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• W3010129440 abstract "Diabetes mellitus is one of the most grave and lethal non-communicable diseases. Insulin isnormally used to medicate diabetes. Due to bioavailability issues, the most regular route ofadministration is through injection, which may pose compliance problems to treatment. The oraladministration thus appears as a suitable alternative, but with several important problems. Lowstability of insulin in the gastrointestinal tract and low intestinal permeation are some of theissues. Encapsulation of insulin into polymer-based particles emerges as a plausible strategy.Different encapsulation approaches and polymers have been used in this regard. Polymers withdifferent characteristics from natural or synthetic origin have been assessed to attain this goal,with natural polymers being preferable. Natural polymer such as tragacanth, an anionicpolysaccharide gum, can be alternative polymeric carrier for physiologically important peptidesand proteins like insulin.Characterisation of tragacanth was explored in the first stage of the study, for providing afoundation for possible applications. Rheological studies colloidal solution of tragacanth at pH 3,5 or 7 were carried out by means of steady shear and small amplitude oscillatory measurements.From preliminary study, 0.5% tragacanth was selected as optimum colloidal solution and 0.2mg/ml insulin was chosen as concentration for a model protein. Tragacanth mucoadhesivity wasalso analysed using an applicable rheological method and compared to chitosan, alginate andPVP. The particle size and zeta potential were measured by a zetasizer. Thermal properties ofsolutions were obtained using a differential scanning calorimetry. The solution exhibited shearthinningcharacteristics. The value of the storage modulus (G′) and the loss modulus (G″)increased with an increase in angular frequency (Ω). In all cases, loss modulus values were higherthan storage values (G″ > G′) and viscous character was, therefore, dominant. Tragacanth and alginate showed a good mucoadhesion. Tragacanth upon dispersion created particles of asubmicron size with z-average diameters (mean) ranging between roughly 431 and 581 nm, witha negative zeta potential (-7.98 to -11.92 mV). These properties were pH dependant resulting inacid gel formation at pH 3.5. Tragacanth has thus a potential to be used as an excipient forpeptide/protein delivery.Since tragacanth has a promising result to be used as a carrier in protein/peptide delivery andneeds a further application, in the second study, insulin microparticles were prepared by theinclusion of insulin into a tragacanth hydrogel followed by freeze drying. The effect of the pHand concentration relationship involving polyelectrolytes offering individual particle size andzeta potential was assessed by zetasizer and scanning electron microscopy (SEM). Insulin–tragacanth interactions were prepared at varying pH (3.7, 4.3, 4.6, or 6), and concentration (0.1,0.5, or 1% w/w) to optimize the conditions for optimal delivery of insulin. The pI of insulin canvary from 5.5 to 6.4, based on its origin. The pH 4.3; 4.6 and 6 was selected because these pH isbelow pI of insulin. At a pH lower than its pI value, insulin will be mainly positively charged.This insulin characteristic could be utilised to facilitate insulin–biopolymer complexes throughelectrostatic attraction with tragacanth (negatively charged). Individual and smaller particles withz-average diameters approximately 601 ± 19 nm (mean ± S.D.), were acquired at pH 4.6 with0.5% of tragacanth. The acid gelation test indicated that insulin could be entrapped in the physicalhydrogel of tragacanth. DSC thermograms of insulin–tragacanth showed shifts on the sameunloaded tragacanth peaks and proposed polyelectrolyte–protein interactions at a pH close to 4.3–4.6. FTIR spectra of tragacanth–insulin complexes exhibited amide absorption bands featuring inthe protein spectra and revealed the creation of a new chemical substance.In the previous stage, tragacanth microparticles seem to have potential functional characteristicsfor oral insulin delivery by creating a complex with insulin under defined conditions followed byfreeze drying. Since freeze-drying is up to 30–50 times more expensive than spray-drying and to make the overall process more industrially applicable, spray drying method has been explored inthe third research. A spray-drying process was utilized to create microparticles frominsulin/tragacanth GDL acidified solutions. The complexation process was performed at twotragacanth concentrations (0.5; 1%w/w) and several pH values (3.7; 4.3; 4.6; or 6). The SEManalysis indicated that almost spherical or sub-spherical microparticles were created with adiameter of less than 10 μm. The in vitro insulin release of microparticles prepared at a pH 4.3and 4.6 was substantially minimized in comparison to other pH indicating improved retention ofinsulin. The selection of complexation pH appears to have an impact on insulin release profileand be an important parameter in protecting against peptic digestion. This finding stem from apossible creation of an insulin/tragacanth complex and hydrogel system. The evaluation of theinteraction between insulin and tragacanth at different pH values by ATR-Fourier transforminfrared and differential scanning calorimetry analysis verified this hypothesis. This findingsuggests that these microparticles may act as a potentially promising device for oral insulindelivery." @default.
• W3010129440 created "2020-03-13" @default.
• W3010129440 creator A5081166997 @default.
• W3010129440 date "2019-01-01" @default.
• W3010129440 modified "2023-09-27" @default.
• W3010129440 title "Tragacanth as a novel excipient in oral insulin delivery" @default.
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