To enhance oral bioavailability of poorly sol...

To enhance oral bioavailability of poorly soluble drug- Agomelatine in controlled release manner by solid lipid nanoparticles

Author Name : Divyanka Nandan, Rishikesh Bachhav

ABSTRACT

Oral drug delivery is continuously looking for new ways due to factors such as poor drug solubility and / or absorption, rapid metabolism, high plasma drug fluctuation, and nutritional variability that plays important role in disappointing results leads to a denial of the conventional transport system. Since the last decade, oral drug transport has taken a recent dimension with the enhancing use of lipids as a transporter or delivering poorly water-soluble, lipophilic drugs.

Agomelatine is poorly water soluble drug with less bioavailability.Solid lipid nanoparticles (SLN) are drug carriers consist of a solid core applicable to target drugs to specific site. SLNs are formed from lipid materials which are biocompatible and biodegradable, making them a favorable therapeutic strategy for drug targeting and transport. Glyceryl monostearate have been reported to improve the dissolution rate of poorly water soluble drugs. AGM-SLNs were prepared by hot homogenization method and evaluated for particle size, SEM, zeta potential, percent entrapment efficiency, drug release, XRD and DSC to characterize SLN formation. The percent entrapment efficiency was found to be 91.97%. The increase in lipid concentration has improved entrapment efficiency.

As quantity of surfactant and co-surfactant increases, the entrapment efficiency decreases. The particle size for the optimized batch was found to be in nanometric range i. e. 227.1nm. As the quantity of lipid is increases, the particle size of solid lipid nanoparticles increases. As the quantity of surfactant increases, the particles increases but the influence is not very strong. The zeta potential of SLN was in the range -26.7 which shows good colloidal stability. The dissolution profile of AGM-SLNs showed up to 91% release in 24hrs, that means the prepared AGM-SLNs showed enhanced dissolution which may leads to enhanced oral bioavailability of Agomelatine.

Keywords: Agomelatine,Solid Lipid Nanoparticles, AGM-SLNs preparation, AGM-SLNs evaluation.