Binary and Ternary Complexes of Arteether β-CD - Characterization, Molecular Modeling and in Vivo Studies

Chadha, Renu; Gupta, Shreya; Pathak, Natasha; Shukla, Geeta; Jain, Dharamvir Singh; Pissurlenkar, Raghuvir R. S.; Coutinho, Evans C.

doi:10.4236/pp.2011.23030

Cited by 8 publications

(3 citation statements)

References 26 publications

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“…We cleaned the obtained supernatants by filtering them through membrane filters of 0.2 microns and analyzing them with a UV-vis spectrophotometer (Jasco, V-630, Tokyo, Japan) to remove any undissolved solids. According to (1) , (2) , the binding constant (K b ) of OTV:M-CD-ICs and OTV:S-CD-ICs can be determined by the slope and intercept of the straight line of the phase solubility diagram [17] :

…”

Section: Methodsmentioning

confidence: 99%

A novel and water-soluble material for coronavirus inactivation from oseltamivir in the cavity of methyl and sulfated-β-cyclodextrins through inclusion complexation

Rajamohan

Mohandoss²,

Ashokkumar³

et al. 2022

Journal of Pharmaceutical and Biomedical Analysis

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…”

Section: Methodsmentioning

confidence: 99%

A novel and water-soluble material for coronavirus inactivation from oseltamivir in the cavity of methyl and sulfated-β-cyclodextrins through inclusion complexation

Rajamohan

Mohandoss²,

Ashokkumar³

et al. 2022

Journal of Pharmaceutical and Biomedical Analysis

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“…Obtained powders dried at room temperature, sieved through the mesh (80#) and stored in a desiccator for subsequent use. 15 .…”

Section: Kneading Methods (Kn) 1314mentioning

confidence: 99%

Dissolution Enhancement of Clarithromycin Using Ternary Cyclodextrin Complexation

Mulimani¹,

Goswami²,

Rughwani³

2018

IJPRS

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The research work presented is new and never been done earlier. Clarithromycin, a semi-synthetic macrolide antibiotic derived from erythromycin having low solubility and high permeability falling in class-II of Biopharmaceutical Classification System (BCS). The drug is practically insoluble in water exhibiting dissolution rate limited absorption. The objective of the research work increasing in the solubility, release properties of Clarithromycin and improve the bioavailability of Clarithromycin using ternary inclusion complex with Beta Cyclodextrin. The research work includes developing a multicomponent system comprising of macrolide: Clarithromycin, Beta-cyclodextrin and a polymer Soluplus to attain enhanced solubility of Clarithromycin. The inclusion complexes were prepared by slurry evaporation and kneading method using different proportions of B-CD'S and Soluplus. The complexes were characterized by solubility, drug content uniformity, dissolution rate, similarity factor analysis and by HPLC. The ternary inclusion complexes prepared by the kneading method were evaluated for solubility enhancement and improved dissolution rate. Formulations with a Soluplus concentration of 20% w/w of drug content and solvent ratio of 70:30 (water: ethanol) showed more than 80% of drug release at the end of one hour.

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“…The structural states and the corresponding energies were sampled from the trajectories after every 10 picoseconds. [ 29 30 31 ]…”

Section: Methodsmentioning

confidence: 99%

Characterization of pioglitazone cyclodextrin complexes: Molecular modeling to in vivo evaluation

et al. 2016

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Aims:The objective of present study was to study the influence of different β-cyclodextrin derivatives and different methods of complexation on aqueous solubility and consequent translation in in vivo performance of Pioglitazone (PE).Material and Methods:Three cyclodextrins: β-cyclodextrin (BCD), hydroxypropyl-β-cyclodextrin (HPBCD) and Sulfobutylether-7-β-cyclodextrin (SBEBCD) were employed in preparation of 1:1 Pioglitazone complexes by three methods viz. co-grinding, kneading and co-evaporation. Complexation was confirmed by phase solubility, proton NMR, Fourier Transform Infrared spectroscopy, Differential Scanning Calorimetry (DSC) and X-Ray diffraction (XRD). Mode of complexation was investigated by molecular dynamic studies. Pharmacodynamic study of blood glucose lowering activity of PE complexes was performed in Alloxan induced diabetic rat model.Results:Aqueous solubility of PE was significantly improved in presence of cyclodextrin. Apparent solubility constants were observed to be 254.33 M–1 for BCD-PE, 737.48 M–1 for HPBCD-PE and 5959.06 M–1 for SBEBCD-PE. The in silico predictions of mode of inclusion were in close agreement with the experimental proton NMR observation. DSC and XRD demonstrated complete amorphization of crystalline PE upon inclusion. All complexes exhibited >95% dissolution within 10 min compared to drug powder that showed <40% at the same time. Marked lowering of blood glucose was recorded for all complexes.Conclusion:Complexation of PE with different BCD significantly influenced its aqueous solubility, improved in vitro dissolution and consequently translated into enhanced pharmacodynamic activity in rats

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Binary and Ternary Complexes of Arteether β-CD - Characterization, Molecular Modeling and in Vivo Studies

Abstract: The purpose of the present work is to improve the antimalarial activity of arteether through enhancing its solubility subsequently bioavailability by incorporating the drug into the cyclodextrins cavity.

Cited by 8 publications

References 26 publications

A novel and water-soluble material for coronavirus inactivation from oseltamivir in the cavity of methyl and sulfated-β-cyclodextrins through inclusion complexation

A novel and water-soluble material for coronavirus inactivation from oseltamivir in the cavity of methyl and sulfated-β-cyclodextrins through inclusion complexation

Dissolution Enhancement of Clarithromycin Using Ternary Cyclodextrin Complexation

Characterization of pioglitazone cyclodextrin complexes: Molecular modeling to in vivo evaluation

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