title: Sumatriptan succinate loaded chitosan solid lipid nanoparticles for enhanced anti-migraine potential.
abstract: The objective of the present investigation was to prepare chitosan solid lipid nanoparticles (SLN), containing sumatriptan succinate using solvent injection method and to optimize the formulations for brain targeting potential. The formulation optimization was performed using three factor two level full factorial design so as to minimize the particle size and zeta potential, maximize the entrapment efficiency as well as maximize the concentration of drug in brain with maximized brain/plasma ratio of the drug. The particle size, zeta potential and entrapment efficiency for all the batches were in the range of 192-301.4nm, 30.2-51.4mV and 76.3-91.1% respectively. The optimized formulation showed a 4.54-fold increase in brain/blood ratio of drug after 2h of drug administration in male Wistar rats. The optimized nanoparticles were characterized by FT-IR spectroscopy, DSC, TGA, powder X-ray diffraction study and TEM analysis. It could be elucidated from the experimental in vivo and behavioral studies that the formulations successfully crossed the blood brain barrier and significantly exhibited its anti-migraine activity. Present investigation indicated that the hydrophilic drug sumatriptan succinate, loaded in chitosan SLN, can be successfully targeted to brain via oral delivery and thus present an effective approach for the therapeutic management of migraine.
authors: Department of Pharmaceutical Sciences, G. J. University of Science & Technology, Hisar 125001, India.
authors: Girotra Priti
authors: GP
authors: Hansraj
authors: Department of Pharmaceutical Sciences, G. J. University of Science & Technology, Hisar 125001, India. Electronic address: sksingh_gju@rediffmail.com.
authors: Shailendra Kumar
authors: SK
authors: Singh
authors: Department of Pharmaceutical Sciences, G. J. University of Science & Technology, Hisar 125001, India.
authors: Pawan
authors: P
authors: Kumar
mesh_terms: D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D001921:Brain / Q000378:metabolism; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D048271:Chitosan / Q000737:chemistry*; D004195:Disease Models, Animal; D004337:Drug Carriers / Q000737:chemistry; D065546:Drug Liberation; D008297:Male; D051379:Mice; D008881:Migraine Disorders / Q000188:drug therapy / Q000378:metabolism; D053758:Nanoparticles / Q000737:chemistry* / Q000648:ultrastructure; D051381:Rats; D058825:Serotonin 5-HT1 Receptor Agonists / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D017550:Spectroscopy, Fourier Transform Infrared; D018170:Sumatriptan / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics; D013818:Thermogravimetry; D014961:X-Ray Diffraction
chemical_list: D004337:Drug Carriers; D058825:Serotonin 5-HT1 Receptor Agonists; D018170:Sumatriptan; D048271:Chitosan
keywords: Chitosan; Migraine; Optimization