Abstract
Nanoparticles or microparticles created by physical complexation between two polyelectrolytes may have a prospective use as an excipient for oral insulin administration. Natural polymers such as tragacanth, alginate, dextran, pullulan, hyaluronic acid, gelatin and chitosan can be potential candidates for this purpose. In this research, insulin particles were prepared by the inclusion of insulin into a tragacanth hydrogel. The effect of the pH and concentration relationship involving polyelectrolytes offering individual particle size and zeta potential was assessed by zetasizer and scanning electron microscopy (SEM). Insulin–tragacanth interactions at varying pH (3.7, 4.3, 4.6, or 6), and concentration (0.1%, 0.5%, or 1% w/w) were evaluated by differential scanning calorimetry (DSC) and ATR Fourier transform infrared (ATR-FTIR) analysis. Individual and smaller particles, approximately 800 nm, were acquired at pH 4.6 with 0.5% of tragacanth. The acid gelation test indicated that insulin could be entrapped in the physical hydrogel of tragacanth. DSC thermograms of insulin–tragacanth showed shifts on the same unloaded tragacanth peaks and suggested polyelectrolyte–protein interactions at a pH close to 4.3–4.6. FTIR spectra of tragacanth–insulin complexes exhibited amide absorption bands featuring in the protein spectra and revealed the creation of a new chemical substance.
Highlights
Development of an appropriate carrier system for the oral delivery of insulin is still the main related problem due to compromised bioavailability hindered by the epithelial barriers of the stomach and gastrointestinal destruction by proteolytic enzymes [1,2,3]
Insulin was entrapped in physical hydrogel and polyelectrolyte complexes (PECs) created using
Insulin was entrapped in physical hydrogel and polyelectrolyte complexes (PECs) created using biodegradable biopolymer—tragacanth
Summary
Development of an appropriate carrier system for the oral delivery of insulin is still the main related problem due to compromised bioavailability hindered by the epithelial barriers of the stomach and gastrointestinal destruction by proteolytic enzymes [1,2,3]. A suitable insulin carrier really should provide biocompatibility as well as stabilisation under conditions in the gut in order to assure that the primary fraction of the insulin would be biologically active when delivered on site [1,2,3]. Biopolymers, for example, chitosan, dextran sulphate, and alginates, have been extensively studied due to their suitability for encapsulating proteins/peptides [4,5]. After encapsulation with these biopolymers, the bioavailability of insulin after oral administration remained low. These biopolymers can be complexed with insulin using various strategies, which include polyelectrolyte complexation (PEC), emulsification, ionotropic pregelation, and spray drying. Particles formed through polyelectrolyte complexation have demonstrated potential for use as an oral insulin carrier
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