ENHANCEMENT OF AQUEOUS SOLUBILITY OF EZOGABINE: PREPARATION AND CHARACTERIZATION OF EZOGABINE NANOSUSPENSION ANTICIPATED FOR NOSE TO BRAIN TARGETING BY 32 FACTORIAL DESIGN
Pawar Anil R, Choudhari Pravin D, Pawar Amol R
Quality Assurance Department, MES`s, College of Pharmacy, Affiliated to Savitribai Phule Pune University, Sonai, Taluka-Newasa, District-Ahmednagar, Maharashtra, India. Department of Pharmaceutics, Modern College of Pharmacy, Nigdi, Pune, Maharashtra, India.Research Scholar, PRIST University, Thanjavur, Tamilnadu, India.
Keywords: Ezogabine, Nanosuspension, Nanoprecipitation, Factorial design, Aqueous solubility.
Abstract

Context:Adverse effects after oral administration, as well as low solubility, present a substantial contest for the suitability of formulations for intranasal drug delivery. Objectives: The objective of the present work was to develop ezogabine nanosuspension for enhancement of solubility and direct olfactory administration by 32 full factorial design and determine its pharmacokinetic and pharmacodynamic profile in rats. Methods:The ezogabine nanosuspension was developed by nanoprecipitation-ultrasonication method. The formulation was planned to develop by using a 2-factor, 3-level factorial design. The formulations were subjected to various in-vitro characterizations like particle size analysis, saturation solubility, in-vitro drug diffusion, zeta potential, SEM and TEM. The selected formulation was intranasally instilled into the nostrils of rats with the help of cannula for determining pharmacokinetic and pharmacodynamic profile in-vivo. Results: The formulation showed better results in terms of in-vitro and in-vivo study. The statistical analysis of data revealed that polymer concentration had significant effect on particle size and no significant effect on saturation solubility and in-vitro drug diffusion. Whereas, ultrasonication time had significant effect on particle size, saturation solubility and in-vitro drug diffusion (solubility). The Cmax revealed concentration of ezogabine in brain and plasma as 0.1812µg/ml and 0.183µg/ml, resp., for plain suspension and concentration of ezogabine in brain and plasma as 0.7885µg/ml and 0.7483µg/ml, resp, for nanosuspension at same dose of 1 mg/ml when administered intranasally. Conclusion:The present investigation confirmed that the potential of ezogabine nanosuspension for enhancement of aqueous solubility and providing direct nose-to-brain delivery.

Article Information

Identifiers and Pagination:
Year:2016
Volume:8
First Page:43
Last Page:60
Publisher Id:19204159.8:3.2016
Article History:
Received:November 24, 2015
Accepted:January 7, 2016
Collection year:2015
First Published:July 3, 2016


© 2016 The Author(s). This open access article is distributed under a Creative Commons Attribution (CC-BY) 4.0 license. You are free to: Share — copy and redistribute the material in any medium or format Adapt — remix, transform, and build upon the material for any purpose, even commercially. The licensor cannot revoke these freedoms as long as you follow the license terms. Under the following terms: Attribution — You must give appropriate credit, provide a link to the license, and indicate if changes were made. You may do so in any reasonable manner, but not in any way that suggests the licensor endorses you or your use. No additional restrictions You may not apply legal terms or technological measures that legally restrict others from doing anything the license permits
Editor in Chief
Prof. Dr. Cornelia M. Keck (Philipps-Universität Marburg)
Marburg, Germany

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Welcome to the research group of Prof. Dr. Cornelia M. Keck in Marburg. Cornelia M. Keck is a pharmacist and obtained her PhD in 2006 from the Freie Universität (FU) in Berlin. In 2009 she was appointed as Adjunct Professor for Pharmaceutical and Nutritional Nanotechnology at the University Putra Malaysia (UPM) and in 2011 she obtained her Venia legendi (Habilitation) at the Freie Universität Berlin and was appointed as a Professor for Pharmacology and Pharmaceutics at the University of Applied Sciences Kaiserslautern. Since 2016 she is Professor of Pharmaceutics and Biopharmaceutics at the Philipps-Universität Marburg. Her field of research is the development and characterization of innovative nanocarriers for improved delivery of poorly soluble actives for healthcare and cosmetics. Prof. Keck is executive board member of the German Association of Nanotechnology (Deutscher Verband Nanotechnologie), Vize-chairman of the unit „Dermocosmetics“ at the German Society of Dermopharmacy, active member in many pharmaceutical societies and member of the BfR Committee for Cosmetics at the Federal Institute for Risk Assessment (BfR).

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