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Preparation and Evaluation of Nimesulide-loaded Ethylcellulose and Methylcellulose Nanoparticles and Microparticles for Oral Delivery

Research Center for Nanoscience and Technology, Department of Biochemistry, P.G. Centre, Kuvempu University Shivagangotri, Davangere 577002, India

B. Madhusudhan

Research Center for Nanoscience and Technology, Department of Biochemistry, P.G. Centre, Kuvempu University Shivagangotri, Davangere 577002, India, basavaraj_madhu{at}hotmail.com

T.S. Nagaraj

SJM College of Pharmacy, Chitradurga 577502, India

Shobarani R. Hiremat

Department of Clinical Pharmacy Practice, Al-Ameen College of Pharmacy, Bangalore 560027, India

Gargi Raina

Nanotechnology Lab, School of Electrical Sciences, VIT Vellore 632014, Tamil Nadu, India

The present study was designed to assess and compare with a range of surfactant-coated, nimesulide-free, and nimesulide-loaded ethylcellulose/methylcellulose (EC/MC) nanoparticles that were prepared by varying drug concentration (ED/MD), polymer concentration (EP/MP), and surfactant concentration (ES/MS). EC/MC nanoparticles prepared by desolvation method produced discrete particles and they were characterized by SEM, AFM, and FTIR studies. The particles mean size diameter (nm) ranged from 244 to 1056 nm and 1065 to 1710 nm for EC and MC nanoparticles, respectively. Studies on drug: polymer ratio showed a linear relationship between drug concentration and percentage of loading in nanoparticles. The encapsulation efficiency decreased with the increase of nimesulide concentration with respect to polymer concentration. Encapsulation efficiency of drug-loaded nanoparticles was varied between 32.8% and 64.9%. The in vitro release of drug-loaded nanoparticles was found to be a first order. This was significantly increased in EC nanoparticles (95.50%) in comparison with MC nanoparticles (95.12%) after 12 h in 24 h long study. Nimesulide release from EC nanoparticles was much slower at slightly alkaline pH 7.4. The in vitro hemolysis tests of nanoparticles were carried out to ascertain the hemocompatibility and shown to be insignificant for EC nanoparticles. In comparison, ES4 from EC formulations with nimesulide was found to be promising with slow and sustained drug release.

Key Words: ethylcellulose • methylcellulose • desolvation method • drug encapsulation • release efficiency • hemolysis.

This version was published on July 1, 2009

Journal of Biomaterials Applications, Vol. 24, No. 1, 47-64 (2009)
DOI: 10.1177/0885328209103406


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