Enhanced solubility and stability of PEGylated liposomal paclitaxel: In vitro and in vivo evaluation

Tao, Yang; Cui, Fu De; Choi, Min Koo; Cho, Jei Won; Chung, Suk Jae; Shim, Chang-Su; Kim, Dae Duk

doi:10.1016/j.ijpharm.2007.02.011

Cited by 364 publications

(201 citation statements)

References 27 publications

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“…Hence, it has been considered for further physicochemical characterization and different in vitro and in vivo pharmacokinetic studies. DTX is an approved drug to tumor of brain in combination therapy, but its entry to the brain is prevented by BBB due to its different physiochemical and pharmacological factors (Chen et al, 2004;van Rooy et al, 2011).We have tried to deliver DTX by incorporating it into the liposomes, based on the hypothesis that the nanosize of the vesicle may help to deliver DTX and the use of nanoliposomes may overcome the solubility problem of DTX and reported toxicity of Taxotere Õ , the marketed formulation (Yang et al, 2007;Yousefi et al, 2009;Costantino & Boraschi, 2012). In this work we have formulated nanoliposomes of DTX using SPC as lipid component, and CHL as a stabilizer of lipid membranes.…”

Section: Discussionmentioning

confidence: 99%

Successful delivery of docetaxel to rat brain using experimentally developed nanoliposome: a treatment strategy for brain tumor

et al. 2017

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Docetaxel (DTX) is found to be very effective against glioma cell in vitro. However, in vivo passage of DTX through BBB is extremely difficult due to the physicochemical and pharmacological characteristics of the drug. No existing formulation is successful in this aspect. Hence, in this study, effort was made to send DTX through blood-brain barrier (BBB) to brain to treat diseases such as solid tumor of brain (glioma) by developing DTX-loaded nanoliposomes. Primarily drug-excipients interaction was evaluated by FTIR spectroscopy. The DTX-loaded nanoliposomes (L-DTX) were prepared by lipid layer hydration technique and characterized physicochemically. In vitro cellular uptake in C6 glioma cells was investigated. FTIR data show that the selected drug and excipients were chemically compatible. The unilamellar vesicle size was less than 50 nm with smooth surface. Drug released slowly from L-DTX in vitro in a sustained manner. The pharmacokinetic data shows more extended action of DTX from L-DTX in experimental rats than the free-drug and Taxotere Õ . DTX from L-DTX enhanced 100% drug concentration in brain as compared with Taxotere Õ in 4 h. Thus, nanoliposomes as vehicle may be an encouraging strategy to treat glioma with DTX.

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Section: Discussionmentioning

confidence: 99%

Successful delivery of docetaxel to rat brain using experimentally developed nanoliposome: a treatment strategy for brain tumor

et al. 2017

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“…Preparation was done by injecting 1 mL of 10 % w/v of polyethylene glycol 10000 to the vesicular dispersions that was being stirred at 500 rpm slowly to ensure uniform coating of PEG around the vesicles (Minghuang et al 2009;Yang and Guangji 2008;Yang et al 2007). …”

Section: Statistical Analysis Of the Data And Optimizationmentioning

confidence: 99%

Factorial design studies of antiretroviral drug-loaded stealth liposomal injectable: PEGylation, lyophilization and pharmacokinetic studies

