Fibrinolytic activity of kaempferol isolated from the fruits of Lagenaria siceraria (Molina) Standley.

This study was undertaken to isolate a flavonol, kaempferol, from the fruits of Lagenaria siceraria (bottle gourd) as a sole compound and to explore the fibrinolytic potential of the methanolic extract of the fruits of L. siceraria and the isolated compound using their in vitro activity. The fibrinolytic activity in terms of percentage of plasma clot liquefaction was determined by plasma clot lysis at 37°C in 24 h. The fibrinolytic activity of both substances was compared to the well-known thrombolytic agent streptokinase (30,000 IU). The percentage of fibrinolytic activity of the extract and isolated compound were found to be 54.72 ± 0.7210 and 77.37 ± 1.3010, respectively. Streptokinase was considered as the standard fibrinolytic enzyme for comparative purposes and had 91.46 ± 0.7625% fibrinolytic activity. The conclusion drawn in our study after testing the hypothesis by experimental procedures is that in vitro fibrinolytic activity on plasma clots is an inherent property of kaempferol isolated from the fruits of L. siceraria, and its comparison with streptokinase is a new aspect for further study.

Formulation and evaluation of verapamil hydrochloride loaded solid lipid microparticles.

The present study aimed to produce verapamil hydrochloride-loaded solid lipid microparticles (SLM) by the w/o/w emulsion solvent evaporation technique, using diethyl ether as solvent phase, glyceryl monostearate as biodegradable polymer and Span 60 as surfactant. SLM of spherical shape were prepared by simple dilution of the emulsion with water. To increase the lipid load the process was conducted at 50 degrees C, and in order to reach sub-micron size, a high-shear homogenizer was used. The encapsulation efficiency of prepared SLM reached 74.29 +/- 0.76%. Particle size (98.55 +/- 1.42 microm), surface morphology (spherical) and drug loading efficiency (18.57 +/- 1.25% w/w) were investigated. And optimization of drug polymer ratio (3:1), nature and concentration of emulsion stabilizer in the external aqueous (0.1%), phase viscosity of external aqueous phase (0.5%), volume of external aqueous phase and stirring rate (1000 rpm) were detected. Analysis of microsphere content after processing showed that verapamil did not undergo any chemical modification within the micro-particles. The in-vitro release of verapamil from the microparticles was very low and an initial burst effect of 17% of the dose was observed. The slow release may help to avoid a high frequency of administration. The prepared solid lipid microparticles appear to have interesting perspectives as delivery systems for the oral administration of verapamil hydrochloride with improved half-life, improved bioavailability, and minimized local and systemic gastrointestinal disturbances of the drug.

Development and characterization of in situ gel system for nasal insulin delivery.

The objective of the present study was to develop a thermosensitive in situ gel system based on chitosan and poly vinyl alcohol (PVA) for nasal delivery of insulin. The hydrogel was prepared by mixing chitosan and PVA. The concentration of the components was optimized during formulation development. The prepared hydrogel was characterized for gelation temperature, gelation time, viscosity changes, degree of swelling, in vitro release and in vivo hypoglycemic effect. The prepared hydrogel was liquid at room temperature while underwent thermal transition from solution below or at room temperature to non-flowing hydrogel when incubated at 37 degrees C for approximately 12 minutes with increased viscosity. The in vitro release of insulin from gel network was observed spectrophotometrically which was good enough to maintain blood glucose level for six hour. Furthermore, the formulation when evaluated for their in vivo hypoglycemic effect, demonstrated its ability to reduce glucose level. The observed in vitro and in vivo results indicate that the proposed thermosensitive in situ gelling system has substantial potential as nasal delivery system for insulin.