Measurements of binding thermodynamics in drug discovery

Holdgate, Geoffrey A.; Ward, Walter H.J.

doi:10.1016/s1359-6446(05)03610-x

Cited by 186 publications

(136 citation statements)

References 61 publications

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“…It has been extensively used to investigate the thermal changes caused by the incorporation of the drugs into the phospholipid bilayers (6,(43)(44)(45)(46)(47). We used this method to show the incorporation of VLB within DSPE-PEG 2000 micelles.…”

Section: Characterization Of Vlb-ssm Formulation Using Differential Smentioning

confidence: 99%

A New Lipid-Based Nano Formulation of Vinorelbine

et al. 2014

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Abstract. Vinorelbine (VLB) is a semi-synthetic Vinca alkaloid which is currently used in treatment of different cancer types mainly advanced breast cancer (ABC) and advanced/metastatic non-small cell lung cancer (NSCLC). However, its marketed formulation has been reported to have serious side effects, such as granulocytopenia, which is the major dose-limiting toxicity. Other unwanted effects include venous discoloration and phlebitis proximal to the site of injection, as well as localized rashes and urticaria, blistering, and skin sloughing. Our long-term aim in synthesizing a novel nanomicellar vinorelbine formulation is to reduce or even eliminate these side effects and increase drug activity by formulating the drug in a lipid-based system as a nanomedicine targeted to the site of action. To this end, the purpose of this study was to prepare, characterize, and determine the in vitro efficacy of vinorelbine-loaded sterically stabilized, biocompatible, and biodegradable phospholipid nanomicelles (SSM; size, ∼15 nm). Our results indicated that vinorelbine incorporate at high quantities and within the interface between the core and palisade sections of the micelles. Incorporation ratio of drug within sterically stabilized micelles increased as the total amount of drug in the system increased, and no drug particles were formed at the highest drug concentrations tested. The nanomicellar formulation of vinorelbine was ∼6.7-fold more potent than vinorelbine dissolved in DMSO on MCF-7 cell line. Collectively, these data indicate that vinorelbine-loaded SSM can be developed as a new, safe, stable, and effective nanomedicine for the treatment of breast and lung cancers.

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Section: Characterization Of Vlb-ssm Formulation Using Differential Smentioning

confidence: 99%

A New Lipid-Based Nano Formulation of Vinorelbine

et al. 2014

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“…Heat capacity, (Δ ), which is influenced by the number of accessible energy state, was determined over the range temperature of studies. As an important parameter, it controls the magnitude of Δ 0 and Δ 0 [59]. Considering temperature dependence of Δ 0 , an equation can be written to represent nonzero temperature independent Δ : The Δ value was calculated in a simple manner, as…”

Section: Estimation Of Thermodynamic Parametermentioning

confidence: 99%

Adsorption of Brilliant Green onto Luffa Cylindrical Sponge: Equilibrium, Kinetics, and Thermodynamic Studies

Esan

Abiola

Owoyomi

et al. 2014

ISRN Physical Chemistry

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The sponge of Luffa cylindrical (LFC), a fibrous material, was employed as adsorbent for the removal of Brilliant Green (BGD) from aqueous effluent via batch studies. The optimum removal of BGD was found at pH 8.2 and the equilibrium was attained within 3 hours. The kinetic data are analyzed using several models including pseudo-first-order, pseudo-second-order, power function, simple elovich, intraparticle diffusion, and liquid film diffusion. The fitting of the different kinetics models to the experimental data, tested by error analysis, using the linear correlation coefficient ( 2 ) and chi-square analysis ( 2 ), showed that the mechanism of adsorption process was better described by pseudo-second-order and power function kinetic models. The equilibrium isotherm data were analyzed using Langmuir, Freundlich, and Temkin models and the sorption process was described by the Langmuir isotherm with maximum monolayer adsorption capacity of 18.2 mg/g at 303 K. The thermodynamic properties Δ 0 , Δ 0 , and Δ 0 showed that adsorption of BGD onto LFC was spontaneous, endothermic, and feasible within the temperature range of 303-313 K.

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“…This universal property is independent of molecule size and so that all chemical and biochemical reactions can be studied [180]. This includes the formation of complexes between proteins, DNA, lipids or low molecular weight biomolecules, which are mostly based on non-covalent bonds.…”

Section: Isothermal Titration Calorimetrymentioning

confidence: 99%