4.3 Article

Rivastigmine-loaded in situ gelling nanostructured lipid carriers for nose to brain delivery

Journal

JOURNAL OF LIPOSOME RESEARCH
Volume 25, Issue 2, Pages 141-149

Publisher

INFORMA HEALTHCARE
DOI: 10.3109/08982104.2014.954129

Keywords

Acetylcholine esterase enzyme inhibition; in situ gel; rheology; rivastigmine; texture analysis

Funding

  1. UGC

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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.

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