title: Hyaluronan-cisplatin conjugate nanoparticles embedded in Eudragit S100-coated pectin/alginate microbeads for colon drug delivery.
abstract: Hyaluronan-cisplatin conjugate nanoparticles (HCNPs) were chosen as colon-targeting drug-delivery carriers due to the observation that a variety of malignant tumors overexpress hyaluronan receptors. HCNPs were prepared by mixing cisplatin with a hyaluronan solution, followed by dialysis to remove trace elements. The cells treated with HCNPs showed significantly lower viability than those treated with cisplatin alone. HCNPs were entrapped in Eudragit S100-coated pectinate/alginate microbeads (PAMs) by using an electrospray method and a polyelectrolyte multilayer-coating technique in aqueous solution. The release profile of HCNPs from Eudragit S100-coated HCNP-PAMs was pH-dependent. The percentage of 24-hour drug release was approximately 25.1% and 39.7% in pH 1.2 and pH 4.5 media, respectively. However, the percentage of drug released quickly rose to 75.6% at pH 7.4. Moreover, the result of an in vivo nephrotoxicity study demonstrated that Eudragit S100-coated HCNP-PAMs treatment could mitigate the nephrotoxicity that resulted from cisplatin. From these results, it can be concluded that Eudragit S100-coated HCNP-PAMs are promising carriers for colon-specific drug delivery.
authors.affiliation: Graduate Institute of Biochemical and Biomedical Engineering, Chang Gung University, Taoyuan, Taiwan.
authors.forename: Shiao-Wen
authors.initials: SW
authors.lastname: Tsai
authors.forename: Ding-Syuan
authors.initials: DS
authors.lastname: Yu
authors.forename: Shu-Wei
authors.initials: SW
authors.lastname: Tsao
authors.forename: Fu-Yin
authors.initials: FY
authors.lastname: Hsu
mesh_terms: D000464:Alginates / Q000737:chemistry / Q000493:pharmacokinetics; D000818:Animals; D001835:Body Weight / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D002945:Cisplatin / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity; D003110:Colonic Neoplasms; D020723:Glucuronic Acid / Q000737:chemistry / Q000493:pharmacokinetics; D045325:HCT116 Cells; D006603:Hexuronic Acids / Q000737:chemistry / Q000493:pharmacokinetics; D006801:Humans; D006820:Hyaluronic Acid / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D008297:Male; D008863:Microspheres; D058726:Nanoconjugates / Q000737:chemistry* / Q000633:toxicity; D010368:Pectins / Q000737:chemistry / Q000493:pharmacokinetics; D011109:Polymethacrylic Acids / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D017208:Rats, Wistar
chemical_list: D000464:Alginates; D006603:Hexuronic Acids; D058726:Nanoconjugates; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; D010368:Pectins; D020723:Glucuronic Acid; D006820:Hyaluronic Acid; D002945:Cisplatin
keywords: alginate; cisplatin; drug delivery; hyaluronan; pH-dependent; pectin