Comparison of Enhanced Solubility Profile Analysis of Thermodynamic Parameters and Pharmacokinetic Profile Related to Tamoxifen Citrate Solubilisation

Laboni Mondal, Biswajit Mukherjee, Shreyasi Chakraborty, Sanchari Bhattacharya, Iman Ehsan, Soma Sengupta and Murari M Pal
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Murari M Pal: Department of Pharmaceutical Technology, Jadavpur University, India

Novel Approaches in Drug Designing & Development, 2018, vol. 3, issue 5, 120-127

Abstract: The aim of this study was to investigate the improvement of solubility of a poorly water soluble drug tamoxifen citrate (TC) by various methods such as cosolvency, micellisation, and complexation. Cosolvents (ethanol, polyethylene glycol-400), surfactants [polyoxyethylene sorbitan monooleate (Tween-80), poloxamer-407 and poloxamer-188], and cyclodextrins [β-cyclodextrin (BCD) and hydroxypropyl-β-cyclodextrin (HPBCD)] were used as solubilizing agents in this study. Solubility improvement approaches showed variable degrees of solubility improvement of TC. Among the solubilizing agents used, the modified β-cyclodextrin was found to be the most effective. The solubility of TC was enhanced to 6.31 mmolL-1 in water (about 7.1 fold solubility improvement) using 0.05% m/v hydroxy propyl-β-cyclodextrin. Different thermodynamic parameters, enthalpy and entropy, were analyzed for solubility enhancement of TC with different cyclodextrins which showed enthalpy not the entropy was the driving force for TC solubilisation. The less positive enthalpy of BCD complexation than HPBCD complexation signifies the higher solubilising efficacy of HPBCD. Pharmacokinetic study was performed using HPBCD as solubility enhancer at its optimized concentration which also resulted in improved bioavailability when compared to the bioavailability obtained with free tamoxifen.

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Date: 2018
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Persistent link: https://EconPapers.repec.org/RePEc:adp:jnapdd:v:3:y:2018:i:5:p:120-127

DOI: 10.19080/NAPDD.2018.03.555624

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