Thermodynamic Solubility Profile of Temozolomide in Different Commonly Used Pharmaceutical Solvents

The solubility parameters, and solution thermodynamics of temozolomide (TMZ) in 10 frequently used solvents were examined at five different temperatures. The maximum mole fraction solubility of TMZ was ascertained in dimethyl sulfoxide (1.35 × 10<sup>−2</sup>), followed by that in polyet...

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Main Authors: Abdul Ahad, Faiyaz Shakeel, Mohammad Raish, Ajaz Ahmad, Yousef A. Bin Jardan, Fahad I. Al-Jenoobi, Abdullah M. Al-Mohizea
Format: Article
Language:English
Published: MDPI AG 2022-02-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/27/4/1437
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author Abdul Ahad
Faiyaz Shakeel
Mohammad Raish
Ajaz Ahmad
Yousef A. Bin Jardan
Fahad I. Al-Jenoobi
Abdullah M. Al-Mohizea
author_facet Abdul Ahad
Faiyaz Shakeel
Mohammad Raish
Ajaz Ahmad
Yousef A. Bin Jardan
Fahad I. Al-Jenoobi
Abdullah M. Al-Mohizea
author_sort Abdul Ahad
collection DOAJ
description The solubility parameters, and solution thermodynamics of temozolomide (TMZ) in 10 frequently used solvents were examined at five different temperatures. The maximum mole fraction solubility of TMZ was ascertained in dimethyl sulfoxide (1.35 × 10<sup>−2</sup>), followed by that in polyethylene glycol-400 (3.32 × 10<sup>−3</sup>) > Transcutol<sup>®</sup> (2.89 × 10<sup>−3</sup>) > ethylene glycol (1.64 × 10<sup>−3</sup>) > propylene glycol (1.47 × 10<sup>−3</sup>) > H<sub>2</sub>O (7.70 × 10<sup>−4</sup>) > ethyl acetate (5.44 × 10<sup>−4</sup>) > ethanol (1.80 × 10<sup>−4</sup>) > isopropyl alcohol (1.32 × 10<sup>−4</sup>) > 1-butanol (1.07 × 10<sup>−4</sup>) at 323.2 K. An analogous pattern was also observed for the other investigated temperatures. The quantitated TMZ solubility values were regressed using Apelblat and Van’t Hoff models and showed overall deviances of 0.96% and 1.33%, respectively. Apparent thermodynamic analysis indicated endothermic, spontaneous, and entropy-driven dissolution of TMZ in all solvents. TMZ solubility data may help to formulate dosage forms, recrystallize, purify, and extract/separate TMZ.
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spelling doaj.art-5162c4cbca7b460585e5cfb8c43716bc2023-11-23T21:23:58ZengMDPI AGMolecules1420-30492022-02-01274143710.3390/molecules27041437Thermodynamic Solubility Profile of Temozolomide in Different Commonly Used Pharmaceutical SolventsAbdul Ahad0Faiyaz Shakeel1Mohammad Raish2Ajaz Ahmad3Yousef A. Bin Jardan4Fahad I. Al-Jenoobi5Abdullah M. Al-Mohizea6Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Clinical Pharmacy, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, Saudi ArabiaThe solubility parameters, and solution thermodynamics of temozolomide (TMZ) in 10 frequently used solvents were examined at five different temperatures. The maximum mole fraction solubility of TMZ was ascertained in dimethyl sulfoxide (1.35 × 10<sup>−2</sup>), followed by that in polyethylene glycol-400 (3.32 × 10<sup>−3</sup>) > Transcutol<sup>®</sup> (2.89 × 10<sup>−3</sup>) > ethylene glycol (1.64 × 10<sup>−3</sup>) > propylene glycol (1.47 × 10<sup>−3</sup>) > H<sub>2</sub>O (7.70 × 10<sup>−4</sup>) > ethyl acetate (5.44 × 10<sup>−4</sup>) > ethanol (1.80 × 10<sup>−4</sup>) > isopropyl alcohol (1.32 × 10<sup>−4</sup>) > 1-butanol (1.07 × 10<sup>−4</sup>) at 323.2 K. An analogous pattern was also observed for the other investigated temperatures. The quantitated TMZ solubility values were regressed using Apelblat and Van’t Hoff models and showed overall deviances of 0.96% and 1.33%, respectively. Apparent thermodynamic analysis indicated endothermic, spontaneous, and entropy-driven dissolution of TMZ in all solvents. TMZ solubility data may help to formulate dosage forms, recrystallize, purify, and extract/separate TMZ.https://www.mdpi.com/1420-3049/27/4/1437Apelblat and Van’t Hoff modelssolubilitysolution thermodynamicstemozolomide
spellingShingle Abdul Ahad
Faiyaz Shakeel
Mohammad Raish
Ajaz Ahmad
Yousef A. Bin Jardan
Fahad I. Al-Jenoobi
Abdullah M. Al-Mohizea
Thermodynamic Solubility Profile of Temozolomide in Different Commonly Used Pharmaceutical Solvents
Molecules
Apelblat and Van’t Hoff models
solubility
solution thermodynamics
temozolomide
title Thermodynamic Solubility Profile of Temozolomide in Different Commonly Used Pharmaceutical Solvents
title_full Thermodynamic Solubility Profile of Temozolomide in Different Commonly Used Pharmaceutical Solvents
title_fullStr Thermodynamic Solubility Profile of Temozolomide in Different Commonly Used Pharmaceutical Solvents
title_full_unstemmed Thermodynamic Solubility Profile of Temozolomide in Different Commonly Used Pharmaceutical Solvents
title_short Thermodynamic Solubility Profile of Temozolomide in Different Commonly Used Pharmaceutical Solvents
title_sort thermodynamic solubility profile of temozolomide in different commonly used pharmaceutical solvents
topic Apelblat and Van’t Hoff models
solubility
solution thermodynamics
temozolomide
url https://www.mdpi.com/1420-3049/27/4/1437
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