An oral colon-targeting controlled release system based on resistant starch acetate: Synthetization, characterization, and preparation of film-coating pellets

Huayin Pu, Ling Chen, Xiaoxi Li, Fengwei Xie, Long Yu, Lin Li

Research output: Contribution to journalArticlepeer-review

102 Citations (SciVal)

Abstract

An oral colon-targeting controlled release system based on resistant starch acetate (RSA) as a film-coating material was developed. The RSA was successfully synthesized, and its digestion resistibility could be improved by increasing the degree of substitution (DS), which was favorable for the colon-targeting purpose. As a delivery carrier material, the characteristics of RSA were investigated by polarized light microscopy, FTIR spectroscopy, and X-ray diffraction. The results revealed a decrease of the crystallinity of RSA and a change of its crystalline structure from B + V hydrid type to V type. To evaluate the colon-targeting release performance, the RSA film-coated pellets loaded with different bioactive components were prepared by extrusion- spheronization and then by fluid bed coating. The effects of the DS, plasticizer content, and coating thickness of the RSA film and those of the content and molecular weight of the loaded bioactive component on the colon-targeting release performance of the resulting delivery system were investigated. By adjusting the DS, the coating thickness, and the plasticizer content of the RSA film, either the pellets loaded with a small molecular bioactive component such as 5-aminosalicylic acid or those with a macromolecular bioactive peptide or protein such as bovine serum albumin, hepatocyte growth-promoting factor, or insulin showed a desirable colon-targeting release performance. The release percentage was less than 12% in simulated upper gastrointestinal tract and went up to 70% over a period of 40 h in simulated colonic fluid. This suggests that the delivery system based on RSA film has an excellent colon-targeting release performance and the universality for a wide range of bioactive components.

Original languageEnglish
Pages (from-to)5738-5745
Number of pages8
JournalJournal of Agricultural and Food Chemistry
Volume59
Issue number10
Early online date3 May 2011
DOIs
Publication statusPublished - 25 May 2011

Bibliographical note

Funding information:
The authors from SCUT, China, acknowledge the NationalNatural Science Foundation of China (Nos. 31071503 and20606014), the Fundamental Research Funds for the CentralUniversities, SCUT (2009ZZ0021), and the Agricultural Scienceand Technology Achievements Transformation Fund Programs(2009GB23600523).

Keywords

  • Bioactive component
  • Colon-targeting
  • Film-coated pellets
  • In vitro release
  • Resistant starch acetate

ASJC Scopus subject areas

  • General Chemistry
  • General Agricultural and Biological Sciences

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