No abstract

The solubilization behavior of paracetamol (PCT) in a diethylene glycol monoethyl ether (Transcutol)–water mixture at (298.15 to 333.15) K is not reported in literature so far. Therefore, attempts were made to investigate the solubilization behavior of PCT in monosolvents and various Transcutol–water mixtures at the temperature range of (298.15 to 333.15) K. The mole fraction solubility of PCT was determined by reported shake flask method. The experimental solubility data of PCT in monosolvents and various Transcutol–water mixtures were found to be correlated well with the modified Apelblat model with the correlation coefficients in the range of 0.996 to 0.999. The solubility of PCT was found to be increased significantly with the increase in temperature and mass fraction of Transcutol. The mole fraction solubility of PCT was found to be highest in pure Transcutol (0.111 at 298.15 K) as compared to water and other cosolvent mixtures. The positive values of enthalpies and entropies indicated that the dissolution of PCT is endothermic. Overall, these results indicated that Transcutol could be used as a physiologically compatible cosolvent to enhance the aqueous solubility of PCT. These preliminary studies could be useful in the formulation development of PCT especially in terms of liquid dosage forms.

Nanoemulsions have been formulated using a variety of pharmaceutically acceptable excipients. In many cases of dermal and transdermal nanoemulsions, the skin irritation or skin toxicity issues on human beings have not been considered which needs to be evaluated properly. In the last decade, much attention has been made in exploring new types of nanoemulsion-based drug delivery system for dermal and transdermal delivery of many hydrophobic compounds. This area of research would be very advantageous for formulation scientists in order to develop some nanoemulsion-based formulations for their commercial exploitation and clinical applications.

The aim of this study was to measure and correlate the temperature dependent solubility data of tadalafil (TDL) in water, ethanol, propylene glycol (PG), polyethylene glycol-400 (PEG-400), and Transcutol from (298.15 to 333.15) K at atmospheric pressure using the shake flask method. The experimental solubilities were regressed by Apelblat equation with a relative deviation in the range of (1.20 to 5.74) % in all solvents investigated at (298.15 to 333.15) K. The root mean square deviation between experimental and calculated solubility was observed less than 1.10 in all solvents investigated. The correlation coefficients in water, ethanol, PG, PEG-400, and Transcutol were observed in the range of 0.997 to 0.999. The solubility of TDL was found to be increased with an increase in temperature in all solvents investigated. The mole fraction solubility of TDL was found to be higher in PEG-400 (1.86•10 −2 at 298.15 K) and Transcutol (8.76•10 −3 at 298.15 K) as compared to water (5.74•10 −7 at 298.15 K), ethanol (1.77• 10 −4 at 298.15 K) and PG (4.1•10 −4 at 298.15 K).

The aim of present study was to measure and correlate the mole fraction solubility of olmesartan medoxomil (OLM) in six green solvents, namely, water, ethanol, propylene glycol (PG), polyethylene glycol-400 (PEG-400), ethylene glycol (EG), and Transcutol from (295.15 to 330.15) K at atmospheric pressure using the shake flask method. The experimental solubilities of OLM were correlated with the Apelblat equation. The root-mean-square deviations between experimental and calculated solubility were observed in the range of 3.360 × 10–8 to 0.013 × 10–3 in all green solvents. However, the correlation coefficients in water, ethanol, PG, PEG-400, EG, and Transcutol were observed in the range of 0.996–0.998, indicating a good fit. The solubility of OLM was found to be higher in PEG-400 (2.58 × 10–3 at 298.15 K) and Transcutol (2.48 × 10–3 at 298.15 K) as compared to water (2.32 × 10–7 at 298.15 K), ethanol (4.67 × 10–4 at 298.15 K), PG (9.23 × 10–5 at 298.15 K) and EG (6.73 × 10–5 at 298.15 K).

In the present study, we explored SA’s activity against DOX-induced cardiotoxicity and revealed its underlying mechanisms. Male Wistar rats (weight, 190-210g; n=6) were randomly divided into four groups: group I, normal control; group II, DOX 15 mg/kg via intraperitoneal (ip) route; group III, administered DOX+SA 20 mg/kg; and group IV, administered DOX+captopril (CAP 30 mg/kg). SA and CAP were administered orally for seven days, and DOX (15 mg/kg) was injected intraperitoneally an hour before SA treatment on the fifth day. Forty-eight hours after DOX administration, animals were anesthetized and sacrificed for molecular and histology experiments. SA significantly mitigated the myocardial effects of DOX, and following daily administration, it reduced serum levels of lactate dehydrogenase (LDH) and creatine kinase isoenzyme-MB to near normal values. Levels of oxidative stress markers, glutathione-peroxidase, superoxide dismutase, and catalase, in the cardiac tissue were significantly increased, whereas malondialdehyde levels decreased after SA treatment in DOX-administered rats. Furthermore, DOX caused an inflammatory reaction by elevating the levels of proinflammatory cytokines, tumor necrosis factor-α (TNF-α), interleukin-1β (IL-1β), and endothelin- (ET-) 1, as well as nuclear factor kappa-B (NF-κB) expression. Daily administration of SA significantly repressed TNF-α, IL-1β, ET-1, and NF-κB levels. caspase-3 and Bax expression, bcl-2-like protein and caspase-3 activities and levels. Overall, we found that SA could inhibit DOX-induced cardiotoxicity by inhibiting oxidative stress, inflammation, and apoptotic damage.

No abstract

The solubility of N-(4-chlorophenyl)-2-(pyridin-4-ylcarbonyl)hydrazinecarbothioamide (isoniazid analogue) in various diethylene glycol monoethyl ether (Transcutol) + water cosolvent mixtures was measured at (298.15 to 338.15) K using the shake flask method. In order to investigate the influence of temperature on solubility, the experimental solubilities of the isoniazid analogue were correlated with the Apelblat equation. To investigate the influence of cosolvent mixtures on solubility, the log−linear model of Yalkowsky was used. For the Apelblat equation, the root-mean-square deviations (RMSDs) were observed in the range of 0.004 to 0.033. For the Yalkowsky model, the RMSDs were observed in the range of 0.021 to 0.114. The correlation coefficients were observed in the range of 0.996 to 0.999. These results indicated the good fitting of experimental solubilities with the Apelblat equation and Yalkowsky model. The solubility of isoniazid analogue was found to be highest and lowest in pure Transcutol (4.23•10 −2 at 298.15 K) and pure water (5.17•10 −7 at 298.15 K), respectively. Thermodynamic parameters such as molar enthalpies and entropies were observed as positive values in all cosolvent mixtures, indicating that the dissolution process for the isoniazid analogue is endothermic and entropy-driven. Based on the solubility data of the current study, the isoniazid analogue has been considered as freely soluble in Transcutol and practically insoluble in water.