Esraa Ghazy, Alaa Abdulhusain Abdulrasool, Jafar Jaber Al-Tamimi, Nawal Ayash


Nebivolol hydrochloride (NEB), is a third generation highly selective β1-blocker, it has an antihypertensive properties. Its elimination half-life is around 10 hrs while its oral bioavailability is about 12%. The objective of the current study was to develop nanostructured lipid carriers (NLCs) for transdermal delivery of (NEB). Through the preparation, characterization and conducting of an in vitro study for (NEB) loaded (NLCs), the formulation of NEB-NLCs based hydrogel using different types of gelling agents was introduced. Moreover, the incorporation of lipid nanoparticles into carbapol 934 as hydrogel base in different formulations was described in this study. The optimized formula (350 mg Glyceryl monostearate, 150 mg oleic acid, 2% (W/W) span 80, and 2% (W/W) Cremophor EL) was tested for entrapment efficiency, particle size and loading capacity then incorporated into hydrogel for expedient transdermal application. A number of measures were implemented for the NEB-NLCs based hydrogel, the results for the optimized formula were found to be as the following: particle size 228 nm, polydispersity index 0.3, zeta potential -29mV, pH 7.05 viscosity 7210cps, spreadability 6 cm, drug content 95%, and Ex Vitro skin permeation 90.8%. The transmission electron microscopy (TEM) and the optical microscope study revealed almost spherical shaped nanoparticles. Nebivolol  based  hydrogel  demonstrated no  skin  irritation  and  showed a  prolong  release  for up  to  24 hrs.  The flux for the permeation study through rat skin was found to be (143μg/cm2/hr). Carbapol 934 was used as a gelling agent; the obtained formula gave evidence for good spreadability, homogeneity and rheological behavior. In conclusion, the data obtained from this study illustrated a successful development of NEB-NLCs-based hydrogel in the increase of the encapsulation efficiency of colloidal lipid carriers. The advantages of the colloidal lipid carriers of the improved performance  were in terms of stability and provides a sustaining NEB transdermal effect.

Keywords: Nebivolol hydrochloride; Nanostructured lipid carriers, Hydrogel, Transdermal delivery


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