Pharmacokinetics, tissue distribution and anti-tumour efficacy of paclitaxel delivered by polyvinylpyrrolidone solid dispersion

Liu, Xiangrui; Sun, Jiabei; Chen, Xiaomei; Wang, Shanshan; Scott, Hannah; Zhang, Xuan; Zhang, Qiang

doi:10.1111/j.2042-7158.2012.01471.x

Cited by 15 publications

(3 citation statements)

References 21 publications

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“…These studies support our current findings that PVP is a better choice for holding PTX in self-assembly grooves. PVP has been used as a solid dispersion for PTX and docetaxel 52 , 53 . In addition, Sharma et al 48 also developed polyvinylpyrrolidone nanoparticle-encapsulated taxol.…”

Section: Discussionmentioning

confidence: 99%

Development of polyvinylpyrrolidone/paclitaxel self-assemblies for breast cancer

Chowdhury

Nagesh

Khan

et al. 2018

Acta Pharmaceutica Sinica B

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The goal of this investigation was to develop and demonstrate a polymer/paclitaxel self-assembly (PTX-SA) formulation. Polymer/PTX-SAs were screened based on smaller size of formulation using dynamic light scattering analysis. Additionally, fluorescence microscopy and flow cytometry studies exhibited that polyvinylpyrrolidone (PVP)-based PTX-SAs (PVP/PTX-SAs) had superior cellular internalization capability in MCF7 and MDA-MB-231 breast cancer cells. The optimized PVP/PTX-SAs exhibited less toxicity to human red blood cells indicating a suitable formulation for reducing systemic toxicity. The formation of PVP and PTX self-assemblies was confirmed using fluorescence quenching and transmission electron microscopy which indicated that the PVP/PTX-SAs were spherical in shape with an average size range of 53.81 nm as detected by transmission electron microscopy (TEM). FTIR spectral analysis demonstrates incorporation of polymer and paclitaxel functional groups in PVP/PTX-SAs. Both proliferation (MTS) and clonogenic (colony formation) assays were used to validate superior anticancer activity of PVP/PTX-SAs in breast cancer cells over paclitaxel. Such superior anticancer activity was also demonstrated by downregulation of the expression of pro-survival protein (Bcl-xL), upregulation of apoptosis-associated proteins (Bid, Bax, cleaved caspase 7, and cleaved PARP) and β-tubulin stabilization. These results support the hypothesis that PVP/PTX-SAs improved paclitaxel delivery to cancer cells.

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Section: Discussionmentioning

confidence: 99%

Development of polyvinylpyrrolidone/paclitaxel self-assemblies for breast cancer

Chowdhury

Nagesh

Khan

et al. 2018

Acta Pharmaceutica Sinica B

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“…36,37 PVP is a water-soluble and biocompatible polymer widely used in pharmaceuticals and cosmetics. 38,39 In a typical synthesis of PVP-coated GaPBNPs, an aqueous Ga(NO 3 ) 3 solution (1 mM, 50 mL) containing 200 mg of PVP (average MW = 8000) was slowly added to an aqueous K 4 [Fe(CN) 6 ] solution (1 mM, 50 mL) under vigorous stirring for 4 h, resulting in a slight color change to pale yellow. The product was isolated by centrifugation and purified by repeated resuspension of the product in water followed by centrifugation (see the SI).…”

mentioning

confidence: 99%

Gallium Analogue of Soluble Prussian Blue KGa[Fe(CN)₆]·nH₂O: Synthesis, Characterization, and Potential Biomedical Applications

et al. 2013

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The gallium analogue of the soluble Prussian blue with the formula KGa[Fe(CN)6]·nH2O is synthesized and structurally characterized. A simple aqueous synthetic procedure for preparing nanoparticles of this novel coordination polymer is reported. The stability, in vitro ion exchange with ferrous ions, cytotoxicity, and cellular uptake of such nanoparticles coated with poly(vinylpyrrolidone) are investigated for potential applications of delivering Ga(3+) ions into cells or removing iron from cells.

