Formulation and Evaluation of Zolmitriptan Loaded Nano-Structured Lipid Carriers for Effective Treatment in Migraine

Abstract

Objective: Zolmitriptan is a BCS class II drug having low solubility and poor bioavailability by formulating Nanostructured lipid carriers that will sustain the release of the drug for a longer period which leads to reduced dose and frequency of dose.

Method: Zolmiptriptan-loaded Nanostructured lipid carriers were fabricated by a solvent diffusion evaporation method. The formulation parameters like the selection of solid (Precirol ATO 5) and liquid lipid (Miglyol 812), solid to liquid lipid ratio (3:1), drug: solid lipid ratio (1:4), the ratio of the organic phase (Acetone: Ethanol, 1:1), the concentration of surfactant (1.5% Tween 80) and temperature               (70 °C) of secondary phase were optimized. NLC dispersion was finally lyophilized and converted into a tablet. A stability study of freeze-dried NLCs tablet was performed according to ICH Q1A (R2) guidelines.

Result: Optimized formulation contained Particle size 11.39 ± 0.85 nm, Zeta potential -38.30 and %EE 76.56 ± 0.12. Characterization was performed by TEM and FTIR analysis. The residual solvent test confirms the concentration of organic solvents was in the acceptable range as per ICH guidelines. In-vitro drug permeation study of NLCs shows 88.91±0.238 % drug release while pure drug suspension shows 58.9±0.578 % drug release after 12 hrs. 

Conclusion: Zolmitriptan-loaded NLCs show better absorption as compared to pure drug suspension which indicates prolonged release of medicament which may reduce dose or dose frequency.