Microparticles on the oxycellulose base – influence of processual variables on encapsulation efficiency

Czech version

Authors: M. Bajerová; K. Dvořáčková; J. Gajdziok; R. Masteiková
Authors‘ workplace: Veterinární a farmaceutická univerzita Brno, Farmaceutická fakulta, Ústav technologie léků
Published in: Čes. slov. Farm., 2010; 59, 67-73
Category: Original Articles

Overview

Microparticles have been a subject of intensive studies in pharmaceutical technology, their encapsulation efficiency being an important parameter in the preparation of microparticles. Higher values of encapsulation efficiency result in a more effective manufacturing process and subsequently in lower economic costs. This study aimed to prepare microparticles with the use of the method of outer gelation of the semisynthetic polymer oxycellulose with diclofenac using sodium salt as the model agent and to examine the influence of selected processual variables on the value of encapsulation efficacy. Processual variables included: the temperature of the hardening solution, the presence of the active ingredient in the hardening solution and the use of ultrasound waves in the process of hardening. The method with the use of which the hardening solution saturated with the active ingredient was cooled to the temperature of 4 °C was selected as the optimal one for the preparation of microparticles on the base of oxycellulose. The combination of these parameters resulted in the highest encapsulation efficiency (batch 4c – 75.24%). Hardening of microparticles by means of ultrasound waves proved to be unsuitable and resulted in a decrease in encapsulation efficiency.

Key words:
microparticles – oxycellulose – outer gelation – encapsulation efficiency – optimization of the process

Sources

1. Manjanna, K. M., Kumar, T. M. P., Shivakumar, B.: Effect of manufacturing conditions on physico-chemical characteristics and drug release profile sof acoclefenac sodium microbeads. Drug InventionToday, 2009; 1(2), 98–107.

2. Park, K., Yeo, Y.: Microencapsulation Technology. In: Swarbrick, J. ed. Encyclopedia of Pharmaceutical Technology, 3rd ed. New York: Marcel Dekker Inc. 2007.

3. Scala Bertola, J., Gajdziok, J., Rabišková, M., Bonneaux, F., Lecompte, T., Sapin, A., Maincent, P.: Pellets for oral administration of low-molecular-weight heparin. Drug Develop. Ind. Pharm., 2009; 35(12), 1503–1510.

4. Rabišková, M.: Částicové lékové formy. Prakt. Lek., 2005; 1, 29–30.

5. Burgess, D. J., Hickey, A. J.: Microsphere Technology and Applications. In: Swarbrick, J., Boylan, J. C. ed. 2nd ed., Encyclopedia of Pharmaceutical Technology. New York: Marcel Dekker Inc. 2002.

6. Mathiowitz, E., Kreitz, M. R., Brannon-Peppas, L.: Microencapsulation. In: Mathiowitz, E. ed. Encyclopedia of Controlled Drug Delivery. New York: John Wiley & Sons, Inc. 1999.

7. Krejčová, K., Gryzcová, E., Rabišková, M.: Polymerové mikročástice pro perorální přívod diklofenaku. Chem. Listy, 2009; 103, 81–87.

8. Fernandes, J. C., Tiera, M. J., Winnik, F. M.: DNA-Chitosan Nanoparticles for Gene Therapy: Current Knowledge and Future Trends. In.: Kumar, Ch. S. S. R. ed. Biological and Pharmaceutical Nanomaterials. 1st ed, Weinheim: WILEY-VCH Verlag GmbH & Co. KGaA 2006.

9. Peretz, S., Cinteza, O.: Removal of some nitrophenol contaminants using alginate gel beat. Colloid Surface A, 2008; 319, 165–172.

10. Thies, C.: Microencapsulation: what it is and purpose. In: Vilstrup, P. ed. Microencapsulation of food ingredients. Surrey: Leathered Publishing, LFRA Lim. 2001.

11. Dulieu, C., Poncelet, D., Neufeld, R. J.: Encapsulation and Immobilization Techniques. In: Kühtreiber W. M., Lanza R. P., Chick W. L. ed. Cell Encapsulation Technology and Therapeutics, Boston: Birkhäuser 1999.

12. Poncelet, D., Markvicheva, E.: Multiple-Core Encapsulation: Microencapsulation and Alginate. In: Thies C., Vilstrup P. ed. Microencapsulation of food ingredients, Surrey: Leathered Publishig LFRA Lim. 2001.

13. Chan, L. W., Lee, H. Y., Heng, P. W. S.: Mechanisms of external and internal gelation and thein impact on the functions of alginate as a coat and delivery system. Carbohyd. Polym., 2006; 63(2), 176–187.

14. Capela, P., Hay, T. K. C., Shah, N. P.: Effect of homogenisation on bead size and survival of encapsulation probiotic bakteria. Food Res. Int., 2007; 40, 1261–1269.

15. Mokarram, R. R., Mortazavi, S. A., Najafi., M. B. N., Shahidi, F.: The influence of multi stage alginate rating on survivability of potential probiotic bakteria in simulated gastrin and intestinal juice. Food Res. Int., 2009; 42, 1040–1045.

