Eudragit S100 Coated Citrus Pectin Nanoparticles for Colon Targeting of 5-Fluorouracil

Abstract

Abstract:In the present study, Eudragit S100 coated Citrus Pectin Nanoparticles (E-CPNs) were prepared for the colon targeting of 5-Fluorouracil (5-FU). Citrus pectin also acts as a ligand for galectin-3 receptors that are over expressed on colorectal cancer cells. Nanoparticles (CPNs and E-CPNs) were characterized for various physical parameters such as particle size, size distribution, and shape etc. In vitro drug release studies revealed selective drug release in the colonic region in the case of E-CPNs of more than 70% after 24 h. In vitro cytoxicity assay (Sulphorhodamine B assay) was performed against HT-29 cancer cells and exhibited 1.5 fold greater cytotoxicity potential of nanoparticles compared to 5-FU solution. In vivo data clearly depicted that Eudragit S100 successfully guarded nanoparticles to reach the colonic region wherein nanoparticles were taken up and showed drug release for an extended period of time. Therefore, a multifaceted strategy is introduced here in terms of receptor mediated uptake and pH-dependent release using E-CPNs for effective chemotherapy of colorectal cancer with uncompromised safety and efficacy.

Eudragit S100 Entrapped Liposome for Curcumin Delivery: Anti-Oxidative Effect in Caco-2 Cells

“…In order to obtain gastro-resistant vesicles, curcumin-loaded liposomes covered with Eudragit®(Eu-Curc-liposome) were obtained according to a recently described method [24], which allows to obtain clusters of vesicles covered with polymer capable of protecting liposomes and their payload from the acid compartments of the gastrointestinal tract. In acid environment, the obtained Eu-curc-liposomes showed micrometric dimensions with negative zeta potentials, as observed by other authors for methacrylic acid-methyl methacrylate (1:2) copolymer nanoparticles [29]. Before proceeding to cell-based experiments, the Eu-curc-liposomes samples were incubated in PBS at pH 7.5, in order to evaluate the behavior of the polymeric coating at pH values similar to those in which they would be found in vivo at absorption site.…”

“…The zeta potential values are negative and, in absolute value, higher than those measured at acid pH. This evidence suggests that Eudragit residues remain on the surface of the vesicles, and the zeta potential values recorded are to be attributed to the presence of free acrylic acid groups on the vesicle surface [29]. The TEM images obtained (Figure 1) confirmed the Eudragit layer dissolution passing from acid environment (panel B) to pH higher than 7.0 (panel C).…”

Chondroitin sulphate: a focus on osteoarthritis

“…[126,127] Novel drug delivery systems of CS Polysaccharide based novel drug delivery systems have emerged with great success [97][98][99]. Over the past few years, plethora of novel drug delivery systems based on CS came into existence either as a ligand or a drug.…”

Novel chewable colon targeted tablets of bumadizone calcium for treatment of ulcerative colitis: Formulation and optimization

“…We aimed to decrease the percentage of drug released before target area (pH 1.2 and 6.8) to less than 20 % [33] and to maximize the BZ released in target area (pH 7.4) and total BZ released after 12 hours.…”