2015

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The aim of the present study was to formulate and evaluate the ritonavir-loaded stealth liposomes by using 3 2 factorial design and intended to delivered by parenteral delivery. Liposomes were prepared by ethanol injection method using 3 2 factorial designs and characterized for various physicochemical parameters such as drug content, size, zeta potential, entrapment efficiency and in vitro drug release. The optimization process was carried out using desirability and overlay plots. The selected formulation was subjected to PEGylation using 10 % PEG-10000 solution. Stealth liposomes were characterized for the above-mentioned parameters along with surface morphology, Fourier transform infrared spectrophotometer, differential scanning calorimeter, stability and in vivo pharmacokinetic studies in rats. Stealth liposomes showed better result compared to conventional liposomes due to effect of PEG-10000. The in vivo studies revealed that stealth liposomes showed better residence time compared to conventional liposomes and pure drug solution. The conventional liposomes and pure drug showed dose-dependent pharmacokinetics, whereas stealth liposomes showed long circulation half-life compared to conventional liposomes and pure ritonavir solution. The results of statistical analysis showed significance difference as the p value is (\0.05) by one-way ANOVA. The result of the present study revealed that stealth liposomes are promising tool in antiretroviral therapy.

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“…8 During the past few years, there has been a great pace in using solubility enhancement techniques for the improvement of the dissolution rate and subsequently the bioavailability of poorly water soluble drugs. Several techniques like nanomaterialization, 9 salt formation, 10 hydrotropy, 11 liposome formation, 12 liquisolid compaction, 13 solid dispersion, 14 SMEDDS, 15 and many other significant techniques have been reported for improving bioavailability of poorly water soluble drugs of class BCS-II and BCS-IV. Solid dispersion (SD) is one of the most promising strategies to improve the dissolution properties and bioavailability of poorly water-soluble drugs where drug materials are dispersed in an inert carrier.…”

Section: Introductionmentioning

confidence: 99%

Improved Dissolution and Bioavailability of Eprosartan Mesylate Formulated as Solid Dispersions using Conventional Methods

Dangre¹,

Godbole²,

Ingale³

et al. 2016

IJPER

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Background: Eprosartan mesylate (EM) is a poorly aqueous soluble drug belonging to BCS-class II suffers from low bioavailability (13%). The present study involves an effort for improving dissolution and thus the bioavailability of EM using solid dispersion approach. Methods: Solid dispersion (SD) was prepared by melting, solvent evaporation and kneading method using different ratios of drug and polymers (PEG-4000, Eudragit E-100, PVP K-30, Poloxamer-407, and Eudragit L-100). Phase solubility study revealed highest solubility in PVP K-30 at 1:2 ratios. The solid state characterizations of selected solid dispersion formulation (SD-15) were performed by infrared spectroscopy, differential scanning calorimeter, X-ray diffraction study and scanning electron microscopy. In vitro dissolution was carried out in phosphate buffer (pH 7.4) at 50 rpm in 900 ml of volume. The in vivo pharmacokinetic study of selected formulation (SD-15) was carried out in male Wistar rats using non-compartment analysis by linear trapezoidal method after a single oral dose of 10 mg/kg of EM. Results: The solid state characterization revealed no such drug-polymer interactions and rapid transformation of crystalline drug in an amorphous state, which amplifies the aqueous solubility and hence the dissolution rate. The in vitro dissolution study of the dispersions prepared by PVP K-30 (1:2) was found to be 95.5% after 1 hr. In vivo pharmacokinetic study in Wistar rats showed significant improvement in oral bioavailability of EM in SD-15 with the 2.4 fold increments than the pure drug. Conclusion: The solid dispersion prepared using PVP K-30 by kneading method showed improved dissolution and bioavailability. Therefore, solid dispersion formulation can be sorted as a promising approach for improving the dissolution and bioavailability of Eprosartan mesylate.

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Enhanced solubility and stability of PEGylated liposomal paclitaxel: In vitro and in vivo evaluation

Cited by 364 publications

References 27 publications

Successful delivery of docetaxel to rat brain using experimentally developed nanoliposome: a treatment strategy for brain tumor

Successful delivery of docetaxel to rat brain using experimentally developed nanoliposome: a treatment strategy for brain tumor

Factorial design studies of antiretroviral drug-loaded stealth liposomal injectable: PEGylation, lyophilization and pharmacokinetic studies

Improved Dissolution and Bioavailability of Eprosartan Mesylate Formulated as Solid Dispersions using Conventional Methods

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