EXPLORING THE POTENTIAL OF EUDRAGIT FOR DEVELOPMENT OF MICROPARTICLES OF WATER SOLUBLE DRUG USING QUALITY BY DESIGN APPROACH

  • SHAILESH SHARMA Pharmaceutical Research Department, ASBASJSM College of Pharmacy, Bela, Punjab, India
  • NIMRATA SETH Department of Pharmaceutics, Rayat Institute of Pharmacy, Railmajra, S. B. S. Nagar, Punjab, India

Abstract

Objective: In the present protocol, employability of polymethacrylate polymer Eudragit RS100 for development of microparticles of water soluble drug with desired values of response variables was investigated by central composite optimization design through application of Design Expert® software (Series DX10).


Methods: The microparticles were developed by emulsion solvent evaporation process employing Eudragit RS100. Two effective independent variables drug: polymer ratio and stirring speed were selected to assess performance prospective of Eudragit on mean particle size, entrapment efficiency, percent yield and drug release in 12 h of microparticles. Thirteen batches generated by software were prepared and subjected to different characterization test parameters obligatory for the evaluation of formulation. Validation of optimization model and Statistical interpretation of results was done using Analysis of Variance (ANOVA)


Results: ANOVA indicated that the independent variables had significant effect on response variables. Optimized formulation demonstrated close agreement amongst experimental and predicted responses with high desirability factor. In vitro drug liberation study for optimized formulation proposed a sustained release of drug from microparticles.


Conclusion: In conclusion, optimization technique was imperative in indicating the efficient applicability of Eudragit RS100 polymer in controlling the drug release of hydrophilic drugs.

Keywords: Microparticles, Eudragit RS100, Optimization, Central composite design

References

1. Nagarwal RC, Srinatha A, Pandit JK. In-situ forming formulation: Development, evaluation and optimization using 33 factorial design. AAPS PharmSciTech 2009;10:977-84.
2. Bas D, Boyaci IH. Modeling and optimization: usability of response surface methodology. J Food Eng 2007;78:836-45.
3. Chopra S, Patil GV, Motwani SK. Release modulating hydrophilic matrix systems of Losartan potassium: optimization of formulation using statistical experimental design. Eur J Pharm Biopharm 2007;66:73-82.
4. Kehoe S, Kilcup N, Boyd D. Evaluation of cytotoxicity for novel composite microspheres: material optimization by response surface methodology. Matter Lett 2012;86:13-7.
5. Martins SA, Prazerers DM, Fonseca LP, Monteiro GP. Application of central composite design for DNA hybridization onto magnetic micropsheres. Anal Biochem 2009;391:17-23.
6. Montgomery DC. Introduction to statistical quality control. 6th ed. John Wiley and Sons: New York; 2008.
7. Das SK, Yuvaraj K, Khanam J, Nanda A. Formulation development and statistical optimization of ibuprofen-loaded polymethacrylate microspheres using response surface methodology. Chem Eng Res Design 2015;96:1-14.
8. Deshmukh RK, Naik JB. The impact of preparation parameters on sustained release aceclofenac microspheres: design of experiments. Adv Powder Tech 2015;26:244-52.
9. Wu PC, Huang YB, Chang JS, Tsai MJ. Design and evaluation of sustained release microspheres of potassium chloride prepared by Eudragit. Eur J Pharm Sci 2003;19:115-22.
10. Barzegar Jalali M, Alaei Beirami M, Javadzadeh Y, Mohammadi G, Hamidi A, Andaiib S, et al. Comparison of physicochemical characteristics and drug release of diclofenac sodium Eudragit RS100 nanoparticles and solid dispersion. Powder Technol 2012;219:211-6.
11. Phutane P, Shidhaye S, Lotokar V, Gule A, Sutar S, Kadam V. In vitro evaluation of novel sustained release microspheres of Glipizide prepared by emulsion solvent diffusion evaporation method. J Young Pharma 2010;2:35-9.
12. Hanan M, EL Nanhas. Optimization of eudragit RS microspheres for controlled release of theophylline using response surface methodology. J Pharm Sci Res 2010;2:663-71.
13. Lee JH, Park TG, Choi HK. 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. Int J Pharm 2000;196:75-83.
14. Sunitha S, Amareshwar P, Santhosh KM. A study on the effect of different cellulose polymers on release rate from tramadol loaded microspheres prepared by emulsion solvent evaporation method. Asian J Pharm Clin Res 2010;3:35-9.
15. Myers RH, Montgomery DC, Anderson Cook CM. Response surface methodology. In: Process and product optimization using designed experiments. 3rd ed. John Wiley and Sons: Hoboken; 2009.
16. Sinko PJ. Martin’s physical pharmacy and pharmaceutical sciences. 6th ed. New Delhi: BI Publications Pvt. Ltd; 2006.
17. Tanwar YS, Naruka P, Ojha GR. Development and evaluation of microspheres of verapamil hydrochloride. Braz J Pharm Sci 2006;43:529-34.
18. Trivedi P, Verma AML, Garud N. Preparation and characterization of aceclofenac microspheres. Asian J Pharm 2008;2:110-5.
19. Tayade PT, Kale RD. Encapsulation of water-insoluble drug by cross-linking technique: effect of process and formulation variables on encapsulation efficiency, particle size and in vitro dissolution rate. AAPS Pharm Sci 2004;6:1-8.
20. Arindam H, Biswanath S. Preparation and in vitro evaluation of polystyrene coated microcapsule of the drug-resin complex for achieving prolonged release of diltiazem hydrochloride. AAPS PharmSciTech 2006;7:34-49.
21. Durgapal S, Mukhopadhyay S, Goswami L. Preparation, characterization and evaluation of floating microparticles of ciprofloxacin. Int J Appl Pharm 2017;9:1-8.
22. Augustijns P. In vitro dissolution models for prediction of in vivo performance of oral dosage forms. Eur J Pharm Sci 2014;57:342-66.
23. Raslan HK, Maswadeh H. In vitro dissolution kinetic study of theophylline from mixed controlled release matrix containing HPMC and glyceryl behenate. Ind J Pharm Sci 2006;68:308-12.
24. Zaslavaskaia RM. Controlled release approach to novel multiparticulate drug delivery system. Int J Pharm Pharm Sci 2012;4:757-63.
25. Kilicarslan M, Baykara T. The effect of the drug/polymer ratio on the properties of the verapamil HCl loaded microspheres. Int J Pharm 2003;252:99-109.
26. Singh S, Arora S, Neelam, Allawadi D. Formulation, optimization and evaluation of sustained release microspheres using Taguchi design. J Pharm Tech Res Mgnt 2014;2:253-64.
27. Malladi M, Jukanti R. Floating pulsatile drug delivery system of Famotidine: design, statistical optimization, and in vitro evaluation. Int J Pharm Pharm Sci 2016;8:169-81.
28. Maiti S, Dey P, Biswanath SA, Ray S. Influence of microenvironmental pH of alginate facilitated ethyl cellulose microspheres on entrapment efficiency and release characteristics of fluconazole. Int J Curr Pharm Res 2010;2:17-23.
Statistics
44 Views | 61 Downloads
Citatons
How to Cite
SHARMA, S., & SETH, N. (2019). EXPLORING THE POTENTIAL OF EUDRAGIT FOR DEVELOPMENT OF MICROPARTICLES OF WATER SOLUBLE DRUG USING QUALITY BY DESIGN APPROACH. International Journal of Applied Pharmaceutics, 11(4), 110-116. https://doi.org/10.22159/ijap.2019v11i4.32816
Section
Original Article(s)