16. Jay, S. M., Saltzman, W. M.: Controlled delivery of VEGF via modulation of alginate microparticle ionic crosslinking. J. Control. Release 2009; 134, 26–34.

17. Goppi, G., Sala, N., Bondi, M., Sergi, S., Iannuccelli, V.: Ex-vivo evaluation of alginate microparticles for Polymyxin B oral administration. J. Drug Targeting, 2006; 14(9), 599–606.

18. Agnihotri, S. A., Jawalkar, S. S., Aminabhavi, T. M.: Controlled repase of cephalexin through gellan gum beat: Effect of formulation parameters on entrapment effieciency, size, and drug repase. Eur. J. Pharm. Biopharm., 2006; 63, 249–261.

19. Babu, R. J., Sathigari, S., Kumar, M. T., Pandit, J. K.: Formulation of Controlled Release Gellan Gum Macro Beads of Amoxicillin. Curr. Drug Deliv., 2010; 7, 36–43.

20. Sinha, V. R., Singla, A. K., Wadhawan, S., Kaushik, R., Kumria, R., Bansal, K., Dhawan, S.: Chitosan microspheres as a potential carrier for drugs. Int. J Pharm., 2004; 274, 1–33.

21. Iannuccelli, V., Forni, F., Vandelli, M. A., Bernabei, M. T.: Effect of the loading method on the drug release from crosslinked carboxymethylcellulose bead. J Control. Release, 1993; 23, 13–20.

22. Sankalia, G. M., Mashru, C. R., Sankalia, M. J., Sutariya, B. V.: Stability improvement of alpha-amylase entrapped in kappa-carrageenan beads: Physicochemical characterizatio and optimization using composite index. Int. J. Pharm., 2006; 312, 1–14.

23. Si, L., Zhao, Y., Huang, J., Li, S., Zhai, X., Li, G.: Calcium Pectinate Gel Bead Intended for Oral Protein Delivery: Preparation Improvement and Formulation Development. Chem. Pharm. Bull. Tokyo, 2009; 57, 663–667.

24. Stilwell, R. L., Marks, M. G., Saferstein, L., Wiseman, D. M.: Oxidized Celulose: Chemistry, Processing and Medical Applications. In: Domb A. J., Kost J., Wiseman D. M. ed. Handbook of Biodegradable Polymers. Amsterdam: Harwood academic publishers 1997.

25. Gajdziok, J., Bajerová, M., Chalupová, Z., Masteiková, R.: Oxycelulosa – celulosový derivát s potenciálem účinné i pomocné látky. Ces. slov Farm., 2007; 6, 259–263.

26. Podoczek, F., Newton, J. M.: The evaluation of a three-dimensional shape factor for the quantitative assessment of the sphericity and surface roughness of pellets. Int. J. Pharm., 1995; 124, 253–259.

27. Silva, C. M., Ribeiro, A. J., Figueiredo, I. V., Gronćalves A. R., Veiga, F.: Alginate microspheres prepared by internal gelation: Development and effect on insulin stability. Int. J. Pharm., 2006; 311, 1–10.

28. Giry, K., Viana, M., Genty, M., Louvet, F., Wüthrich, P., Chulia, D.: Comparison of single pot and multiphase granulation. Part I. Effect of the high shear granulator on granule properties according to the drug substance and its concentration. Pharm. Dev. Technol., 2009; 14(2), 139–149.

29. Halder, A., Maiti, S., Sa, B.: Entrapment efficiency and release characteristics of polyethyleneimine-treated or -untreated calcium alginate beads loaded with propranolol-resin complex. Int. J. Pharm., 2005; 302, 84–94.

30. Yu, C.-Y., Yin, B.-Ch., Zhang, W., Cheng, A.-X., Zhang, X.-Z., Zhuo, R.-X.: Composite microparticle drug delivery systems based on chitosan, alginate and pectin with improved pH-sensitive drug release property. Colloid Surface B, 2009; 68, 245–249.

31. Kincl, M., Vrečer, F., Veber, M.: Characterization of factors affecting the repase of low-solubility drug from prolonged repase tablets, Anal. Chim. Acta, 2004; 502, 107–113.

32. Catro, M. D. L., Priego-Capote, F.: Ultrasound-assisted preparation of liquid samples. Talanta, 2007; 72, 321–334.

Labels

Pharmacy Clinical pharmacology

Manufacture of granulates containing high potency drugs

Implementation of radio-frequency identification (RFID) in the process of preparation and administration of drugs – part 2

Identification and susceptibility evaluation of Candida yeasts due to the optimization of ciclopiroxolamine release from mucoadhesive oral tablets

Medicinal preparations in Czech pharmacies at the end of the 17th century

A study of the compaction process and the properties of tablets from two types of directly compressible sorbitol

Article was published in

Czech and Slovak Pharmacy

2010 Issue 2