Nebivolol Hydrochloride Loaded Nanostructured Lipid Carriers as Transdermal Delivery System: Part 1: Preparation, Characterization and In Vitro Evaluation

Abstract

Nebivolol hydrochloride (NEB) is a 3^rd generation highly selective β₁-blocker with antihypertensive properties, the elimination half-life is about 10 hrs and the oral bioavailability is about 12%.

            The study was aimed to develop nanostructured lipid carriers (NLC) for transdermal delivery of NEB.

            The study involves two separate parts, part 1 (current) involves preparation and characterization of NEB loaded NLCs (NEB-NLCs). Part 2 of the study, NEB-NLCs based gel was formulated using gelling agent carbapol 934 as transdermal delivery system using rat skin. Part 2 of the study will be presented separately in the forthcoming issue.

            The current investigation describes the effect of type and concentration of different solid lipids, liquid lipids, and surfactant/co-surfactant on the characteristics of NLC such as particle size, polydispersity index, zeta potential, drug entrapment efficiency, and drug release profile. Transmission electron microscopy, scanning electron microscope and atomic force microscope revealed nearly spherical shape NLC with negligible effect of liquid lipid (oleic acid) content on the particle morphology. The differential scanning calorimetry demonstrated depression in the melting point and crystallinity index of the NLCs with increasing the amount of liquid lipid. The in vitro drug release studies demonstrated that 93% of the drug was released over 24hrs. The NEB-NLCs possessed a biphasic release pattern characterized by a rapid initial release followed by a sustained release.