Impact of formulation and process parameters on the properties of chitosan-based microspheres prepared by external ionic gelation
Authors:
Romana Kubánková; Jakub Vysloužil; Martina Kejdušová; David Vetchý; Kateřina Dvořáčková
Published in:
Čes. slov. Farm., 2014; 63, 127-135
Category:
Original Articles
Overview
The aim of this experimental study was to optimize a preparation of microspheres from high viscosity chitosan by external ion gelation and to evaluate selected aspects of their preparation. For drug-free microparticles, the concentration of chitosan dispersions was chosen as a formulation variable; the position of instrument for a dispersion extrusion (horizontal vs. vertical) was evaluated as a process variable. On the basis of sphericity and equivalent diameter results, three different concentrations of chitosan dispersions were used for 5-aminosalicylic acid (5-ASA) encapsulation with the extrusion instrument in horizontal position, which was considered as the optimal. In consequent drug-loaded microparticle preparation, the influence of the concentration of chitosan dispersions and composition of hardening solution (10% sodium tripolyphosphate (TPP) vs. 10% TPP containing drug) was evaluated. In prepared 5-ASA microspheres it was found that the equivalent diameter increased with increasing chitosan concentration. In the case of sphericity, significant differences were not found. Samples prepared with the drug in both chitosan dispersion and hardening solution had a higher drug content, a smaller equivalent diameter and they showed a faster in vitro drug release in comparison with the samples prepared with the drug in chitosan dispersion only.
Keywords:
microparticles • external ionic gelation • chitosan • formulation and process parameters • dissolution profile
Sources
1. Park J., Ye M., Park K. Biodegradable polymers for microencapsulation of drugs. Molecules 2005; 10, 146–161.
2. Yen M. T., Yang J. H., Mau J. L. Antioxidant properties of chitosanu from crab shells. Carbohydr. Polym. 2008; 74, 840–844.
3. Croisier F., Jérôme Ch. Chitosan-based biomaterials for tissue engineering. Eur. Polym. J. 2013; 49, 780–792.
4. Singla A. K., Chawla M. Chitosan: some pharmaceutical and biological aspects - an update. J. Pharm. Pharmacol. 2001; 53, 1047–1067.
5. Ilium L. Chitosan and its use as a pharmaceutical excipient. Pharmaceut. Res. 1998; 15, 1326–1331.
6. Meng-Lund E., Muff-Westergaard Ch., Sander C., Madelung P., Jacobsen J. A mechanistic based approach for enhancing buccal mucoadhesion of chitosanu. Int. J. Pharm. 2014; 461, 280–285.
7. Bravo-Osuna I., Vauthier Ch., Farabollini A., Palmieri G. F., Ponchel G. Mucoadhesion mechanism of chitosan and thiolated chitosan-poly(isobutyl cyanoacrylate) core-shell nanoparticles. Biomaterials 2007; 28, 2233–2243.
8. Yang T. C., Chou C. C., Li C. F. Antibacterial aktivity of N-alkylated disacharide chitosan derivatives. Int. J. Food Microbiol. 2005; 97, 237–245.
9. Dehghani F., Hoseini M. H. M., Memarnejadian A., Yeganeh F., Rezaie A. M., Khaze V., Sattari M., Darbandi Tamijani H., Labibi F., Mossaffa N. Immunomodulatory activities of chitin microparticles on Leishmania major-infected murine macrophages: interaction with a bacterial membrane model. Arch. Med. Res. 2011; 42, 572–576.
10. Baldrick P. The safety of chitosan as a pharmaceutical excipient. Regul. Toxicol. Pharm. 2010; 56, 290–299.
11. Evans J. R., Davids W. G., MacRae J. D., Amirbahman A. Kinetics of kadmium uptake by chitosan-based crab shells. Water Res. 2002; 36, 3219–3226.
12. Pusateri A. E., McCarthy S. J., Gregory K. W., Harris R. A., Cardenas L., McManus A. T., Goodwin C. W. Effect of a chitosan-based hemostatic dressing on blood loss and survival in a model of severe velus hemorrhage and hepatic injury in swine. J. Trauma 2003; 54, 177.
13. Wassmer S., Rafat M., Fong W. G., Baker A. N., Tsilfidis C. Chitosan microparticles for delivery of proteins to the retina. Acta Biomater. 2013; 9, 7855–7864.
