Abstract

Poor solubility, erratic bioavailability and delivery challenges associated with gliclazide, which is commonly used in type 2 diabetes mellitus (T2DM) treatment, are overcome by exploring electrospun nanofibers technology. Employing emulsion electrospinning method with polyvinyl alcohol (PVA) alone and in combination with poly(d/l-lactide-co-glycolide) (PLGA), nanofibers were fabricated. Different concentrations of PLGA at 0.05%, 0.10% and 0.15% w/v were added to PVA to achieve a modified drug release profile to meet the typical physiological needs of T2DM, such as a faster drug release at meals followed by prolonged release to maintain constant plasma glucose level, which is highly desirable in T2DM management. Fabricated gliclazide-nanofibers were characterized by various studies, such as solubility, in-vitro drug release, drug release kinetic, scanning electron microscopy (SEM), differential scanning calorimetric (DSC), and Fourier transform infrared (FTIR) spectroscopy. GLZNF2, formulation of Drug:PVA:PLGA 0.1:10:0.05% w/v produced optimized gliclazide nanofibers. The optimized GLZNF2 nanofibers were incorporated into gelatin capsule for oral administration. SEM image of optimized formulation (GLZNF2) shows cylindrical shaped fiber, indicating gliclazide incorporated homogeneously in polymers with average fiber diameter 4.357 ± 0.83 µm. The solubility and dissolution rate of gliclazide nanofibers significantly improved compared to pure gliclazide. The gliclazide nanofibers produce a biphasic drug release profile, initial fast release, followed by prolonged release. Oral fabricated gliclazide fibers have tremendous potential as a drug carrier, and alternative technology for the improvement of solubility, dissolution rate, reduction in the dosing frequency and better blood glucose control could be explored in T2DM management.

Highlights

  • The electrospun method of making electrostatic fiber is one of the advanced and straightforward techniques of nanotechnology, and has tremendous potential as a drug carrier for the delivery of therapeutics

  • Different concentrations of PLGA at 0.05%, 0.10% and 0.15% w/v were added to polyvinyl alcohol (PVA) to achieve a modified drug release profile to meet the typical physiological needs of type 2 diabetes mellitus (T2DM), such as a faster drug release at the time of meals followed by prolonged drug release profile over an extended period to maintain constant plasma glucose level, highly desirable for better

  • A conventional gliclazide oral treatment failed to meet the typical physiological goal of T2DM, such as basic needs between meals and during the night, which demands a faster drug release followed by prolonged drug release profile to maintain a constant plasma glucose level over an extended period of time

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Summary

Introduction

The electrospun method of making electrostatic fiber is one of the advanced and straightforward techniques of nanotechnology, and has tremendous potential as a drug carrier for the delivery of therapeutics. Polymeric electrospun fibers of diameters ranging from several nanometers to several micrometres are developed as drug carriers employing polymer solutions under the influence of an electrostatic field [1]. Gliclazide is a second generation of sulphonylurea commonly used in the treatment of Type 2 Diabetes Mellitus. It promotes the production of insulin from the beta cells in the pancreas and stimulates insulin sensitivity.

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