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Examining Insulin Adsorption onto Mesoporous Silica Microparticles for Oral Delivery

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Background: Microencapsulation is one of the most common techniques for the delivery of macromolecules; however, it can cause various stability problems, such as degradation or loss of bioactivity of the loaded molecules. For this reason, several techniques were investigated to load insulin into pre-formed porous microparticles (MPs).

Objective: The high loading of insulin is a prerequisite of its delivery in sufficient concentration; hence we examined insulin loading in mesoporous silica (SBA15-NH2) as a model for uniformly porous microparticles using different loading methods and factors.

Method: The MPs were characterized with respect to their morphology, porosity and pore diameter while insulin adsorption into the porous substrates was investigated using immersion and freeze-drying at different pH and initial peptide concentrations. MPs were further coated with Chitosan as a technique for pore blocking.

Results: The results showed that the extent of insulin adsorption by freeze-drying varied depending on substrate affinity to insulin and pH where it could achieve the highest loading capacity at a pH near its isoelectric point. A significant increase in drug loading along with slower drug release was observed with Chitosan coated SBA15-NH2 MPs. In addition, the structural integrity of insulin was maintained after loading into the MPs, as confirmed by gel electrophoresis and fluorescent spectroscopy together with the in vivo study which in turn confirmed the preservation of insulin bioactivity in lowering blood glucose after oral administration.

Conclusion: The present work displays the various factors that can control insulin loading in mesoporous silica MPs and their effects in enhancing the efficiency of insulin oral delivery using such substrates.
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Keywords: Chitosan coating; freeze-drying; insulin; mesoporous silica; microparticles; post-synthetic loading

Document Type: Research Article

Publication date: May 1, 2018

This article was made available online on October 18, 2017 as a Fast Track article with title: "Examining Insulin Adsorption onto Mesoporous Silica Microparticles for Oral Delivery".

More about this publication?
  • The aim of Current Drug Delivery is to publish peer-reviewed articles, short communications, short and in-depth reviews in the rapidly developing field of drug delivery. Modern drug research aims to build in delivery properties of a drug at the design phase, however in many cases this ideal cannot be met and the development of delivery systems becomes as important as the development as the drugs themselves.

    The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance.

    The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.
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