Open AccessNose‐to‐brain delivery of sumatriptan‐loaded nanostructured lipid carriers: preparation, optimization, characterization and pharmacokinetic evaluation
Author(s) -
Masjedi Moein,
Azadi Amir,
Heidari Reza,
MohammadiSamani Soliman
Publication year - 2020
Publication title -
journal of pharmacy and pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.745
H-Index - 118
eISSN - 2042-7158
pISSN - 0022-3573
DOI - 10.1111/jphp.13316
Subject(s) - sumatriptan , nasal administration , pharmacokinetics , zeta potential , dispersity , drug delivery , solid lipid nanoparticle , bioequivalence , materials science , drug carrier , pharmacology , vomiting , in vivo , migraine , medicine , biomedical engineering , nanoparticle , nanotechnology , anesthesia , receptor , microbiology and biotechnology , polymer chemistry , biology , agonist
Objectives Migraine is a neurological disorder with unilateral pulsatile headache which can affect the functions of sufferers. Migraineurs experience some undesirable symptoms such as pain, nausea, vomiting and in some cases auras which make the oral delivery non‐selective. The lipid nanoparticles are considered as good carriers for nose‐to‐brain drug delivery. The present study aimed to formulate and evaluate a sumatriptan‐loaded nanostructured lipid carrier (NLC). Methods A drug‐loaded NLC was optimized using D‐optimal design of experiment and then the characterization of the formulated NLC including particle size, zeta potential, electron microscopy, thermal analysis, drug loading efficiency and release kinetics were carried out. Pharmacokinetic evaluations were also performed during an in‐vivo study on Sprague–Dawley rats and neuropharmacokinetic parameters such as drug targeting efficiency (DTE) and direct transport percentage (DTP) were calculated. Key findings The optimization of experiments led to nanoparticles with 101 nm mean diameter and polydispersity index (PDI) of 0.27. The drug entrapment efficiency (EE) for optimized nanoparticle was found to be 91.00%. DTE and DTP of intranasal‐administered NLC were calculated 258.02% and 61.23%, respectively. Conclusions Neuropharmacokinetic evaluation of intranasal NLC dispersion represents a suitable brain delivery system. The DTP of NLC formulation suggests the desirable entrance of sumatriptan into the brain.