Abstract
The principal challenge for the use of boronic acids (BA) as glucose sensors is their lack of specificity for glucose. We examined the selectivity of and insulin release from two boronic acids- (2-formyl-3-thienylboronic acid (FTBA) and 4-formylphenylboronic acid (FPBA)) conjugated chitosan scaffolds to glucose and fructose. Adsorption of glucose to BA: chitosan conjugates was dose-dependent up to 1:1 at 35 and 42% for FPBA and FTBA respectively but the FTBA conjugates adsorbed more glucose and fructose at respective FPBA ratios. The affinity of both BA conjugates to glucose decreased with increase in BA ratio. On the other hand, the affinity of both BA conjugates for fructose decreased from ratio 1:1 to 2:1 then rose again at 3:1. Insulin release from FPBA nanoparticles (FPBAINP) and FTBA nanoparticles (FTBAINP) were both concentration-dependent within glyceamically relevant values (1–3 mg/ml glucose and 0.002 mg/ml fructose). Furthermore, the total amounts of insulin released from FPBAINP in both the media were higher than from FTBAINP. Both FPBAINP and FTBAINP have the potential for development as a glucose-selective insulin delivery system in physiological settings.
Highlights
As one of the most common chronic diseases in almost every country, the incidence of diabetes is on the rise
Both FPBAINP and FTBAINP have the potential for development as a glucose-selective insulin delivery system in physiological settings
In an attempt to address the lack of specificity to glucose sensing by boronic acids, we report for the first time, the use of 2-formyl-3thienylboronic acid (FTBA) as the boronic acid conjugated to chitosan in the development of a glucose chemosensor
Summary
As one of the most common chronic diseases in almost every country, the incidence of diabetes is on the rise. The current treatment option for type 1 and end-stage type 2 diabetes is insulin replacement therapy in the form of multiple daily subcutaneous injections of insulin, which is discomforting and lead to poor patient compliance [2]. This has necessitated research interest amongst scientists working toward developing glucoseregulated insulin replacement therapies that are painless, relatively inexpensive to manufacture compared to the current mode and readily available [3]. The three most extensively studied glucose sensors are glucose oxidase, glucose-binding proteins (GBPs) and glucose-binding small molecules Using these glucose responsive molecules, insulin loaded nanoparticles can be formulated which will release the drug via degradation, disassembly or swelling in response to changes in glucose concentrations [4,6]. Small molecule glucose binders such as boronic acids (BAs) offer a chemical approach to glucose-mediated insulin release via reversible interactions with cis-1,2- or 1,3-diols
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