Enhancement of solubility and dissolution profile of artesunate by employing solid dispersion approach: An in-vitro evaluation.

Current study was designed with an aim to improve the solubility and dissolution profile of artesunate by preparing solid dispersions through solvent evaporation and freeze-drying techniques using polyethylene glycol 4000 (PEG4000) as solubility enhancer. Developed formulations were characterized for FTIR, XRD, TGA and SEM. Maximum increase in solubility was attained by freeze-dried solid dispersions (FD F444) i.e. 2.99 folds and 2.66 folds by solvent evaporation solid dispersion (SE F44) as compare to pure drug. Amorphous nature of artesunate in solid dispersions was confirmed from XRD diffractographs. Surface morphology indicated the existence of rough surface in freeze- dried solid dispersions (FDDs) and smooth surface in solvent evaporation solid dispersions (SEDs). Rapid dissolution rates were exhibited by fast dissolving tablets of optimized formulations. Moreover, the release of the drug was dominated by the first order kinetics (R2 = 0.9932) with the Fickian type of diffusion mechanism (n<0.450).

Diuretic and serum electrolyte regulation potential of aqueous methanolic extract of Solanum surattense fruit validates its folkloric use in dysuria.

BACKGROUND: Solanum surattense Burm. (Solanaceae) is traditionally used for management of various ailments. The study was conducted for provision of pharmacological justification for folkloric uses of Solanum surattense in the treatment of dysuria. METHODS: Rats were randomly divided into 5 groups, each of (n = 6). Aqueous methanolic fruit extract of S. surattense were also administered intraperitoneally to the rats at doses of 50, 70 and 100 mg/kg. Furosemide (10 mg/kg i.p) was used as standard drug whereas controls were given saline solution (40 mL/kg i.p). The electrolytes in urine were measured using a flame photometer whereas serum sodium, potassium, calcium, bicarbonate and blood urea nitrogen (BUN) were determined by using an automatic analyzer. Urine osmolality was assayed by the micro-osmometer. RESULTS: The extract S. surattense induced diuretic effects in a dose-dependent manner as compared with control. Upon administration of extract (70 and 100 mg/kg), we observed the prominent (p < 0.01) increase in the urine volume and osmolality in comparison to control group. However, plant extract (100 mg/kg) significantly increase the urinary electrolyte excretion especially calcium (p < 0.05) to that of the furosemide whereas level of magnesium remains constant. Moreover, our results showed a decrease in serum levels of sodium, potassium, calcium and blood urea nitrogen (BUN), but concentration dependent increase in bicarbonate was found in the test groups. There was no substantial change in the pH of urine samples of the extract-treated groups. CONCLUSION: These results indicate that S. surattense investigated exert its action by causing diuresis in the treatment of dysuria.

RP-HPLC Method for the Determination and Quantification of Artesunate.

A simple, rapid and cost-effective reverse phase high-performance liquid chromatographic (RP-HPLC) method was developed for the quantification of artesunate. C18 Promosil (ODS, 150 × 4.6 mm, 5 µm) column was used as stationary phase to separate the drug. Mobile phase comprised of ethanol: water (65:35) having pH 4.5 was run isocratically at a flow rate of 1 mL/min at 27°C. The method was validated according to ICH guidelines for linearity, precision, accuracy, robustness, specificity, limit of detection (LOD) and limit of quantification (LOQ). The method was found accurate, precise and robust with an average retention time of 4.509 min and 0.5357 %RSD. Good linearity was observed in the concentration range of 2-10 mg/ml with regression coefficient R2 value of 0.9995 and slope value of 369,928. Conclusively, as per ICH norms, the developed method was successfully validated and used for the quantification of artesunate in fast dissolving tablets (FDTs).

Immunomodulatory, Cytotoxicity, and Antioxidant Activities of Roots of Ziziphus mauritiana.

AIMS: The study is conducted to evaluate the immunomodulatory, cytotoxicity, and antioxidant potential of Ziziphus mauritiana (Rhamnaceae). Phytochemical analysis of Z. mauritiana revealed the presence of alkaloids, anthraquinone glycoside, cardiac glycoside, saponin, tannin, and flavonoids. METHODOLOGY: The cytotoxicity of the plant Z. mauritiana was evaluated by brine shrimp lethality test. Antioxidant parameters such as superoxide dismutase (SOD), total antioxidant capacity (T-AOC), and malondialdehyde (MDA) levels were calculated in the plasma of rats after chronic administration of 400 mg/kg of Z. mauritiana for 6 weeks. RESULTS: The dichloromethane extract of the plant exhibited significant immunomodulatory activity, with inhibitory concentration 50% of 55.43 ± 7.9. The dichloromethane extracts of the plant showed 70% mortality at concentration 1000 µg/ml. SOD and T-AOC levels were increased while MDA level in the plasma was reduced in the plasma of rats treated with dichloromethane Z. mauritiana. CONCLUSION: This can be deduced that the root of Z. mauritiana has immunomodulatory, cytotoxic, and antioxidant potential. SUMMARY: Roots of Z. mauritiana was exhibited immunomodulator, cytotoxic and antioxidant activitiesZ. mauritiana showed potential antioxidant activity in rats Abbreviations used: SOD: Superoxide dismutase; T-AOC: Total antioxidant capacity; MDA: Malondialdehyde; ZMRD: Z. mauritiana root extract of dichloromethane fraction; LD50: Z. mauritiana root extract of methanol fraction ZMRM, lethal dose 50.