Preparation of Mucoadhesive Chitosan-Poly(Acrylic acid) Microspheres by Interpolymer Complexation and Solvent Evaporation Method II

  • Cho, Sang-Min (College of Pharmacy, Chosun University) ;
  • Choi, Hoo-Kyun (College of Pharmacy, Chosun University, Research Center for Resistant Cells, Chosun University)
  • Published : 2005.01.01

Abstract

A mucoadhesive microsphere was prepared by an interpolymer complexation and solvent evaporation method, using chitosan and poly(acrylic acid) (PAA), to prolong the gastric resid ence time of the delivery system. The Fourier transform infrared results showed that microspheres were formed by an electrostatic interaction between the carboxyl groups of the PAA and the amine groups of the chitosan. X-ray diffraction and differential scanning calorimetry analysis showed that the enrofloxacin in the chitosan-PAA microsphere was molecularly dispersed in an amorphous state. Scanning electron microscopy of the surface and the quantity of mucin attached to the microspheres indicated that chitosan-PAA microspheres had a higher affinity for mucin than those of chitosan alone. The swelling and dissolution of the chitosan-PAA microspheres were found to be dependent on the pH of the medium. The rate of enrofloxacin released from the chitosan-PAA microspheres was slower at higher pH; therefore, based on their mucoadhesive properties and morphology, the chitosan-PAA microspheres can be used as a mucoadhesive oral drug delivery system.

Keywords

References

  1. Ahn, J. S., Choi, H. K., and Cho, C. S., A novel mucoadhesive polymer prepared by template polymerization of a acrylic acid in the presence of chitosan. Biomaterials, 22, 923-928 (2001) https://doi.org/10.1016/S0142-9612(00)00256-8
  2. Ahn, J. S., Choi, H. K., Chun, M. K., Ryu, J, M., Jung, J. H., Kim Y. U., and Cho, C. S., Release of triamcinolone acetonide from mucoadhesive polymer composed of chitosan and poly(acrylic acid) in vitro. Biomaterials, 23, 1411-1416 (2002) https://doi.org/10.1016/S0142-9612(01)00261-7
  3. Chavasit, V. and Torres, J. A. Chitosan-Poly(acrylic acid): Mechanism of complex formation and potential industrial applications. Biotechnol. Prog., 6, 2-6 (1990) https://doi.org/10.1021/bp00001a001
  4. Cho, S.-M. and Choi, H.-K., Preparation of Mucoadhesive Chitosan-Poly (acrylic acid) Microsphere by Interpolymer Complexation and Solvent Evaporation Method I, submitted for publication in Kor. J. Pharm. Sci., (2005)
  5. Chun, M. K., Cho, C. S., and Choi, H. K., Mucoadhesive microspheres prepared by interpolymer complexation and solvent diffusion method. Int. J. Pharm., 288, 295-303 (2005) https://doi.org/10.1016/j.ijpharm.2004.10.016
  6. Fiebrig, I., Harding S. E., Rowe, A. J., Hyman, S. C., and Davis S. S., Transmission electron microscopy studies on pig gastric mucin and its interactions with chitosan. Carbohyd. Polym., 28, 239-244 (1995) https://doi.org/10.1016/0144-8617(95)00105-0
  7. Hu, Y., Jiang, X., Ding, Y., Ge, H., Yuan, Y., and Yang, C., Synthesis and characterization of chitosan-poly(acrylic acid) nanoparticles. Biomaterials, 23. 3193-3201 (2002) https://doi.org/10.1016/S0142-9612(02)00071-6
  8. Illum, L., Farraj, N. F., and Davis S. S., Chitosan as a novel nasal delivery system for peptide drugs. Pharm. Res., 11, 1186-1189 (1994) https://doi.org/10.1023/A:1018901302450
  9. Kockisch, S., Rees, G. D., Young, S. A., Tsibouklis, J., and Smart, J. D., Polymeric microspheres for drug delivery to the oral cavity: An in vitro evaluation of mucoadhesive potential. J. Pharm. Sci., 92, 1614-1623 (2003) https://doi.org/10.1002/jps.10423
  10. Lee, J. H., Park, T. G., and Choi, H. K., Development of oral drug delivery system using floating microspheres. J. Microencapsulation, 16, 715-729 (1999) https://doi.org/10.1080/026520499288663
  11. LueBen, H. L., Lehr, C. -M., Rentel, C. -O., Noach, A. B. J., DeBoer, A. G., Verhoef, J. C., and Junginger, H, E., Bioadhesive polymers for the peroral delivery of peptide drugs. J. Control. Rel., 29, 329-338 (1994) https://doi.org/10.1016/0168-3659(94)90078-7
  12. Miyazaki, S., Yamaguchi, H., Yokouchi, C., Takada, M., and Hou, W.-M., Sustained release and intragastric-floating granules of indomethacin using chitosan in rabbits. Chem. Pharm. Bull., 36, 4033-4038 (1988) https://doi.org/10.1248/cpb.36.4033
  13. Needleman, I. G. and Smales F. C., In vitro assessment of bioadhesion for periodontal and buccal drug delivery. Biomaterials, 16, 617-624 (1995) https://doi.org/10.1016/0142-9612(95)93859-C
  14. Park, H. and Robinson, J. R., Mechanism of mucoadhesion of poly(acrylic acid) hydrogels. Pharm. Res., 4, 457-464 (1987) https://doi.org/10.1023/A:1016467219657
  15. Polk, A., Amsden, B., De, Y. K., Peng, T., Doosen, M. F., Controlled release of albumin from chitosan-alginate microcapsules. J. Pharm. Sci., 83, 178-185 (1994) https://doi.org/10.1002/jps.2600830213
  16. Robinson, J. R., and Longer, M. A., and Veillard, M., Bioadhesive polymers for controlled delivery. New York Acad. Sci., 507, 307-314 (1987) https://doi.org/10.1111/j.1749-6632.1987.tb45810.x