Abstract
Irbesartan is an antihypertensive with limited bioavailability and solid lipid nanoparticles (SLN) is one of the approaches to improve bioavailability. Solid lipid nanoparticles were prepared using glyceryl monostearate by solvent emulsification method followed by probe sonication. Irbesartan loaded SLNs were characterized and optimized by parameters like particle size, zeta potential, surface morphology entrapment efficiency and in vitro release. The optimized formulation was then further evaluated for the pharmacokinetic studies in Wistar rats. Irbesartan-loaded SLN of particle size 523.7 nm and 73.8% entrapment efficiency showed good bioavailability in Wistar rats and also showed optimum stability in the studies. The SLN prepared using glyceryl monostearate by solvent emulsification method leads to improve bioavailability of the drug.
Highlights
Colloidal systems are the most promising alternative drug delivery systems for improving the bioavailability and therapeutic availability of the drugs
The particle size was observed in the range of 360 to 1129 nm with zeta potential -13 to -21.5 mV for the prepared batches of Solid lipid nanoparticles (SLN)
It has been observed that an increase in lipid content (GMS) does not significantly affect the particle size; the particle size increased with increasing poloxamer 407 concentrations
Summary
Colloidal systems are the most promising alternative drug delivery systems for improving the bioavailability and therapeutic availability of the drugs. The solid lipids are used for the preparation of SLN instead of liquid lipids (used in case of liposomes) to overcome the disadvantages associated with the liquid state and to improve physical stability. SLN possesses advantages over other colloidal delivery systems of increased physical stability, high drug payload and absence of carrier biotoxicity. Various literature suggested solid lipid nanoparticle as an efficient way to improve bioavailability of drugs along with improved physical stability (Ganapuram et al, 2013; Zhang et al, 2012; Hirlekar, Kadam, 2009). The present study was carried out with the aim to improve the solubility and dissolution profile of irbesartan by preparing its solid lipid nanoparticles using the solvent emulsification method. The prepared nanoformulation was characterized and evaluated for in vitro release and in vivo studies
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