Comparative in vitro and in vivo evaluation of lipid based nanocarriers of Huperzine A.

The purpose of the present investigation was to explore feasibility of nanocarrier based transdermal delivery of Huperzine A (HupA) for the treatment of Alzheimer's disease. For this investigation, microemulsion (ME), solid lipid nanoparticles (SLNs), and nanostructured lipid carriers (NLCs) were formulated and characterized for physicochemical parameters. The pseudo-ternary phase diagrams for microemulsion region were developed using generally recognized as safe (GRAS) excipients. The SLNs and NLCs were prepared by microemulsion template technique. These nanodispersions were formulated into gels for transdermal application and evaluated for various physicochemical parameters. In vitro permeation profiles in rat skin exhibited zero-order kinetics. HupA loaded ME exhibited superior permeation than NLCs followed by SLNs and cumulative amount permeated after 24h was found to be 147.68±9.42 μg/cm(2), 129.11±32.76 μg/cm(2) and 10.74±0.68 μg/cm(2), respectively. Furthermore, optimized gels were subjected to primary skin irritation testing over a period of 48 h and were found to be safe for skin application. In vivo efficacy tested in scopolamine induced amnesia model indicated significant improvement in cognitive function in mice group treated with developed nanocarrier based formulations as compared to the control group.
AuthorsPratikkumar A Patel, Sushant C Patil, Dhaval R Kalaria, Yogeshwar N Kalia, Vandana B Patravale
JournalInternational journal of pharmaceutics (Int J Pharm) Vol. 446 Issue 1-2 Pg. 16-23 (Mar 25 2013) ISSN: 1873-3476 [Electronic] Netherlands
PMID23410989 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCrown Copyright © 2013. Published by Elsevier B.V. All rights reserved.
Chemical References
  • Alkaloids
  • Cholinesterase Inhibitors
  • Drug Carriers
  • Gels
  • Neuroprotective Agents
  • Sesquiterpenes
  • huperzine A
  • Scopolamine Hydrobromide
  • Administration, Cutaneous
  • Alkaloids (administration & dosage, chemistry)
  • Amnesia (chemically induced, drug therapy, physiopathology)
  • Animals
  • Cholinesterase Inhibitors (administration & dosage, chemistry)
  • Drug Carriers (administration & dosage, chemistry)
  • Drug Stability
  • Gels
  • Hydrogen-Ion Concentration
  • In Vitro Techniques
  • Male
  • Maze Learning
  • Mice
  • Nanoparticles (administration & dosage, chemistry)
  • Neuroprotective Agents (administration & dosage, chemistry)
  • Particle Size
  • Rabbits
  • Rats
  • Rats, Wistar
  • Scopolamine Hydrobromide
  • Sesquiterpenes (administration & dosage, chemistry)
  • Skin (metabolism)
  • Skin Absorption
  • Skin Irritancy Tests
  • Viscosity

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