14. Keegan G. M., Smart J. D., Ingram M. J., Barnes L.-M., Burnett G. R., Rees G. D. Chitosan microparticles for the controlled delivery of fluoride. J. Dent. 2012; 40, 229–240.
15. Bajerová M., Gajdziok J., Dvořáčková K., Masteiková R., Rabišková M. Metody přípravy mikročástic ve farmaceutické technologii. Čes. slov. Farm. 2009; 58, 191–199.
16. Lamprecht A., Torres H. R., Schäfer U., Lehr C. M. Biodegradable microparticles as a two-drug controlled release formulation: a potential treatment of inflammatory bowel disease. J. Control. Release 2000; 69, 445–454.
17. Rabišková M., Bautzová T., Gajdziok J., Dvořáčková K., Lamprecht A., Pellequer Y., Spilková J. Coated chitosanu pellets containing rutin intended for the treatment of inflammatory bowel disease: in vitro characteristics and in vivo evaluation. Int. J. Pharm. 2012; 422, 151–159.
18. Garekani H. A., Moghaddam Z. F., Sadeghi F. Organic solution versus aqueous dispersion of Eudragit RS in preparation of sustained release microparticles of theophylline using spray drying. Colloid Surface B. 2013; 108, 374–379.
19. Vysloužil J., Kejdušová M., Dvořáčková K., Vetchý D. Influence of formulation and process parameters on the characteristics of P LGA-based microparticles with controlled drug release. Čes. slov. Farm. 2013; 62, 120–126.
20. Bajerová M., Dvořáčková K., Gajdziok J., Masteiková R. Mikročástice na bázi oxycelulosy – vliv procesních proměnných na enkapsulační účinnost. Čes. slov. Farm. 2010; 59, 67–73.
21. Shu X. Z., Zhu K. J. A novel approach to prepare tripolyphosphate/chitosanu komplex beat for controlled release drug delivery. Int. J. Pharm. 2000; 201, 51–58.
22. Mi F. L., Sung H. W., Shyu S. S., Su C. C., Peng C. K. Synthesis and characterization of biodegradable TPP/genipin co-crosslinked chitosan gel beads: a new matrix for controlled release of pindolol. Polymer 2003; 44, 6521–6530.
23. Lemoine D., Wauters F., Bouchend’homme S., Préat V. Preparation and characterization of alginate microspheres containing a model antigen. Int. J. Pharm. 1998; 176, 9–19.
24. Narra K., Dhanalekshmi U., Rangaraj G., Raja D., Kumar C. S., Reddy P. N., Mandal A. B. Effect of formulation variables on rifampicin loaded alginate beads. Iran. J. Pharm. Res. 2012; 11, 715–721.
25. Siso M. I. G., Lang E., Carrenõ-Gómez B., Becerra M., Espinar F. O., Méndez J. B. Enzyme encapsulation on chitosan microbeads. Process Biochem. 1997; 32, 211–216.
26. Chan E.-S., Lee B.-B., Ravindra P., Poncelet D. Prediction models for shape and size of ca-alginate macrobeads produced through extrusion-dripping method. J. Colloid Interf. Sci. 2009; 338, 63–72.
27. Patel Y. L., Sher P., Pawar A. P. The effect of drug concentration and curing time on processing and properties of calcium alginate beads containing metronidazole by response surface metodology. AAPS Pharm. Sci. Tech. 2006; 7, E24–E30.
28. 5-Aminosalicylic acid.: Santa Cruz Biotech [online]. [cit. 2013-08-18]. Dostupné z: http://www.scbt.com/datasheet-202890-5-aminosalicylic-acid.html.
29. Smýkalová I., Horáček J., Hýbl M., Bjelková M., Pavelek M., Krulikovská T., Hampel D. Posuzování tvarových a barevných charakteristik semen modelových plodin i v korelaci s jejich obsahovými látkami. Chem. Listy 2011; 105, 138–145.
30. Desai K. G. H., Park H. J. Preparation and characterization of drug-loaded chitosan–tripolyphosphate microspheres by spray drying. Drug Develop. Res. 2005; 64, 114–128.
31. Bajerová M., Dvořáčková K., Gajdziok J., Masteiková R. Mikročástice na bázi oxycelulosy – vliv procesních proměnných na enkapsulační účinnost. Čes. slov. Farm. 2010; 59, 67–73.
