期刊
JOURNAL OF NANOBIOTECHNOLOGY
卷 20, 期 1, 页码 -出版社
BMC
DOI: 10.1186/s12951-022-01260-9
关键词
Oral insulin; Small molecule natural product; Multi-functional nanoparticles; pH-sensitive; Mucoadhesive; Tight junction
资金
- National Natural Science Foundation of China [82073974, 81603256]
- Beijing Municipal Natural Science Foundation [7202116]
- Beijing Nova program [Z201100006820026]
- project of China Association of Chinese Medicine [CACM-2018-QNRC2-B08]
- Fundamental Research Funds for the Central Universities [2020-JYB-ZDGG-044, BUCM-2019-JCRC002, 2019-JYB-TD005]
- Beijing Key Laboratory for Basic and Development Research on Chinese Medicine [100102]
This study developed multi-functional self-assembly nanoparticles as carriers for oral insulin delivery. These nanoparticles exhibited pH stimuli-responsive insulin release, intestinal mucoadhesion, and enhanced absorption. The carrier also improved the paracellular permeability for insulin absorption through downregulation of internal tight junction proteins.
Background: Oral administration of insulin (INS) could be absorbed into systemic circulation only if the carrier protected it from the hostile gastrointestinal conditions. However, traditional macromolecular carriers have not totally overcome challenges in addressing these biological barriers. Result: In this study, inspired by small molecule natural products (SMNPs), we demonstrate the multi-functional self-assembly nanoparticles (BA-Al NPs) originating from baicalin (BA) and AlCl3 through coordination bonds and hydrogen bonds. As a novel carrier for oral insulin delivery (INS@BA-Al NPs), it displayed effective capacity in pH stimuli-responsive insulin release, intestinal mucoadhesion and transepithelial absorption enhance. Meanwhile, BA improved the paracellular permeability for insulin absorption, because of its downregulation at both mRNA and protein level on internal tight junction proteins. In vivo experiments exhibited remarkable bioavailability of INS and an ideal glucose homeostasis in the type I diabetic rat model. Conclusion: This study offers a novel frontier of multi-functional carriers based on SMNPs with self-assembly character and bioactivity, which could be a promising strategy for diabetes therapy.
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