Thiolated pectin-chitosan composites: Potential mucoadhesive drug delivery system with selective cytotoxicity towards colorectal cancer.

Mucoadhesive drug delivery systems (DDS) may promote safer chemotherapy for colorectal cancer (CRC) by maximizing local drug distribution and residence time. Carbohydrate polymers, e.g. pectin (P) and chitosan (CS), are potential biomaterials for CRC-targeted DDS due to their gelling ability, mucoadhesive property, colonic digestibility, and anticancer activity. Polymer mucoadhesion is augmentable by thiolation, e.g. pectin to thiolated pectin (TP). Meanwhile, P-CS polyelectrolyte complex has been shown to improve structural stability. Herein, we fabricated, characterized, and evaluated 5-fluorouracil-loaded primary DDS combining TP and CS as a composite (TPCF) through triple crosslinking actions (calcium pectinate, polyelectrolyte complex, disulfide). Combination of these crosslinking yields superior mucoadhesion property relative to single- or dual-crosslinked counterparts, with comparable drug release profile and drug compatibility. PCF and TPCF exhibited targeted cytotoxicity towards HT29 CRC cells with milder cytotoxicity towards HEK293 normal cells. In conclusion, TP-CS composites are promising next-generation mucoadhesive and selectively cytotoxic biomaterials for CRC-targeted DDS.

Curcuma longa ethanol extract and Curcumin inhibit the growth of Acanthamoeba triangularis trophozoites and cysts isolated from water reservoirs at Walailak University, Thailand.

CURCUMA LONGA: (C. longa) rhizome extract has been traditionally used to treat many infections. Curcumin, a pure compound isolated from the plant, has been documented to possess a wide spectrum of pharmacological effects. The present study aimed to investigate the effects of Thai medicinal plant extracts including C. longa extract and Curcumin on Acanthamoeba triangularis, a causative agent of human Acanthamoeba keratitis. The parasite was isolated from the recreational reservoir at Walailak University, Thailand. The organism was identified as A. triangularis using morphology and 18S rDNA nucleotide sequences. The pathogen was tested for their susceptibility to ethanol extracts of Thai medicinal plants based on eye infection treatment. The ethanol C. longa extract showed the strongest anti-Acanthamoeba activity against both the trophozoites and cysts, followed by Coscinium fenestratum, Coccinia grandis, and Acmella oleracea extracts, respectively. After 24 h, 95% reduction of trophozoite viability was significantly decreased following the treatment with C. longa extract at 125 µg/mL, compared with the control (P < 0.05). The extract at 1,000 µg/mL inhibited 90% viability of Acanthamoeba cyst within 24 h, compared with the control. It was found that the cysts treated with C. longa extract at 500 µg/mL demonstrated abnormal shape after 24 h. The MIC values of C. longa extract and Curcumin against the trophozoites were 125 and 62.5 µg/mL, respectively. While the MICs of the extract and curcumin against the cysts were 500 and 1,000 µg/mL, respectively. The results suggested the potential medicinal benefits of C. longa extract and Curcumin as the alternative treatment of Acanthamoeba infections.