title: Rivastigmine-loaded in situ gelling nanostructured lipid carriers for nose to brain delivery.
abstract: In the current research work, rivastigmine (RV)-loaded in situ gelling nanostructured lipid carriers (NLCs) were developed for nose to brain delivery. NLCs were fabricated by ethanol injection method using glyceryl monosterate, Capmul MCM C8, Lecithin and Tween 80. NLCs showed average particle size of 123.2 ± 2.3 nm with entrapment efficiency of 68.34 ± 3.4%. DSC, XRD and IR studies showed complete amorphization and incorporation of the drug into nanoparticles. NLCs were incorporated into an in situ gelling system using 0.8% gellan gum and 15% Lutrol F 127. RV in situ gel showed excellent elasticity, rheology, mucoadhesion and adhesiveness to facilitate its adhesion to the upper nasal mucosa. NLC-based in situ gel showed a 2-fold increase in nasal permeation of the drug over plain RV solution. In situ gelling NLCs showed a 3-fold increase in enzyme inhibition efficacy.
authors.affiliation: Department of Pharmaceutical Sciences and Technology, Center for Novel Drug Delivery Systems, Institute of Chemical Technology , Mumbai, Maharashtra , India.
authors.forename: Preeti R
authors.initials: PR
authors.lastname: Wavikar
authors.forename: Pradeep R
authors.initials: PR
authors.lastname: Vavia
mesh_terms: D000818:Animals; D001921:Brain / Q000378:metabolism*; D004337:Drug Carriers / Q000737:chemistry / Q000378:metabolism; D005782:Gels / Q000737:chemistry / Q000378:metabolism*; D008055:Lipids / Q000737:chemistry*; D049329:Nanostructures / Q000737:chemistry*; D009297:Nasal Mucosa / Q000378:metabolism*; D009666:Nose / Q000737:chemistry; D009821:Oils / Q000737:chemistry; D010316:Particle Size; D000068836:Rivastigmine / Q000737:chemistry / Q000378:metabolism*; D012756:Sheep; D012995:Solubility; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry / Q000378:metabolism
chemical_list: D004337:Drug Carriers; D005782:Gels; D008055:Lipids; D009821:Oils; D013501:Surface-Active Agents; D000068836:Rivastigmine
keywords: Acetylcholine esterase enzyme inhibition; in situ gel; rheology; rivastigmine; texture analysis