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“…21 ICR mice were randomly divided into ten groups (five groups for treatment with the CLA-PTX solution and another five groups for treatment with the CLA-PTX microemulsion), containing ten mice each. All animals were fasted for 12 hours before intravenous administration of the study formulations.…”

Section: Acute Toxicitymentioning

confidence: 99%

Antitumor efficacy of a novel CLA-PTX microemulsion against brain tumors: in vitro and in vivo findings

Li¹,

Yang²,

Li³

et al. 2012

IJN

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Background: Considering the observations that linoleic acid conjugated with paclitaxel (CLA-PTX) possesses antitumor activity against brain tumors, is able to cross the blood-brain barrier, but has poor water solubility, the purpose of this study was to prepare a novel CLA-PTX microemulsion and evaluate its activity against brain tumors in vitro and in vivo. Methods: The in vitro cytotoxicity of a CLA-PTX microemulsion was investigated in C6 glioma cells. The in vivo antitumor activity of the CLA-PTX microemulsion was evaluated in tumorbearing nude mice and rats. The pharmacokinetics of the CLA-PTX microemulsion were investigated in rats, and its safety was also evaluated in mice. Results: The average droplet size of the CLA-PTX microemulsion was approximately 176.3 ± 0.8 nm and the polydispersity index was 0.294 ± 0.024. In vitro cytotoxicity results showed that the IC 50 of the CLA-PTX microemulsion was 1.61 ± 0.83 µM for a C6 glioma cell line, which was similar to that of free paclitaxel and CLA-PTX solution (P . 0.05). The antitumor activity of the CLA-PTX microemulsion against brain tumors was confirmed in our in vivo C6 glioma tumor-bearing nude mice as well as in a rat model. In contrast, Taxol ® had almost no significant antitumor effect in C6 glioma tumor-bearing rats, but could markedly inhibit growth of C6 tumors in C6 glioma tumor-bearing nude mice. The pharmacokinetic results indicated that CLA-PTX in solution has a much longer circulation time and produces higher drug plasma concentrations compared with the CLA-PTX microemulsion. The results of the acute toxicity study showed that the LD 50 of CLA-PTX solution was 103.9 mg/kg. In contrast, the CLA-PTX microemulsion was well tolerated in mice when administered at doses up to 200 mg/kg. Conclusion: CLA-PTX microemulsion is a novel formulation with significant antitumor efficacy in the treatment of brain tumors, and is safer than CLA-PTX solution.

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Pharmacokinetics, tissue distribution and anti-tumour efficacy of paclitaxel delivered by polyvinylpyrrolidone solid dispersion

Abstract: These results suggest that the PSD, a CrEL-free formulation, is a promising approach to increase the safety and efficacy of paclitaxel.

Cited by 15 publications

References 21 publications

Development of polyvinylpyrrolidone/paclitaxel self-assemblies for breast cancer

Development of polyvinylpyrrolidone/paclitaxel self-assemblies for breast cancer

Gallium Analogue of Soluble Prussian Blue KGa[Fe(CN)₆]·nH₂O: Synthesis, Characterization, and Potential Biomedical Applications

Antitumor efficacy of a novel CLA-PTX microemulsion against brain tumors: in vitro and in vivo findings

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Pharmacokinetics, tissue distribution and anti-tumour efficacy of paclitaxel delivered by polyvinylpyrrolidone solid dispersion

Abstract: These results suggest that the PSD, a CrEL-free formulation, is a promising approach to increase the safety and efficacy of paclitaxel.

Cited by 15 publications

References 21 publications

Development of polyvinylpyrrolidone/paclitaxel self-assemblies for breast cancer

Development of polyvinylpyrrolidone/paclitaxel self-assemblies for breast cancer

Gallium Analogue of Soluble Prussian Blue KGa[Fe(CN)6]·nH2O: Synthesis, Characterization, and Potential Biomedical Applications

Antitumor efficacy of a novel CLA-PTX microemulsion against brain tumors: in vitro and in vivo findings

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Product

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Gallium Analogue of Soluble Prussian Blue KGa[Fe(CN)₆]·nH₂O: Synthesis, Characterization, and Potential Biomedical Applications