Starch film-coated microparticles for oral colon-specific drug delivery

Jin Chen; Xiaoxi Li; Ling Chen; Fengwei Xie

doi:10.1016/j.carbpol.2018.03.025

Starch film-coated microparticles for oral colon-specific drug delivery

Carbohydr Polym. 2018 Jul 1:191:242-254. doi: 10.1016/j.carbpol.2018.03.025. Epub 2018 Mar 14.

Authors

Jin Chen¹, Xiaoxi Li², Ling Chen³, Fengwei Xie⁴

Affiliations

¹ Ministry of Education Engineering Research Center of Starch & Protein Processing, Guangdong Province Key Laboratory for Green Processing of Natural Products and Product Safety, School of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China; School of Chemical Engineering, The University of Queensland, Brisbane, Qld 4072, Australia.
² Ministry of Education Engineering Research Center of Starch & Protein Processing, Guangdong Province Key Laboratory for Green Processing of Natural Products and Product Safety, School of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China.
³ Ministry of Education Engineering Research Center of Starch & Protein Processing, Guangdong Province Key Laboratory for Green Processing of Natural Products and Product Safety, School of Food Science and Engineering, South China University of Technology, Guangzhou 510640, China. Electronic address: felchen@scut.edu.cn.
⁴ School of Chemical Engineering, The University of Queensland, Brisbane, Qld 4072, Australia. Electronic address: f.xie@uq.edu.au.

PMID: 29661315
DOI: 10.1016/j.carbpol.2018.03.025

Abstract

The aim of this study was to prepare and characterize a novel type of starch-coated microparticles (MPs) allowing site-specific delivery of bioactives to the colon. An oral colon-specific controlled-release system was developed in the form of MPs coated with a resistant starch (RS2/RS3) film (RS@MPs) through an aqueous suspension coating process. The RS2 was chosen from a high-amylose cornstarch with 88.5% digestion resistibility. The RS3 was prepared by a high-temperature/pressure (HTP) treatment, with the following of enzymatic debranching, and retrogradation, resulting in a dramatic increase in enzymatic resistance (RS3 content: 76.6%). RS@MPs showed 40.7% of 5-aminosalicylic acid release within 8 h. The in vivo study of fluorescein-loaded RS@MPs indicated the high acidic and enzymatic resistibility of RS@MPs and a restrained release in the upper GIT. Therefore, RS@MPs has revealed to be a high potential system for accurately targeting bioactive compound delivery to the colon.

Keywords: 4′,6-diamidino-2-phenylindole (DAPI) (PubChem CID: 2954); 5-aminosalicylic acid (5-ASA) (PubChem CID: 4075); Acetic acid (PubChem CID: 176); Aqueous suspension film coating; Citric acid (PubChem CID: 311); Controlled release; D-Glucose (PubChem CID: 5793); Dimethyl sulfoxide (DMSO) (PubChem CID: 679); Dipotassium hydrogen phosphate (PubChem CID: 24450); Ethanol (PubChem CID: 702); Fluorescein isothiocyanate (FITC) (PubChem CID: 18730); Hydrochloric acid (PubChem CID: 313); Iodine (PubChem CID: 807); Isoflurane (PubChem CID: 3763); Lithium bromide (PubChem CID: 82050); Oral colon-specific delivery; Phenol (PubChem CID: 996); Potassium chloride (PubChem CID: 4873); Potassium dihydrogen phosphate (PubChem CID: 516951); Potassium iodine (PubChem CID: 4875); Resistant starch; Sodium chloride (PubChem CID: 5234); Sodium hydroxide (PubChem CID: 14798); Starch (PubChem CID: 24836924); Sulfuric acid (PubChem CID: 1118); Triethyl citrate (PubChem CID: 6506); Water (PubChem CID: 962).

MeSH terms

Administration, Oral
Animals
Colon / metabolism*
Drug Carriers / chemistry*
Drug Liberation
Male
Mesalamine / administration & dosage
Mesalamine / chemistry
Mesalamine / metabolism
Mice
Microspheres*
Organ Specificity
Starch / chemistry*
Water / chemistry

Substances

Drug Carriers
Water
Mesalamine
Starch