Pectin Microspheres for Oral Colon Delivery: Preparation Using Spray Drying Method and In Vitro Release of Release of Indomethacin

  • Lee, Chang-Moon (Interdisciplinary Program of Biomedical Engineering, Chonnam National University) ;
  • Kim, Dong-Woon (Department of Health and Hygiene, Gwang-Yang Health College) ;
  • Lee, Hyun-Chul (Department of Microbiology, Chonnam National University Medical School) ;
  • Lee, Ki-Young (Faculty of Applied Chemical Engineering and The Research Institute for Catalysis, Chonnam National University)
  • 발행 : 2004.06.01

초록

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 microspheres 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, indomethacin (IND) release was more suppressed 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${\pm}$2% of the total loaded weight for 24 h 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.

키워드

참고문헌

  1. Biomaterials v.24 Pectin-based systems for colon-specific drug delivery via oral route LinShu,L.;L.F.Marshall;K.Joseph;B.H.Kevin https://doi.org/10.1016/S0142-9612(03)00213-8
  2. Adv. Drug Deliv. Rev. v.34 Oral particulate delivery: Status and future trends Chen,H.;R.Langer https://doi.org/10.1016/S0169-409X(98)00047-7
  3. Int. J. Pharm. v.169 Investigation of pectin as a carrier for ora delivery of proteins using calcium pectinate gel beads Sriamornsak,P. https://doi.org/10.1016/S0378-5173(98)00129-X
  4. J. Control. Release v.93 Oral colon-specific drug delivery for bee venom peptide: development of a coated calcium alginate gel beads-entrapped liposome Xing,L.;C.Dawei;X.Liping;R.Zhang https://doi.org/10.1016/j.jconrel.2003.08.019
  5. Int. J. Pham. v.129 In vitro evaluation of pectin-based colonic drug delivery systems Wakerly,Z.;J.T.Fell;D.Attwood;D.A.Parkins https://doi.org/10.1016/0378-5173(95)04251-2
  6. Int. J. Pharm. v.232 Oral delayed-release system based on Zn-pectinate gel (ZPG) microparticles as an alternative carrier to calcium pectinate beads for colonic drug delivery El-Gibaly,I. https://doi.org/10.1016/S0378-5173(01)00903-6
  7. Carbohydr. Polym. v.48 The use of polysaccharides to target drugs to the colon Vandamme,T.F.;A.Lenourry;C.Charrueau;J.C.Chaumeil https://doi.org/10.1016/S0144-8617(01)00263-6
  8. J. Control. Release v.46 Hydrogel bead on amidated pectins for colon-specific drug delivery: the role of chitosan in modifying drug release Munjeri,O.;J.H.Collett;J.T.Fell https://doi.org/10.1016/S0168-3659(96)01607-0
  9. Int. J. Pharm. v.235 Colon-specific drug delivery: new approaches and in vitro/in vivo evaluation Yang,L.;J.S.Chu;J.A.Fix https://doi.org/10.1016/S0378-5173(02)00004-2
  10. Int. J. Pharm. v.156 Calcium pectinate gel beads for controlled release drug delivery: I. Preparation and in vitro release studies Sriamornsak,P.;J.Nunthanid https://doi.org/10.1016/S0378-5173(97)00192-0
  11. Int. J. Pharm. v.242 Drug release properties of pectinate microspheres prepared by emulsification method Wong,T.W.;H.Y.Lee;L.W.Chan;P.W.S.Heng https://doi.org/10.1016/S0378-5173(02)00163-1
  12. Drug Dev. Ind. Pharm. v.24 Influence of formulation variables on the morphology of biodegradable microspheres prepared by spray drying Clarke,N.;K.O'Connor;Z.Ramtoola https://doi.org/10.3109/03639049809085602
  13. Eur. J. Pharm. Biopharm. v.55 Preparation of bupiva-caine-loaded poly(ε-caprolactone) microspheres by spray drying: drug release studies and biocompatibility Blanco,M.D.;M.V.Bernardo;R.L.Sastre;R.Olmo;E.Muniz;J.M.Teijon https://doi.org/10.1016/S0939-6411(02)00169-8
  14. Biopolymers v.28 Properties of amidated pectins. II. Polyelectrolyte behaviour and calcium binding of amidated pectins and amidated pectin acids Racope,E.;J.F.Thibault;J.C.E.Rietsma;W.Pilnik https://doi.org/10.1002/bip.360280809
  15. Pharm. Res. v.10 In vitro evaluation of calcium pectinate: A potential colon-specific drug delivery carrier Rubinstein,A.;R.Radai;M.Ezra;S.Pathak;S.Rokem https://doi.org/10.1023/A:1018995029167
  16. Pharm. Res. v.9 Hydrogels for site-specific drug delivery to the colon: in vitro and in vivo degradation Brondsted,H.;J.Kopecek https://doi.org/10.1023/A:1015847921435
  17. Eur. J. Pharm. Biopharm. v.53 In vitro evaluation of pectin-HPMC compression coated 5-aminosalicylic acid tablets for colonic delivery Mural,T.;T.Timucin https://doi.org/10.1016/S0939-6411(01)00225-9