Abstract

The objective of this study is to utilize the pH sensitivity of modified silica nanoparticles (SNIL) by imidazole-based ionic liquid for oral delivery of insulin. In the first time, the imidazole was covalently attached to the 3-trimethoxysily-lpropyl chloride with replacement of all the chlorine atoms. Then, a silica nanoparticle was modified by N-(3-trimeth-oxysilylpropyl) imidazole. The nanocapsule (NCIL) was achieved after the etching of the modified silica nanoparticle template with hydrofluoric acid. The nanoparticles connected through an ionic liquid-like network were characterized by FTIR and SEM. Insulin was entrapped in these carriers and the in vitro release profiles were established separately in both enzyme-free simulated gastric and intestinal fluids (SGF, pH 1) and (SIF, pH 7.4), respectively. When these drug-loaded nanoparticles was placed in physiological buffer solution (pH 7.4), a partial negative surface charge on the modified silica nanoparticle was generated due to the deprotonation of silanol groups, and the strong electrostatic repulsion triggered a sustained release of the loaded molecules.

Highlights

  • Oral delivery of drugs, especially therapeutic proteins, is the preferred route of administration because it offers advantages over injection, which is the presently accepted route of therapeutic protein administration

  • When these drugloaded nanoparticles was placed in physiological buffer solution, a partial negative surface charge on the modified silica nanoparticle was generated due to the deprotonation of silanol groups, and the strong electrostatic repulsion triggered a sustained release of the loaded molecules

  • We report a synthesis of positively charged SN by attaching imidazole ionic liquid to silica nanoparticles

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Summary

Introduction

Especially therapeutic proteins, is the preferred route of administration because it offers advantages over injection, which is the presently accepted route of therapeutic protein administration. Several approaches have been studied to deliver drugs to colon tissue, their efficiency in the delivery still encounters a lot of challenges. Our response to this challenge was to design a porous nano carrier with a controlled-release function that decreased the degradation and the non-specific release of drug molecules in the GI tract. Due to its nano size, MSN has much higher cellular uptake efficiency than the micron-sized mesoporous silica particle [7], therapeutic drugs or tracing molecules that are not membrane-transportable could be incorporated into the nano channels of SN to be delivered into cells

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