Solid lipid nanoparticles of ondansetron HCl for intranasal delivery: development, optimization and evaluation

Abstract

The present investigation deals with the development and statistical optimization of solid lipid nanoparticles (SLNs) of ondansetron HCl (OND) for intranasal (i.n.) delivery. SLNs were prepared using the solvent diffusion technique and a 2(3) factorial design. The concentrations of lipid, surfactant and cosurfactant were independent variables in this design, whereas, particle size and entrapment efficiency (EE) were dependent variables. The particle size of the SLNs was found to be 320-498 nm, and the EE was between 32.89 and 56.56 %. The influence of the lipid, surfactant and cosurfactant on the particle size and EE was studied. A histological study revealed no adverse response of SLNs on sheep nasal mucosa. Transmission electron microscopic analysis showed spherical shape particles. Differential scanning calorimetry and X-ray diffraction studies indicated that the drug was completely encapsulated in a lipid matrix. In vitro drug release studies carried out in phosphate buffer (pH 6.6) indicated that the drug transport was of Fickian type. Gamma scintigraphic imaging in rabbits after i.n. administration showed rapid localization of the drug in the brain. Hence, OND SLNs is a promising nasal delivery system for rapid and direct nose-to-brain delivery.

Formulations for Intranasal Delivery of Pharmacological Agents to Combat Brain Disease: A New Opportunity to Tackle GBM?

“…Joshi et al . formulated ondansetron HCl in solid lipid nanoparticles based on glycerol monostearate, which were also created by solvent diffusion [111]. Radiolabelling of these lipid nanoparticles showed a rapid uptake of these complexes in the brain of rabbits.…”

Preparation of Solid Lipid Nanoparticles and Nanostructured Lipid Carriers for Drug Delivery and the Effects of Preparation Parameters of Solvent Injection Method

“…A 2 3 factorial design was used to optimize the SLNs, which exhibited a PS of 320 nm, a PDI of 0.296, and an EE of 49.7%. The SLNs effectively delivered the drug to brain by intranasal administration in rabbits, as evidenced by gamma scintigraphic imaging [ 43 ]. Table 2 summarizes the major features of studies that utilized the solvent injection method, including the lipids used, drugs incorporated, and primary outcomes.…”

“…Some studies have investigated the solvent injection method for the production of SLNs and NLCs for different applications [ 40 , 41 ]. Others have investigated the effects of solvent injection process parameters on the physicochemical properties of SLNs and NLCs [ 42 , 43 , 44 ].…”

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“…This might be due to expelling out of excess lipid during particle formation. [27] Polydispersity index <0.300 indicates narrow and uniform particle size distribution. [28] The uniformity in particle size was also increased with the increase in the concentration of surfactant as reflected in batches D5 and D6 in Table 2.…”