Formulation and evaluation of nano structured lipid carriers for intranasal delivery of Buspirone hydrochloride

Abstract

The aim of this work was to formulate buspirone hydrochloride (BH) NLCs for intranasal administration to improve BH bioavailability. The BH loaded NLCs were prepared by hot high-pressure homogenization technique using Precirol ATO 5, olive oil and tween 80 as solid lipid, liquid lipid and surfactant, respectively. Carbopol 934P and HPMC K4M were used to convert NLCs dispersion into NLCs based in-situ nasal gelling solution to improve its mucoadhesive property for intranasal administration. A factorial design approach was used to study the effect of independent variable (amount of Precirol ATO 5 and olive oil) on the dependent variables (particle size and percentage entrapment efficiency (%EE). The optimized formulation was characterized for particle size, zeta potential, %EE, and surface morphology. Fourier transform infrared (FTIR) spectroscopy was used to study the possible BH-lipid complex formation. Further, viscosity determination, stability studies, in-vitro drug release, ex-vivo skin permeation studies and ex-vivo nasal toxicity studies of BH loaded NLCs nasal gelling solution were carried out. The BH loaded NLCs (batch F8) showed particle size of 111.8nm, %EE of 78.34% and zeta potential of-44.3mV. Scanning electron microscopy (SEM) confirmed spherical shape of NLCs. In vitro drug release and ex vivo skin permeation studies of BH loaded NLCs and BH loaded NLCs in-situ nasal gelling solution showed 71.26% drug permeation.