Functionalized mesoporous silica nanoparticles for glucose- and pH-stimulated release of insulin

Rachit N. Jain, Xiaoxi Huang, Sayantani Das, Rafael Silva, Vera Ivanova, Tamara Minko, Teddy Asefa

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

Multi-stimuli responsive porous silica nanoparticles for controlled release of insulin were synthesized by tethering insulin molecules onto boronic acid-functionalized mesoporous silica nanoparticles (BA-MSNs) and then coating the BA-MSNs with the bioadhesive and pH-sensitive polymer polyacrylic acid (PAA). The insulin molecules were conjugated onto the exterior surfaces of BA-MSNs via gluconic acid linker groups [or by making first the gluconic acid-modified insulin (Gins)]. The surfaces of the resulting BA-MSNs containing Gins were coated with PAA, which was used to protect the entrapped insulin from undergoing possible enzymatic degradations in such locations as the gastrointestinal (GI) tract. The PAA, which has excellent dispersibility and adherence to the mucosa, might also allow the permeation of such nanoparticles through the colon, and thereby improve their potential application for insulin delivery. The drug release properties of the resulting nanoparticles, denoted PAA-Gins-BA-MSNs, as well as their control samples were studied in enzyme-free simulated gastric fluid (SGF) (pH = 2.0), simulated intestinal fluid (SIF) (pH = 6.8), and phosphate buffer saline (PBS) (pH = 7.4). Because of their shrinkage at low pH and swelling at high pH, the PAA-coated MSNs exhibited pH-dependent insulin release properties. Besides pH, glucose was shown to trigger the release of insulin from the nanoparticles, which demonstrates the nanoparticles' multi-stimuli-responsive properties for controlled release of insulin. Finally, we show that the PAA-coated MSNs were non-cytotoxic.

Original languageEnglish
Pages (from-to)616-623
Number of pages8
JournalZeitschrift fur Anorganische und Allgemeine Chemie
Volume640
Issue number3-4
DOIs
Publication statusPublished - 2014

Fingerprint

carbopol 940
Silicon Dioxide
Boronic Acids
Insulin
Nanoparticles
Glucose
Molecules
Fluids
Permeation
Swelling
Buffers
Polymers
Phosphates

Keywords

  • Insulin
  • Mesoporous silica nanoparticles
  • Nanomedicine
  • Nanoparticle drug delivery vehicle
  • Stimuli-responsive drug release

ASJC Scopus subject areas

  • Inorganic Chemistry

Cite this

Functionalized mesoporous silica nanoparticles for glucose- and pH-stimulated release of insulin. / Jain, Rachit N.; Huang, Xiaoxi; Das, Sayantani; Silva, Rafael; Ivanova, Vera; Minko, Tamara; Asefa, Teddy.

In: Zeitschrift fur Anorganische und Allgemeine Chemie, Vol. 640, No. 3-4, 2014, p. 616-623.

Research output: Contribution to journalArticle

Jain, Rachit N. ; Huang, Xiaoxi ; Das, Sayantani ; Silva, Rafael ; Ivanova, Vera ; Minko, Tamara ; Asefa, Teddy. / Functionalized mesoporous silica nanoparticles for glucose- and pH-stimulated release of insulin. In: Zeitschrift fur Anorganische und Allgemeine Chemie. 2014 ; Vol. 640, No. 3-4. pp. 616-623.
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