Skip to main content
Log in

Pectin microspheres for oral colon delivery: Preparation using spray drying method andin vitro release of indomethacin

  • Published:
Biotechnology and Bioprocess Engineering Aims and scope Submit manuscript

Abstract

Drug delivery systems that are based on pectin have been studied for colon specific delivery using the specific activity of colon microflora. The aim of this study was to design a novel method of manufacturing pectin microspheres without oils and surfactants and to investigate the potential use of the pectin microsphere as an oral colon-specific drug carrier. The pectin microspheres were successfully formed using the spray drying method and crosslinking with calcium chloride. From the crosslinked pectin microspheres, indomethancin (IND) release was more supressed than its release from non-crosslinked microspheres. In a low pH (pH 1.4) environment, the pectin microspheres released IND at an amount of about 18±2% of the total loaded weight for 24h while the release rate of IND was stimulated at neutral pH (pH 7.4). IND release from the pectin microspheres was increased by the addition of pectinase. The results clearly demonstrate that the pectin microspheres that were prepared by the spray drying and crosslinking methods are potential carriers for colon-specific drug deliveries.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  1. LinShu, L., L. F. Marshall, K. Joseph, and B. H. Kevin (2003) Pectin-based systems for colon-specific drug delivery via oral route.Biomaterials 24: 3333–3343.

    Article  Google Scholar 

  2. Chen, H. and R. Langer (1998) Oral particulate delivery: Status and future trends.Adv. Drug Deliv. Rev. 34: 339–350.

    Article  CAS  Google Scholar 

  3. Sriamornsak, P. (1998) Investigation of pectin as a carrier for oral delivery of proteins using calcium pectinate gel beads.Int. J. Pharm. 169: 213–220.

    Article  CAS  Google Scholar 

  4. Xing, L., C. Dawei, X. Liping, and R. Zhang (2003) Oral colon-specific drug delivery for bee venom peptide: development of a coated calcium alginate gel beads-entrapped liposome.J. Control. Release 93: 293–300.

    Article  Google Scholar 

  5. Wakerly, Z., J. T. Fell, D. Attwood, and D. A. Parkins (1996)In vitro evaluation of pectin-based colonic drug delivery systems.Int. J. Pharm. 129: 73–77.

    Article  CAS  Google Scholar 

  6. El-Gibaly, I. (2002) Oral delayed-release system based on Zn-pectinate gel (ZPG) microparticles as an alternative carrier to calcium pectinate beads for colonic drug delivery.Int. J. Pharm. 232: 199–211.

    Article  CAS  Google Scholar 

  7. Vandamme, T. F., A. Lenourry, C. Charrueau, and J. C. Chaumeil (2002) The use of polysaccharides to target drugs to the colon.Carbohydr. Polym. 48: 219–231.

    Article  CAS  Google Scholar 

  8. Munjeri, O., J. H. Collett, and J. T. Fell (1997) Hydrogel bead on amidated pectins for colon-specific drug delivery: the role of chitosan in modifying drug release.J. Control. Release 46: 273–278.

    Article  CAS  Google Scholar 

  9. Yang, L., J. S. Chu, and J. A. Fix (2002) Colon-specific drug delivery: new approaches andin vitro/in vivo evaluation.Int. J. Pharm. 235: 1–15.

    Article  CAS  Google Scholar 

  10. Sriamornsak, P. and J. Nunthanid (1998) Calcium pectinate gel beads for controlled release drug delivery: I. Preparation andin vitro release studies.Int. J. Pharm. 156: 189–194.

    Article  Google Scholar 

  11. Wong T. W., H. Y. Lee, L. W. Chan, and P. W. S. Heng (2002) Drug release properties of pectinate microspheres prepared by emulsification method.Int. J. Pharm. 242: 233–237.

    Article  CAS  Google Scholar 

  12. Clarke, N., K. O’Connor, and Z. Ramtoola (1998) Influence of formulation variables on the morphology of biodegradable microspheres prepared by spray drying.Drug Dev. Ind. Pharm. 24: 169–174.

    Article  CAS  Google Scholar 

  13. Blanco, M. D., M. V. Bernardo, R. L. Sastre, R. Olmo, E. Muniz, and J. M. Teijon (2003) Preparation of bupivacaine-loaded poly(ε-caprolactone) microspheres by spray drying: drug release studies and biocompatibility.Eur. J. Pharm. Biopharm. 55: 229–236.

    Article  CAS  Google Scholar 

  14. Racope, E., J.-F. Thibault, J. C. E. Rietsma, and W. Pilnik (1989) Properties of amidated pectins. II. Polyelectrolyte behaviour and calcium binding of amidated pectins and amidated pectin acids.Biopolymers 28: 1433–1448.

    Google Scholar 

  15. Rubinstein, A., R. Radai, M. Ezra, S. Pathak, and S. Rokem (1993)In vitro evaluation of calcium pectinate: A potential colon-specific drug delivery carrier.Pharm. Res. 10: 258–263.

    Article  CAS  Google Scholar 

  16. Brondsted, H. and J. Kopecek (1992) hydrogels for sitespecific drug delivery to the colon:in vitro andin vivo degradation.Pharm. Res. 9: 1540–1545.

    Article  CAS  Google Scholar 

  17. Murat, T. and U. Timucin (2002)In vitro evaluation of pectin-HPMC compression coated 5-aminosalicylic acid tablets for colonic delivery.Eur. J. Pharm. Biopharm. 53: 65–73.

    Article  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Ki-Young Lee.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Lee, CM., Kim, DW., Lee, HC. et al. Pectin microspheres for oral colon delivery: Preparation using spray drying method andin vitro release of indomethacin. Biotechnol. Bioprocess Eng. 9, 191–195 (2004). https://doi.org/10.1007/BF02942291

Download citation

  • Received:

  • Accepted:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF02942291

Keywords

Navigation