Abstract

Herein, poly[quaternized 2-(dimethylamino)ethyl methacrylate-b-lauryl methacrylate-b-(oligo ethylene glycol)methacrylate] (QPDMAEMA-b-PLMA-b-POEGMA) cationic amphiphilic triblock terpolymers were used as vehicles for the complexation/encapsulation of insulin (INS). The terpolymers self-assemble in spherical micelles with PLMA cores and mixed QPDMAEMA/POEGMA coronas in aqueous solutions. The cationic micelles were complexed via electrostatic interactions with INS, which contains anionic charges at pH 7. The solutions were colloidally stable in all INS ratios used. Light-scattering techniques were used for investigation of the complexation ability and the size and surface charge of the terpolymer/INS complexes. The results showed that the size of the complexes increases as INS ratio increases, while at the same time the surface charge remains positive, indicating the formation of clusters of micelles/INS complexes in the solution. Fluorescence spectroscopy measurements revealed that the conformation of the protein is not affected after the complexation with the terpolymer micellar aggregates. It was observed that as the solution ionic strength increases, the size of the QPDMAEMA-b-PLMA-b-POEGMA/INS complexes initially decreases and then remains practically constant at higher ionic strength, indicating further aggregation of the complexes. atomic force microscopy (AFM) measurements showed the existence of both clusters and isolated nanoparticulate terpolymer/protein complexes.

Highlights

  • Diabetes mellitus is one of the most common and serious chronic diseases, affecting millions of patients worldwide [1,2]

  • The ability of QPDMAEMA-b-PLMA-b-POEGMA cationic triblock terpolymer micelles to complex with insulin through electrostatic interactions is investigated

  • Mw /Mn a Determined by size exclusion chromatography (SEC), (1 H-NMR)

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Summary

Introduction

Diabetes mellitus is one of the most common and serious chronic diseases, affecting millions of patients worldwide [1,2]. The discovery of insulin was one of the most important scientific achievements of the last century [3]. Patients suffering from diabetes need to be administered with several doses of insulin daily, to maintain their blood glycose levels in the desirable rates. The main way for insulin administration is through subcutaneous injections [4]. The need exists for the development of novel, effective nanocarriers that will employ alternative routes, such as oral administration, for the delivery of insulin. The evolution of synthetic polymer chemistry gives scientists the ability to design and synthesize polymers with tailored properties, a very important feature when it comes to gene/protein delivery applications [5,6]

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