J. Pharm. Technol. Res. Manag.

Formulation, Optimization and Evaluation of Sustained Release Microspheres using Taguchi Design

Sukhbir singh, Sandeep Arora, Neelam and Dharna Allawadi

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Taguchi, Response Variables, Independent Variables, Drug Entrapment Efficiency, Drug Loading, Higuchi Model.

PUBLISHER The author(s) 2014. This article is published with open access at www.chitkara.edu.in/publications

The aim of present study is to prepare microspheres of eudragit RL 100 loaded with Nefopam Hydrochloride by single emulsion solvent evaporation technique. Taguchi L9 orthogonal array design has been used to optimize the composition and operating conditions for preparation of formulations. Nine batches (F1-F9) were prepared by taking three independent variables (X1- drug: polymer ratio, X2- stirring speed and X3- stirring time) at three levels (+1, 0, -1). Response variables studied for batches (F1-F9) were mean particle size (μm) (Y1), drug entrapment efficiency (% w/w) (Y2) and drug loading (% w/w) (Y3). Drug- polymer compatibility study was carried out by DSC and FTIR spectroscopy and indicates no physicochemical interaction. Microspheres were analyzed for morphological characteristics, mean particle size, drug entrapment efficiency, drug loading and in-vitro drug release. Percentage cumulative drug release for optimized batch F5 was found to be 85.421 ± 0.054 and followed higuchi model for release of drug.

