4.7 Article

Glucose sensitive konjac glucomannan/concanavalin A nanoparticles as oral insulin delivery system

Journal

INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Volume 202, Issue -, Pages 296-308

Publisher

ELSEVIER
DOI: 10.1016/j.ijbiomac.2022.01.048

Keywords

Insulin oral delivery; Nanoparticle; Glucose response

Funding

  1. National Natural Science Foundation of China [31370967]
  2. Guangdong Province Universities and Colleges Pearl River Scholar Funded Scheme (2014), China
  3. Science and Technology Planning Project of Guangdong Province [2015A020212033]
  4. Science and Technology Project of Guangzhou [201805010002]
  5. Open Research Funds of the State Key Laboratory of Ophthalmology, China

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Compared with injection, oral drug delivery is a preferred mode of administration due to its security, low pain, and simplicity. In this study, a targeted oral delivery system was developed using ConA-INS-KGM nanoparticles loaded with insulin, which demonstrated reversible glucose-responsive insulin release and high biocompatibility. These nanoparticles show significant potential for diabetes treatment and have various applications in biomedical fields.
Compared with injection, oral drug delivery is a better mode of administration because of its security, low pain and simplicity. Insulin is the first choice for clinical treatment of type 1 diabetes, but, because insulin inability to resist gastrointestinal (GI) digestion results in poor oral bioavailability of insulin. Herein, we developed a targeted oral delivery system for diabetes. ConA-INS-KGM nanoparticles were prepared, loaded with insulin, fabricated from konjac glucomannan (KGM) and concanavalin A (ConA) through a crosslinking method, as an insulin oral delivery system in response to different blood glucose levels. The size of nanoparticles was characterized by TEM, which showed that these nanoparticles were formed spherical particles with a diameter of about 500 nm. In vitro release of insulin from these nanoparticles was studied, which indicated that insulin release is reversible at different glucose concentrations. In vivo tests demonstrated that they are safe and have high biocompatibility. Using the nanoparticles to treat diabetic mice, we found that they can control blood sugar levels for 6 h, retaining their glucose-sensitive properties during this time. Therefore, these nanoparticles have significant potential as glucose-responsive systems for diabetes and show great applications in biomedical fields.

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