2. Academic Validation
  3. Inclusion complex based on N-acetyl-L-cysteine and arginine modified hydroxypropyl-β-cyclodextrin for oral insulin delivery

Inclusion complex based on N-acetyl-L-cysteine and arginine modified hydroxypropyl-β-cyclodextrin for oral insulin delivery

  • Carbohydr Polym. 2021 Jan 15:252:117202. doi: 10.1016/j.carbpol.2020.117202.
Siyi Li 1,  Na Liang 2,  Pengfei Yan 3,  Yoshiaki Kawashima 4,  Shaoping Sun 5
Affiliations

Affiliations

  • 1 Key Laboratory of Functional Inorganic Materials Chemistry (Ministry of Education), School of Chemistry and Material Science, Heilongjiang University, Harbin 150080, China. Electronic address: lisiyi626@163.com.
  • 2 College of Chemistry & Chemical Engineering, Harbin Normal University, Harbin 150025, China. Electronic address: liangna528@163.com.
  • 3 Key Laboratory of Functional Inorganic Materials Chemistry (Ministry of Education), School of Chemistry and Material Science, Heilongjiang University, Harbin 150080, China. Electronic address: yanpf@vip.sina.com.
  • 4 Department of Pharmaceutical Engineering, School of Pharmacy, Aichi Gakuin University, Nagoya 464-8650, Japan. Electronic address: sykawa123@163.com.
  • 5 Key Laboratory of Functional Inorganic Materials Chemistry (Ministry of Education), School of Chemistry and Material Science, Heilongjiang University, Harbin 150080, China. Electronic address: sunshaoping111@163.com.
PMID: 33183638 DOI: 10.1016/j.carbpol.2020.117202
Abstract

Insulin is the most effective drug in the treatment of diabetes mellitus. At present, subcutaneous injection is still the common way for Insulin delivery. However, oral delivery is considered as the most preferred way for its high patient compliance and the minimal invasiveness. In this study, a novel N-acetyl-L-cysteine and arginine modified hydroxypropyl-β-cyclodextrin (NAC-HP-β-CD-Arg) was successfully synthesized and characterized. The polymer was used as a carrier for oral delivery of Insulin by forming NAC-HP-β-CD-Arg@insulin complex. Enzymatic degradation study indicated that the NAC-HP-β-CD-Arg could protect Insulin from enzymolysis. Moreover, the polymer exhibited strong binding ability with Mucin. The transportation efficiency of NAC-HP-β-CD-Arg@insulin across the Caco-2 cell monolayer was much greater than free Insulin. The in vivo study demonstrated that the orally administered NAC-HP-β-CD-Arg@insulin exhibited an excellent and sustained hypoglycemic effect in diabetic rats. It can be concluded that the NAC-HP-β-CD-Arg is a potential carrier for oral delivery of Insulin.

Keywords

Arginine; Hydroxypropyl-β-cyclodextrin; Insulin; N-acetyl-L-cysteine; Oral delivery.

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