Preparation and In Vitro/In Vivo Evaluation of Gliclazide Loaded Eudragit Nanoparticles as a Sustained Release Carriers

Abstract

The aim of this study was to formulate and optimize gliclazide-loaded Eudragit nanoparticles (Eudragit L100 and Eudragit RS) as a sustained release carrier with enhanced efficacy. Eudragit L 100 nanoparticles (ELNP) were prepared by controlled precipitation method whereas Eudragit RSPO nanoparticles (ERSNP) were prepared by solvent evaporation method. The influence of various formulation factors (stirring speed, drug:polymer ratio, homogenization, and addition of surfactants) on particle size, drug loading, and encapsulation efficiency were investigated. The developed Eudragit nanoparticles (L100 and RS) showed high drug loading and encapsulation efficiencies with nanosize. Mean particle size altered by changing the drug:polymer ratio and stirring speed. Addition of surfactants showed a promise to increase drug loading, encapsulation efficiency, and decreased particle size of ELNP as well as ERSNP. Dissolution study revealed sustained release of gliclazide from Eudragit L100 as well as Eudragit RSPO NP. SEM study revealed spherical morphology of the developed Eudragit (L100 and RS) NP. FT-IR and DSC studies showed no interaction of gliclazide with polymers. Stability studies revealed that the gliclazide-loaded nanoparticles were stable at the end of 6 months. Developed Eudragit NPs revealed a decreased t(min) (ELNP), and enhanced bioavailability and sustained activity (ELNP and ERSNP) and hence superior activity as compared to plain gliclazide in streptozotocin induced diabetic rat model and glucose-loaded diabetic rat model. The developed Eudragit (L100 and RSPO) NP could reduce dose frequency, decrease side effects, and improve patient compliance.

Comparative pharmaceutical study on colon targeted micro-particles of celecoxib:in-vitro–in-vivoevaluation

“…Both Eudragit L microparticles showed no drug release in the acidic medium, and this was the opposite from the findings of Eerikäinen et al (2004); Devarajan & Sonavane (2007); Paola et al (2008), where the Eudragit L Figure 2. In-vitro release of celecoxib from the prepared microparticles.…”

Preparation and Evaluation of Glibenclamide-Loaded Biodegradable Nanoparticles

“…PLGA and GB were dissolved in 25 ml of solvent mixture containing methanol to dichloromethane in a ratio 2:1, using a vortex shaker to form a homogeneous solution of drug and polymer. This homogeneous solution was added slowly to 120 ml of aqueous surfactant solution containing 0.5 % w/v polyvinyl alcohol and polysorbate-80, and homogenised using a high pressure homogenizer (Ika, Japan) to obtain an emulsion [13][14][15]. The emulsion formed was stirred with a laboratory magnetic stirrer (Remi, India) for 5 h at 25 ºC followed by centrifugation (Remi, India) for 22 min.…”

Enhancement of Entrapment Efficiency of Porous Chitosan Scaffold Formulation by the Addition of Peg 4000

“…The % entrapment efficiency of the scaffold formulations were calculated from the following equation. Entrapment efficiency (%) = D L -D F / D L x 100, where D L and D F are initial drug loaded (mg) and free drug (mg) respectively [2].…”