Page(s) 1–12
URL http://dspace.chitkara.edu.in/jspui/bitstream/1/506/1/21001_JPTRM_Sukhbir%20Singh.pdf
ISSN Print : 2321-2217, Online : 2321-2225
DOI https://doi.org/10.15415/jptrm.2014.21001
  • Alfonsi, P. Adam, F. Assard, A. Guignard, B. Sessler, D. I. and Chauvin, M. (2004) ‘Nefopam, a Non-sedative Benzoxazocine Analgesic, Selectively Reduces the Shivering Threshold’.Anesthesiology, 100, 1, 37–43.
  • Arindam, H. and Biswanath, S. (2006) ‘Preparation and In-vitro evaluation of Polystyrene-Coated (PS-coated) microcapsule of drug-resin complex for achieving prolonged release of Diltiazem Hydrochloride’. AAPS PharmSciTech , 7, 2, 34-49. DOI: 10.1208/pt070246
  • Aymard, G. Warot, D. and Demolis, P. (2003) ‘Comparative pharmacokinetics and pharmacodynamics of intravenous and oral nefopam in healthy volunteers’. Pharmacoogy & Toxicology , 92, 279-86.DOI: 10.1034/j.1600-0773.2003.920605.x
  • Barratt, G. M. (2000) ‘Therapeutic applications of colloidal drug carriers’. Pharmaceutical Science and Technology Today , 3, 5, 163-171. DOI: 10.1016/S1461-5347(00)00255-8
  • Costa, P. Manuel, J. and Lobo, S. (2001) ‘Modeling and comparison of dissolution profiles’. European Journal of Pharmaceutical Sciences, 13, 123–133. DOI: 10.1016/S0928-0987(01)00095-1
  • Das, S. K. and Das, N. G. (1998) ‘Preparation and in-vitro dissolution profile of dual polymer (Eudragit RS 100 and RL 100) microparticles of diltiazem hydrochloride’. Journal of Microencapsulation, 15, 445–452. DOI: 10.3109/02652049809006871
  • Del, P. Damodharan, N. Mallick, S. Mukherjee, B. (2009) ‘Development and Evaluation of Nefopam Transdermal Matrix Patch System in Human Volunteers’. Parenteral Drug Association Journal of Pharmaceutical Sciences and Technology, 63, 6, 537-546.
  • Gholap, S. B. Banarjee, S. K. Gaikwad, D.D. Jadhav, S. L. and Thorat, R.M. (2010) ‘Hollow Microsphere: A Review’. International Journal of Pharmaceutical Sciences Review and Research, 1, 1, 74-79.
  • Jose, S. Fangueiro, J. F. Smitha, J. Cinu, T. A. Chacko, A. J. Premaletha, K. and Souto, E. B. (2012) ‘Cross-linked chitosan microspheres for oral delivery of insulin: Taguchi design and in vivo testing’. Colloids and Surfaces B: Biointerfaces , 92, 175-179.DOI: 10.1016/j.colsurfb.2011.11.040
  • Kumar, A. and Sharma, P. K. and Banik, A. (2011) ‘Microencapsulation as a novel drug delivery system’. Internationale Pharmaceutia Scientia , 1, 1, 1-7
  • Kumar, R. and Majeti, N. V. (2000) ‘Nano and microparticles as controlled drug delivery devices’. Journal of Pharmacy and Pharmaceutical Sciences, 3, 2, 234-258.
  • Lee, J. H. Park, T. G. and Choi, H. K. (2000) ‘Effect of formulation and processing variables on the characteristics of microspheres for water soluble drugs prepared by w/o/o double emulsion solvent diffusion method’. International Journal of Pharmaceutics 196, 75–83. DOI: 10.1016/S0378-5173(99)00440-8
  • Lewis, G. A. Mathieu, D. and Phan-Tan-Luu, R. (2005) ‘ Pharmaceutical Experimental Design’ (2nd Ed). Marcel Dekker, Inc., New York
  • Myers, R. H. Montgomery, D. C. Anderson-Cook, M. C. (1995) ‘ Response Surface Methodology Process and Product Optimization Using Designed Experiments ’ (3rd Ed). Wiley, New York.
  • Neelesh, K. V. and Daniel, W. P. (2004) ‘Microspheres for controlled release drug delivery’ Expert Opinion on Biological Therapy, 4, 1, 1-17.
  • Phutane, P. Shidhaye, S. Lotikar, V. Ghule, A. Sutar, S. and Kadam, V. (2010) ‘ In-vitro evaluation of Novel Sustained Release Microspheres of Glipzide prepared by the Emulsion Solvent Diffusion- evaporation method’. Journal of Young Pharmacists , 2, 1, 35. DOI: 10.4103/0975-1483.62210
  • Prasanth, V. V. Akash, C. M. Sam, T. M. and Rinku, M. (2011) ‘Microspheres - An Overview’. International Journal of Research in Pharmaceutical and Biomedical Sciences, 2, 2, 332-338
  • Saharan, V. Kukkar, V. Kataria, M. Gera, M. and Choudhury, P. (2009) ‘Dissolution enhancement of drugs. Part I: Technologies and effect of carriers’. International Journal of Health Research, 2,2, 107-124. DOI: 10.4314/ijhr.v2i2.55401
  • Srivastava, A. K. Ridhurkar, D. N. and Wadhwa, S. (2005) ‘Floating Microspheres of Cimetidine: formulation, characterization and in-vitro evaluation. Acta Pharmaceutica , 55, 277–285.
  • Starek, M. Browska, M. D. and Tarsa, M. (2011) ‘Analysis of Nefopam by LC-densitometry. A Study of Degradation Mechanism in Solutions under Stress Conditions’. Acta Chimica Slovenica, 58, 262–269.
  • Taguchi, G. (1987) ‘System of Experimental Design. Engineering Methods to Optimize Quality and Minimize Costs ’. Kraus International, White Plains, New York.
  • Umer, H. Nigam, H. Tamboli, A. M. and Moorthi, M. S. M. (2011) ‘Microencapsulation: process, techniques and applications’. International Journal of Pharmacy Research and Biological Sciences , 2, 2, 474-481.
  • Varshosaz, J. Tavakoli, N. Minayian, M. and Rahdari, N. (2009) ‘Applying the Taguchi Design for Optimized Formulation of Sustained Release Gliclazide Chitosan Beads: An In-Vitro/In-Vivo Study. AAPS PharmSciTech , 10, 1, 158-165. DOI: 10.1208/s12249-009-9191-8