release results were also supported by the swelling measurements of the microspheres. Release kinetics was described by Fickian and non-Fickian approaches.

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Formulation and characterization of Paclitaxel, 5-FU and Paclitaxel + 5-FU microspheres

Cited by 56 publications

References 21 publications

In Vitro and In Vivo Evaluation of a Folate-Targeted Copolymeric Submicrohydrogel Based on N-Isopropylacrylamide as 5-Fluorouracil Delivery System

In Vitro and In Vivo Evaluation of a Folate-Targeted Copolymeric Submicrohydrogel Based on N-Isopropylacrylamide as 5-Fluorouracil Delivery System

Uma revisão das atividades biológicas da trans-desidrocrotonina, um produto natural obtido de Croton cajucara

Preparation of ferric ion crosslinked acrylamide grafted poly (vinyl alcohol)/sodium alginate microspheres and application in controlled release of anticancer drug 5-fluorouracil

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