32. Cho J., Heuzey M. C., Bégin A., Carreau P. J. Viscoelastic properties of chitosanu solutions: Effect of concentration and ionic strength. J. Food Eng. 2006; 74, 500–515.
33. Mura C., Nácher A., Merino V., Merino-Sanjuán M., Manconi M., Loy G., Fadda A. M., Díez-Sales O. Design, characterization and in vitro evaluation of 5-aminosalicylic acid loaded N-succinyl-chitosan microparticles for colon specific delivery. Colloid Surface B. Biointerfaces 2012; 94, 199–205.
34. Ouwerx C., Velings N., Mestdagh M. M., Axelos M. A. V. Physico-chemical properties and rheology of alginate gel beads formed with various divalent cations. Polym. gels Netw. 1998; 6, 393–408.
35. Ko J. A., Park H. J., Hwang S. J., Park J. B., Lee J. S. Preparation and characterization of chitosanu microparticles intended for controlled drug delivery. Int. J. Pharm. 2002; 249, 165–174.
36. Chen Ch. T., Maa J. R., Yang Y. M., Chang Ch. H. Drop formativ from flat tip nozzles in liquid-liquid systém. Int. Commun. Heat Mass 2001; 28, 681–692.
37. Yeom S., Lee S. Y. Dependence of micro-drop generation performance on dispenser geometry. Exp. Therm. Fluid Sci. 2011; 35, 1565–1574.
38. Lupo B., Maestro A., Porras M., Gutiérrez J. M., González C. Preparation of alginate microspheres by emulsification/internal gelation to encapsulate cocoa polyphenols. Food hydrocolloid. 2014; 38, 56–65.
39. Das S., Chaudhury A., Ng K. Y. Preparation and evaluation of zinc-pectin-chitosanu composite particles for drug delivery to the colon: Role of chitosan in modifying in vitro and in vivo drug release. Int. J. Pharm. 2011; 406, 11–20.
40. Shu X. Z., Zhu K. J. Controlled drug release properties of ionically cross-linked chitosan beads: the influence of anion structure. Int. J. Pharm. 2002; 233, 217–225.
41. Smrdel P., Bogataj M., Zega A., Planinšek O., Mrhar A. Shape optimization and characterization of polysaccharide beads prepared by ionotropic gelation. J. Microencapsul. 2008; 25, 90–105.
42. Sezer A. D., Akbuga J. Controlled release of piroxicam from chitosan beads. Int. J. Pharm. 1995; 121, 113–116.
43. Berger J., Reist M., Mayer J. M., Felt O., Peppas N. A., Gurny R. Structure and interactions in covalently and ionically crosslinked chitosan hydrogels for biomedical applications. Eur. J. Pharm. Biopharm. 2004; 57, 19–34.
44. Nandi S., Winter H. H. Swelling behavior of partially cross-linked polymers: A ternary system. Macromolecules 2005; 38, 4447–4455.
45. Aranaz I., Mengíbar M., Harris R., Paños I., Miralles B., Acosta N., Galed G., Heras Á. Functional characterization of chitin and chitosan. Curr. Chem. Biol. 2009; 3, 203–230.
46. Vaghani S. S., Patel M. M., Satish C. S. Synthesis and characterization of pH-sensitive hydrogel composed of carboxymethyl chitosan for colon targeted delivery of ornidazole. Carbohyd. Res. 2012; 347, 76–82.
47. Chiou S.-H., Wu W.-T., Huang Y.-Y., Chung T.-W. Effects of the characteristics of chitosan on controlling drug release of chitosan coated PLLA microspheres. J. Microencapsulation. 2001; 18, 613–625.
48. Kouřil J., Vysloužil J., Kejdušová M., Dvořáčková K., Vetchý D. Možnosti ovlivnění obsahu léčiva a enkapsulační účinnosti chitosanových mikrosfér připravených procesem iontové gelace. Čes. slov. Farm. 2014; 63, 75–83.
49. Williams C., Panaccione R., Ghosh S., Rioux K.: Optimizing clinical use of mesalazine (5-aminosalicylic acid) in inflammatory bowel disease. Therap. Adv. Gastroenterol. 2011; 4, 237–248.
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Pharmacy Clinical pharmacologyArticle was published in
Czech and Slovak Pharmacy
2014 Issue 3
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