Preparation, Characterization and in vivo Evaluation of Parenteral Sustained Release Microsphere Formulation of Zopiclone

The aim of this study was to prepare zopiclone-loaded polycaprolactone microspheres by emulsion solvent evaporation technique with different drug-to-carrier ratios {MP 1 (1:1), MP 2 (1:2), MP 3 (1:3), and MP 4 (1:4)}, characterize and evaluate the in vivo performance. The microspheres were characterized for particle size, surface morphology, drug excipient compatibility, percentage yield, drug entrapment, and in vitro release kinetics. Pharmacokinetics and pharmacodynamics were evaluated after parenteral administration so as to determine the sustained action of the drug after one-time administration of the formulation in a rat model. Of four formulations prepared, MP 2, i.e., 1:2 (drug–polymer) ratio was selected as the optimized formulation based on particle size, particle shape, and the release behavior. The size of microspheres was found to be ranging from 5.4 to 12.1 µm. The shape of microspheres was found to be spherical by SEM. Among the four formulations, MP 2 (1:2) showed maximum percentage yield of 75% ± 2.68%. There was no interaction between drug and polymer by FT-IR study. In the in vitro release study, formulation MP 2 (1:2) showed 86.5% drug release and was found to be sustained for 10 days. The microsphere formulations were able to sustain the release of drug both in vitro and in vivo. Pharmacodynamic study (Maze apparatus) indicated that the anxiolytic activity shown by zopiclone microspheres was significant when compared to the zopiclone solution given daily

Trapa bispinosa Roxb.: A Review on Nutritional and Pharmacological Aspects

Trapa bispinosa Roxb. which belongs to the family Trapaceae is a small herb well known for its medicinal properties and is widely used worldwide. Trapa bispinosa or Trapa natans is an important plant of Indian Ayurvedic system of medicine which is used in the problems of stomach, genitourinary system, liver, kidney, and spleen. It is bitter, astringent, stomachic, diuretic, febrifuge, and antiseptic. The whole plant is used in gonorrhea, menorrhagia, and other genital affections. It is useful in diarrhea, dysentery, ophthalmopathy, ulcers, and wounds. These are used in the validated conditions in pitta, burning sensation, dipsia, dyspepsia, hemorrhage, hemoptysis, diarrhea, dysentery, strangely, intermittent fever, leprosy, fatigue, inflammation, urethrorrhea, fractures, erysipelas, lumbago, pharyngitis, bronchitis and general debility, and suppressing stomach and heart burning. Maybe it is due to photochemical content of Trapa bispinosa having high quantity of minerals, ions, namely, Ca, K, Na, Zn, and vitamins; saponins, phenols, alkaloids, H-donation, flavonoids are reported in the plants. Nutritional and biochemical analyses of fruits of Trapa bispinosa in 100 g showed 22.30 and 71.55% carbohydrate, protein contents were 4.40% and 10.80%, a percentage of moisture, fiber, ash, and fat contents were 70.35 and 7.30, 2.05 and 6.35, 2.30 and 8.50, and 0.65 and 1.85, mineral contents of the seeds were 32 mg and 102.85 mg calcium, 1.4 and 3.8 mg Iron, and 121 and 325 mg phosphorus in 100 g, and seeds of Trapa bispinosa produced 115.52 and 354.85 Kcal of energy, in fresh and dry fruits, respectively. Chemical analysis of the fruit and fresh nuts having considerable water content citric acid and fresh fruit which substantiates its importance as dietary food also reported low crude lipid, and major mineral present with confirming good amount of minerals as an iron and manganese potassium were contained in the fruit. Crude fiber, total protein content of the water chestnut kernel, Trapa bispinosa are reported. In this paper, the recent reports on nutritional, phytochemical, and pharmacological aspects of Trapa bispinosa Roxb, as a medicinal and nutritional food, are reviewed

Anti-inflammatory activity of <i>Jatropha gossypifolia </i>L. leaves in albino mice and Wistar rat

289-292Methanolic extract of Jatropha gossypifolia L. leaves showed systemic and significant anti-inflammatory activity in acute carrageenan-induced rat paw edema and chronic cotton pellet induced granuloma formation after oral treatment for 7 days in Wistar rats. Anti-inflammatory activity might be due to effects on several mediators and arachidonic granular tissue formation and leukocyte migration from vessels

Evaluation of anti-inflammatory activity of Solanum xanthocarpum Schrad and Wendl (Kaṇṭakāri) extract in laboratory animals

Context: Solanum xanthocarpum Schrad and Wendl (Kaṇṭakāri) is a diffuse herb with prickly stem, traditionally used for the treatment of inflammation and one in the group of daśamūla (group of ten herbs) herbs commonly used drug in Ayurveda. Aims: In continuation of search for potent natural anti-inflammatory agents, the present research work was planned to evaluate the anti-inflammatory activity of ethanol extract of S. xanthocarpum whole plant. Settings and Design: The ethanol extract was evaluated at dose 10, 30 and 100 mg/kg p.o. in rats. Materials and Methods: Using pharmacological screening models carrageenan induced rat paw edema, histamine induced rat paw edema and cotton pellet granuloma in rats. Statistical Analysis Used: Data obtained was analyzed statistically using analysis of variance followed by post-hoc Dunnett test, P < 0.05 is considered as statistically significant. Results: Acute treatment didn′t show anti-inflammatory activity against carrageenan and histamine induced paw edema. However, administration of 100 mg/kg p.o for 7 day reduced the granuloma formation in cotton pellet granuloma model. Conclusions: Present results support the traditional use of plant for anti-inflammatory activity. In brief, the results provide scientific pharmacological basis for the therapeutic use of S. xanthocarpum

Effect of hydroalcoholic extract of Sphaeranthus indicus against experimentally induced anxiety, depression and convulsions in rodents

To investigate the effects of a hydroalcoholic extract of the Sphaeranthus indicus (SIE) against experimentally induced anxiety, depression and convulsions in rodents. The SIE (100, 200, 500 mg/kg, p.o.) was used in elevated plus maze, open field, forced swimming, and tail suspension tests in mice. The same doses were also used to evaluate its anticonvulsant effect on pentylenetetrazole (PTZ)-induced convulsions in mice and maximal electroshock (MES)-induced convulsions in rats. SIE was found to increase the number of entries and the time spent in the open arms of the maze at a dose of 100 mg/kg, p.o., indicating its anxiolytic activity. On the other hand, higher doses of SIE (200 and 500 mg/kg, p.o.) decreased open arm entries and time spent in the open arms of the maze in the elevated plus maze test indicating an absence of anxiolytic activity. However, this effect could have been related to a decrease in the locomotor activity of the mice and not to an anxiogenic effect, as indicated by the reduction in the total number of entries in the elevated plus maze. SIE also (at doses of 200 and 500 mg/kg, p.o.) decreased locomotor activity but did not affect emotional activity parameters in the open field test, suggesting a possible central nervous depressant activity. SIE also increased the immobility time in the forced swimming test at an oral dose of 500 mg/kg but did not significantly modify the activity in the tail suspension test. SIE protected rats against MES-induced convulsions and mice against PTZ-induced convulsions. Sphaeranthus indicus demonstrated anxiolytic, central nervous depressant, and anticonvulsant activities in rodents, thus supporting the folk medicinal use of this plant in nervous disorders