JOURNAL OF THE CZECH PHARMACEUTICAL SOCIETY AND THE SLOVAK PHARMACEUTICAL SOCIETY

Čes. slov. farm. 2017, 66(6):274-280 | DOI: 10.36290/csf.2017.039

The size-reduced Eudragit® RS microparticles prepared by solvent evaporation method - monitoring the effect of selected variables on tested parameters

Kalliopi Vasileiou1, Jakub Vysloužil1,*, Miroslava Pavelková1, Jan Vysloužil2, Kateřina Kubová1
1 Department of Pharmaceutics, Faculty of Pharmacy, University of Veterinary and Pharmaceutical Sciences, Brno, Czech Republic
2 Department of Biochemistry, Faculty of Science, Masaryk University, Brno, Czech Republic

Size-reduced microparticles were successfully obtained by solvent evaporation method. Different parameters were applied in each sample and their influence on microparticles was evaluated. As a model drug the insoluble ibuprofen was selected for the encapsulation process with Eudragit® RS. The obtained microparticles were inspected by optical microscopy and scanning electron microscopy. The effect of aqueous phase volume (600, 400, 200 ml) and the concentration of polyvinyl alcohol (PVA; 1.0% and 0.1%) were studied. It was evaluated how those variations and also size can affect microparticle characteristics such as encapsulation efficiency, drug loading, burst effect and microparticle morphology. It was observed that the sample prepared with 600 ml aqueous phase and 1% concentration of polyvinyl alcohol gave the most favorable results.

Keywords: microparticles; solvent evaporation; sustained drug release; Eudragit RS®

Received: August 23, 2017; Accepted: November 11, 2017; Published: June 1, 2017  Show citation

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Vasileiou K, Vysloužil J, Pavelková M, Vysloužil J, Kubová K. The size-reduced Eudragit® RS microparticles prepared by solvent evaporation method - monitoring the effect of selected variables on tested parameters. Čes. slov. farm. 2017;66(6):274-280. doi: 10.36290/csf.2017.039.
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    References

