Production of aceclofenac-loaded sustained release micro/nanoparticles using pressure homogenization and spray drying

ABSTRACT

The aim of the present study was to characterize polymeric micro/nanoparticles of aceclofenac produced using a high-pressure homogenizer and a spray dryer. The micro/nanoparticles were characterized in terms of their encapsulation efficiency (E.E.), particle size, morphology, and in vitro drug release performance. Interaction between the drug and the polymer (Eudragit RS 100 and ethylcellulose) was evaluated using Fourier transform infrared (FTIR) spectroscopy and X-ray powder diffractometry. Analysis of the results showed that speed and operating pressure have significant negative effect on E.E. of the micro/nanoparticles. The nanoparticles (970–197 nm) had E.E. of 74.09 ± 1.17 to 83.66 ± 1.63% while microparticles displayed EE. of 72.15 ± 2.5%. The micro/nanoparticles were observed to be discrete and spherical. The FTIR analysis confirmed compatibility of aceclofenac with Eudragit RS 100 as well as ethylcellulose. In vitro study showed sustained drug release of 65 and 90% over a period of 12 h, thus prolonging the drug activity to treat the musculoskeletal disorder.

KEYWORDS:

• Drug release
• high pressure homogenization
• micro/nanoparticles
• spray drying
• statistical experimental design

Acknowledgments

The authors want to express their sincere thanks to University Grants Commission, New Delhi, India for financial support (F. No. 37-276/2009 and No. F. 4-1/2006 (BSR)/11-58/2008 (BSR) - RFSMS fellowship). Authors are very much thankful to Natco Pharma Limited, (Hyderabad, India), Evonik Degussa India Pvt. Ltd. (Mumbai, India), and Colorcon India Pvt. Ltd. (Mumbai, India) for providing the gift sample of aceclofenac, Eudragit® RS 100 and EC, respectively.