Disulfide-Bridged Chitosan-Eudragit S-100 Nanoparticles for Colorectal Cancer

Abstract

Covalently bonded Eudragit S-100 (EU) and chitosan (CS) based colon-specific nanoparticles (CSE NPs) were fabricated as drug carriers for treating colorectal cancers through oral administration. Thiolation of EU and CS prevents the usage of the cross-linking agent. This gives an advantage over the shortcomings of existing EU- and CS-based delivery systems that are associated with large sized nanoparticles with a broad range of size distribution. Paclitaxel (PTX)-loaded CSE NPs presented an efficacy of 8–10% after 48 h of treatment on the HCT 116 cell line signifying uniform distribution of drug inside the cells. About 66% accumulation of cell population was observed in G2/M phase for PTX-loaded CSE NPs, indicating arrest of cell division during the mitotic phase. Biodistribution studies on male Balb/C mice demonstrated retention of CSE NPs in the colon region up to 24 h post oral administration. These findings confer a convenient and effective way for preparing CS- and EU-based drug delivery systems with sustained release and target specificity for colorectal cancers.

The influence of the gut microbiota on the bioavailability of oral drugs

“… Polysaccharide Delivery system Drug/payload molecule Therapeutic application Feature Ref. Chitosan Chitosan-capped enzyme-responsive hollow mesoporous silica nanoplatforms Doxorubicin Not mentioned in the literature Bacterial enzyme sensitive 192 Chitosan Eudragit S-100 and chitosan-based nanoparticles Paclitaxel Colorectal cancer Sustained release, pH responsive, bacterial enzyme sensitive and cancer-targeted 193 Amphipathic chitosan derivative Amphiphilic chitosan derivatives and cell-penetrating peptides modified nanoparticles Insulin Lowering the blood glucose The bacterial enzyme sensitive delivery and the use of cell-penetrating peptides 194 Chondroitin sulfate Tablets coated by Surelease® and chondroitin sulfate Dapsone Not mentioned in the literature Time-dependent and bacterial enzyme sensitive 195 Dextran The doxorubicin and superparamagnetic iron oxide nanoparticles-loaded solid lipid nanoparticle coated with folate and dextran Doxorubicin and superparamagnetic iron oxide nanoparticles Colon cancer The microbial enzyme sensitive and tumor-targeted delivery system used for chemo/magnetothermal combination therapy 196 Guar gum The guar gum modified upconversion nanocomposite 5-Fluorouracil Colorectal cancer Bacterial enzyme sensitive and NIR triggered 197 Guar gum Transformable capsules containing indomethacin immediate-release pellets Indomethacin Colon cancer Bacterial enzyme sensitive 198 Guar gum Microspheres Mesalamine and synbiotics Ulcerative colitis Bacterial enzyme sensitive 199 Guar gum 5-Flurouracil-containing mesoporous silica nanoparticles with guar gum capping 5-Flurouracil …”

Disulfide Bridged Nanoparticles of Thiolated Sodium Alginate and Eudragit RS100 for Oral Delivery of Paclitaxel: In Vitro and In Vivo Evaluation

“…5 Over the past ten years, the importance of ERS100, a synthetic polymer with a pH verge of more than 7, has grown in the field of medicinal formulations. 6 Some of the features that make ERS100 a reliable choice for treating colorectal malignancies are gut targeting and value in sustained drug release. We have the possibility to improve the efficacy of drug therapy and transition to an oral route of drug administration by combining ERS100 with SA nanoparticulate systems.…”

Thiolated Nanoparticles for Biomedical Applications: Mimicking the Workhorses of Our Body

“…[34,185] Chang et al developed thiolated alginate-based nanoparticles with improved colonic targeting potential, demonstrated by a marked increase in drug release in a colonic pH mimic and reducing fluid. [34] Providing a highly effective tool in the targeted treatment of colon cancer and inflammatory bowel disease, other research groups have followed and established thiolate alginate-based nanocarriers for budesonide, docetaxel, and doxorubicin [186,187] In addition, paclitaxel (PTX)-loaded NPs based on chitosan-Eudragit S-100 with disulfide bond (CSE NP) were developed by Sood et al [188] After 48 h of treatment of HCT116 colon cancer cells, they observed a uniform distribution of PTX within the cells and a significant accumulation in the G2/M phase after 24 h, indicating the arrest of cell division during the mitotic phase. In subsequent in vivo biodistribution studies in male Balb/C mice, a retention of NPs in the colonic region up to 24 h after oral administration provided strong evidence for colon-specific targeting.…”