Abstract
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 × 10−2), followed by that in polyethylene glycol-400 (3.32 × 10−3) > Transcutol® (2.89 × 10−3) > ethylene glycol (1.64 × 10−3) > propylene glycol (1.47 × 10−3) > H2O (7.70 × 10−4) > ethyl acetate (5.44 × 10−4) > ethanol (1.80 × 10−4) > isopropyl alcohol (1.32 × 10−4) > 1-butanol (1.07 × 10−4) 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.
Highlights
Temozolomide (TMZ; CAS number: 85622-93-1; molar mass: 194.15 g mol−1; molecular formula: C6H6N6O2; Figure 1) is indicated in brain tumors such as glioblastoma and malignant glioma as an oral adjuvant chemotherapy agent [1,2,3]
Many approaches for the delivery of TMZ, including complexation [8], niosomes [6], solid lipid nanoparticles [9] lipid-based nanoparticles [1], nanomicelles [10], and chitosan engineered PAMAM dendrimers, [11] have previously been described for the augmentation of drug dissolution and bioavailability
Pure TMZ and the equilibrated sample exhibited mass loss at approximately 473.13 K and 475.22 K, respectively (Figure 2C,D). Results for both the samples demonstrated that TGA signals for pure TMZ and the equilibrated sample were analogous to each other
Summary
Temozolomide (TMZ; CAS number: 85622-93-1; molar mass: 194.15 g mol−1; molecular formula: C6H6N6O2; Figure 1) is indicated in brain tumors such as glioblastoma and malignant glioma as an oral adjuvant chemotherapy agent [1,2,3]. TMZ is usually prescribed by practitioners because of its comparatively exceptional cytotoxic characteristics for cancer cells [4]. TMZ is a prodrug and its metabolite alkylates nucleophiles (i.e., DNA) and induces cell death [5]. Many approaches for the delivery of TMZ, including complexation [8], niosomes [6], solid lipid nanoparticles [9] lipid-based nanoparticles [1], nanomicelles [10], and chitosan engineered PAMAM dendrimers, [11] have previously been described for the augmentation of drug dissolution and bioavailability. The solubility of TMZ in H2O (2–4 mg/mL) and ethanol (EtOH, 0.4–0.6 mg/mL) is reported elsewhere [12]; the solubility of TMZ in solvents such as Transcutol® (TC), propylene glycol (PG), isopropyl alcohol (IPA), ethylene glycol (EG), polyethylene glycol-400 (PEG-400), 1-butanol (1-BuOH), dimethyl sulfoxide (DMSO), and ethyl acetate (EA) has not been described far
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