    1. Panicker Varuna P., Anu Gopalakrishnan. Advances in drug delivery systems 2014.
    2. Schmidt C., et al. Nano-and microscaled particles for drug targeting to inflamed intestinal mucosa - A first in vivo study in human patients. Journal of controlled release 2013; 165(2), 139-145. Go to original source... Go to PubMed...
    3. Chowdhury S., et al. An overview of drug delivery vehicles for cancer treatment: Nanocarriers and nanoparticles including photovoltaic nanoparticles. Journal of Photochemistry and Photobiology B: Biology 2016; 164, 151-159. Go to original source... Go to PubMed...
    4. Campos E., et al. Designing polymeric microparticles for biomedical and industrial applications. European Polymer Journal 2013; 49(8), 2005-2021. Go to original source...
    5. Beck L. R., Cowsar D. R., Lewis D. H., Gibson J. W., Flowers C. E. New long-acting injectable microcapsule contraceptive system. Am J Obstet Gynecol. 1979; 135, 419-426. Go to original source... Go to PubMed...
    6. Iqbal M., Zafar N., Fessi H., Elaissari A. Double emulsion solvent evaporation techniques used for drug encapsulation. International journal of pharmaceutics 2015; 496(2), 173-190. Go to original source... Go to PubMed...
    7. Padalkar A. N., Sadhana R. S., Thube M. W. Microparticles: an approach for betterment of drug delivery system. Int. J. Pharm. Res. Dev. 2011; 1, 99-115.
    8. Iqbal M., et al. Double emulsion solvent evaporation techniques used for drug encapsulation. International journal of pharmaceutics 2015; 496(2), 173-190. Go to original source... Go to PubMed...
    9. Bodmeier R., McGinity J. W. Solvent selection in the preparation of poly (DL-lactide) microspheres prepared by the solvent evaporation method. International journal of pharmaceutics 1988; 43(1-2), 179-186. Go to original source...
    10. Patel R. S., et al. Doxycycline delivery from PLGA microspheres prepared by a modified solvent removal method. Journal of microencapsulation 2012; 29(4), 344-352. Go to original source... Go to PubMed...
    11. Han N. S., Basri M., Abd R. M., Abd R. R., Salleh A. B., Ismail Z. Preparation of emulsions by rotor-stator homogenizer and ultrasonic cavitation for the cosmeceutical industry. Journal of cosmetic science 2012; 63(5), 333-344.
    12. Kim K. K., Pack D. W. Microspheres for drug delivery. BioMEMS and Biomedical Nanotechnology. Springer US 2006; 19-50. Go to original source...
    13. O'Donnell P. B., McGinity J. W. Preparation of microspheres by the solvent evaporation technique. Advanced drug delivery reviews 1997; 28(1), 25-42. Go to original source... Go to PubMed...
    14. Gentile P., et al. Localised controlled release of simvastatin from porous chitosan-gelatin scaffolds engrafted with simvastatin loaded PLGA-microparticles for bone tissue engineering application. Materials Science and Engineering: C 59 2016; 249-257. Go to original source... Go to PubMed...
    15. Liu X., Sun Q., Wang H., et al. Microspheres of corn protein, zein, for an ivermectin drug delivery system. Biomaterials 2005; 26, 109-115. Go to original source... Go to PubMed...
    16. Saravanan M., Bhaskar K., Maharajan G., Pillai K. S. Ultrasonicallycontrolled release and targeted delivery of diclofenac sodium via gelatin magnetic microspheres. Int. J. Pharm. 2004; 283, 71-82. Go to original source... Go to PubMed...
    17. Shaikh H. K., Kshirsagar R. V., Patil S. G. Mathematical models for drug release characterization: a review. World J. Pharm. Pharmacent. Sci. 2015; 4, 324-338.
    18. Berkland C., Kim K. K., Pack D. W. PLG microsphere size controls drug release rate through several competing factors. Pharmaceutical research 2003; 20(7), 1055-1062. Go to original source... Go to PubMed...
    19. Esbensen K. H., Guyot D., Westad F., Houmoller L. P. Multivariate data analysis: in practice: an introduction to multivariate data analysisand experimental design. Oslo: CAMO AS Publications 2004.
    20. Jelvehgari M., et al. Control of encapsulation efficiency in polymeric microparticle system of tolmetin. Pharmaceutical development and technology 2010; 15(1), 71-79. Go to original source... Go to PubMed...
    21. Capan Y., Woo B. H., Gebrekidan S., Ahmed S., DeLuca P. P. Influence of formulation parameterson the characteristics of poly(D, L-lactide-co-glycolide) microspheres containing poly(L-lysine)complexed plasmid DNA, J. Control. Release 1999; 60, 279-286. doi: 10.1016/S0168-3659(99)00076-0 Go to original source... Go to PubMed...
    22. Mao S., Shi Y., Li L., Xu J., Schaper A., Kissel T. Effects of process and formulation parameterson characteristics and internal morphology of poly(d,l-lactide-co-glycolide) microspheres formedby the solvent evaporation method. Eur. J. Pharm. Biopharm. 2008; 68, 214-223. doi: 10.1016/j.ejpb.2007.06.008 Go to original source... Go to PubMed...
    23. Chen W., Palazzo A., Hennink W. E., Kok R. J. The effect of particle size on drug loading and release kinetics of gefitinib-loaded PLGA microspheres. Molecular Pharmaceutics 2016. Go to original source... Go to PubMed...
    24. Čalija B. (ed.) Microsized and nanosized carriers for nonsteroidal anti-inflammatory drugs: formulation challenges and potential benefits. Academic Press 2017.
    25. Thies C. Microcapsules and nanoparticles in medicine and pharmacy. Boca Raton: CRC press 1992.
    26. O'Donnell P. B., McGinity J. W. Preparation of microspheres by the solvent evaporation technique. Adv. Drug Deliv. Rev. 1997; 28, 25-42. doi: 10.1016/S0169-409X(97)00049-5 Go to original source... Go to PubMed...
    27. Freiberg S., Zhu X. X. Polymer microspheres for controlled drug release. International journal of pharmaceutics 2004; 282(1), 1-18. Go to original source... Go to PubMed...
    28. Yan Ch., et al. Characterization and morphological analysis of protein-loaded poly (lactide-co-glycolide) microparticles prepared by water-in-oil-in-water emulsion technique. Journal of Controlled Release 1994; 32(3), 231-241. Go to original source...
    29. Khan A. U., Nasir M. A., Nasir M. Rheological studies on stabilised zirconia aqueous suspensions. Journal of Colloid Science and Biotechnology 2012; 1(2), 175-184. Go to original source...
    30. Ibraheem D., et al. Effects of process parameters on the colloidal properties of polycaprolactone microparticles prepared by double emulsion like process. Colloids and Surfaces A: Physicochemical and Engineering Aspects 2014; 445, 79-91. Go to original source...
    31. Cai Y., Chen Y., Hong X., Liu Z., Yuan W. Porous microsphere and its applications. International journal of nanomedicine 2013; 8: 1111. Go to original source... Go to PubMed...
    32. Mao S., et al. Effect of WOW process parameters on morphology and burst release of FITC-dextran loaded PLGA microspheres. International journal of pharmaceutics 2007; 334(1), 137-148. Go to original source... Go to PubMed...
    33. Nath, Bipul, Lila Kanta Nath, Pradeep Kumar. Preparation and in vitro dissolution profile of zidovudine loaded microspheres made of Eudragit RS 100, RL 100 and their combinations. Acta Pol Pharm 2011; 68(3), 409-415.
    34. Yeo Y, Park K. Control of encapsulation efficiency and initial burst in polymeric microparticle systems. Archives of pharmacal research 2004; 27(1), 1. Go to original source... Go to PubMed...
    35. Huang X., Brazel C. S. On the importance and mechanisms of burst release in matrix-controlled drug delivery systems, J. Control. Release 2001; 73, 121-136. Go to original source... Go to PubMed...
    36. Huang X., Brazel C. S. On the importance and mechanisms of burst release in matrix-controlled drug delivery systems. Journal of controlled release 2001; 73(2), 121-136. Go to original source... Go to PubMed...
    37. Yang Yi-Yan, et al. Effect of preparation conditions on morphology and release profiles of biodegradable polymeric microspheres containing protein fabricated by double-emulsion method. Chemical Engineering Science 2000; 55(12), 2223-2236. Go to original source...
    38. Ramirez L. Biodegradable poly (DL-lactic-co-glycolic acid) microspheres containing tetracaine hydrochloride. In-vitro release profile. Journal of microencapsulation 1999; 16(1), 105-115. Go to original source... Go to PubMed...
    39. Herrero-Vanrell R., Refojo M. F. Biodegradable microspheres for vitreoretinal drug delivery. Advanced drug delivery reviews 2001; 52(1): 5-16. Go to original source... Go to PubMed...
    40. Yin C., Li X. Anomalous diffusion of drug release from a slab matrix: Fractional diffusion models. International journal of pharmaceutics 2011; 418(1), 78-87. Go to original source... Go to PubMed...
    41. Akhgari A., Tavakol A. Prediction of optimum combination of Eudragit RS/Eudragit RL/ethyl cellulose polymeric free films based on experimental design for using as a coating system for sustained release theophylline pellets. Advanced pharmaceutical bulletin 2016; 6(2), 219. Go to original source... Go to PubMed...

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