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Preparation and evaluation of insulin-loaded nanoparticles based on hydroxypropyl-β-cyclodextrin modified carboxymethyl chitosan for oral delivery

  • Biomaterials
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Abstract

Novel insulin-loaded nanoparticles based on hydroxypropyl-β-cyclodextrin modified carboxymethyl chitosan (CMC-HP-β-CD) were prepared to improve the oral bioavailability of insulin. The CMC-HP-β-CD was characterized by FT-IR spectroscopy and 1H-NMR spectra. The insulin-loaded nanoparticles were prepared through crosslinking with calcium ions, and the morphology and size of the prepared nanoparticles were characterized by transmission electron microscopy (TEM) and dynamic light scattering (DLS). Cumulative release in vitro study was performed respectively in simulated gastric medium fluid (SGF, pH=1.2), simulated intestinal fluid (SIF, pH=6.8) and simulated colonic fluid (SCF, pH=7.4). The encapsulation efficiency of insulin was up to 87.14 ± 4.32% through high-performance liquid chromatography (HPLC). Statistics indicated that only 15% of the encapsulated insulin was released from the CMC-HP-β-CD nanoparticles in 36 h in SGF, and about 50% of the insulin could be released from the nanoparticles in SIF, whereas more than 80% was released in SCF. In addition, the solution containing insulin nanoparticles could effectively reduce the blood glucose level of diabetic mice. The cytotoxicity test showed that the samples had no cytotoxicity. CMC-HP-β-CD nanoparticles are promising candidates as potential carriers in oral insulin delivery systems.

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Authors and Affiliations

  1. Department of Pharmaceutical Engineering, School of Chemistry, Chemical Engineering and Life Sciences, Wuhan University of Technology, Wuhan, 430070, China

    Haoyuan Song  (宋豪源), Fuliang Xiong, Hui Hong, Chunfu Li, Lianghong Li, Shanshan Wu & Xueqiong Zhang

  2. Hubei Key Laboratory of Purification and Application of Plant Anti-cancer Active Ingredients, Hubei University of Education, Wuhan, 430000, China

    Xiaoling Ma  (马晓玲)

  3. Maternal and Child Health Hospital of Hubei, Wuhan, 430070, China

    Juan Zhang  (张娟)

  4. Beijing You’an Hospital attached to the Capital University of Medical Science, Beijin, 100069, China

    Jianhua Hu  (胡建华)

Authors
  1. Haoyuan Song  (宋豪源)
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  2. Xiaoling Ma  (马晓玲)
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  3. Fuliang Xiong
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  4. Hui Hong
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  5. Chunfu Li
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  6. Lianghong Li
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  7. Shanshan Wu
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  8. Xueqiong Zhang
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  9. Juan Zhang  (张娟)
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  10. Jianhua Hu  (胡建华)
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Corresponding authors

Correspondence to Juan Zhang  (张娟) or Jianhua Hu  (胡建华).

Additional information

SONG Haoyuan and MA Xiaoling contributed equally to this study

Funded by the National Nature Science Foundation of China (No. 51273156) and the Open Foundation of Hubei key laboratory of Purification and Application of Plant Anti-cancer Active Ingredients (No. HLPAI2014005)

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Song, H., Ma, X., Xiong, F. et al. Preparation and evaluation of insulin-loaded nanoparticles based on hydroxypropyl-β-cyclodextrin modified carboxymethyl chitosan for oral delivery. J. Wuhan Univ. Technol.-Mat. Sci. Edit. 31, 1394–1400 (2016). https://doi.org/10.1007/s11595-016-1544-z

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  • DOI: https://doi.org/10.1007/s11595-016-1544-z

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