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  • In vitro evaluation of thiolated polydimethylaminoethylmethacrylate hydrogel sub-microparticles for oral insulin delivery.

In vitro evaluation of thiolated polydimethylaminoethylmethacrylate hydrogel sub-microparticles for oral insulin delivery.

Journal of biomedical nanotechnology (2013-04-30)
T A Sonia, Chandra P Sharma
ABSTRACT

In this investigation, novel cationic thiomer, Thiolated polydimethylaminoethylmethacrylate (PDCys) is synthesised and the feasibility of PDCys sub-microparticles as oral insulin delivery carriers is evaluated in vitro. The presence of both positive charge and thiol group in the same matrix plays a vital role in improving the paracellular permeability. Thiol groups interacts with cysteine rich subdomains via disulfide bond formation and positive charge interacts with sialic residues of mucus glycoproteins via electrostatic interaction, thereby increasing the mucoadhesivity. Cytotoxic evaluation by MTT assay shows that PDCys is nontoxic. Force and Work of adhesion of PDCys was found found to be higher than that of parent polymer. ELISA and Circular dichroism spectra confirms that PDCys retains the biological activity and conformation of insulin. Moreover, PDCys is capable of opening the tight junctions by actin and occludin filament dislocation. Furthermore, permeation of FD4 on Caco-2 cells is improved by 3.9 fold compared to the parent polymer. Preliminary studies suggest that thiolated particles can serve as potential vehicles for oral insulin delivery.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Poly(ethylene glycol) dimethacrylate, average Mn 550, contains 80-120 ppm MEHQ as inhibitor, 270-330 ppm BHT as inhibitor
Sigma-Aldrich
Poly(ethylene glycol) dimethacrylate, average Mn 750, contains 900-1100 ppm MEHQ as inhibitor
Sigma-Aldrich
Poly(ethylene glycol) dimethacrylate, average Mn 20,000, contains MEHQ as inhibitor
Sigma-Aldrich
Poly(ethylene glycol) dimethacrylate, average Mn 10,000, contains MEHQ as inhibitor
Sigma-Aldrich
Poly(ethylene glycol) dimethacrylate, average Mn 2000, contains ~1000 ppm MeHQ as stabilizer
Sigma-Aldrich
Poly(ethylene glycol) dimethacrylate, average Mn 6,000, contains 1000 ppm 4-methoxyphenol as inhibitor
Sigma-Aldrich
Poly(methyl methacrylate-co-methacrylic acid), average Mw ~34,000 by GPC, average Mn ~15,000 by GPC