title: The effects of the thiolation with thioglycolic acid and l-cysteine on the mucoadhesion properties of the starch-graft-poly(acrylic acid).
abstract: The aim of this study is to investigate the effects of the thiolation on the mucoadhesion characteristics of the gelatinized and crosslinked wheat starch-graft-poly(acrylic acid) [(WS-g-PAA)gc] for potential use in drug delivery via vaginal route. Thiolation of (WS-g-PAA)gcwas first time realized using l-cysteine hydrochloride monohydrate (CyS) and thioglycolic acid (TGA). These conjugates [(WS-g-PAA)gcth] were characterized using FTIR. The free SH group, mucoadhesion, cytotoxicity characteristics and the mechanism of the thiolation were also evaluated. To obtain fundamental data for possible application such as drug carrier, in vitro and in vivo progesterone release profiles from the mucoadhesive tablet formulations were also determined. The results showed that, vaginal tablet containing (WS-g-PAA)gc-TGA, which has not contain free SH groups in its structure, displays higher mucoadhesion than (WS-g-PAA)gcand (WS-g-PAA)gc-CyS. This tablet formulation can also be used as a drug carrier in vaginal applications.
authors.affiliation: Department of Chemical Engineering, Faculty of Engineering, Istanbul University, 34320 Avcilar, Istanbul, Turkey.
authors.forename: M Koray
authors.initials: MK
authors.lastname: Gök
authors.affiliation: Department of Reproduction and Artificial Insemination, Faculty of Veterinary Medicine, Istanbul University, 34320 Avcilar, Istanbul, Turkey.
authors.forename: Kamber
authors.initials: K
authors.lastname: Demir
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, Istanbul University, 34116 Beyazit, Istanbul, Turkey.
authors.forename: Erdal
authors.initials: E
authors.lastname: Cevher
authors.affiliation: Department of Pharmaceutical Technology, Faculty of Pharmacy, Istanbul University, 34116 Beyazit, Istanbul, Turkey.
authors.forename: Yıldız
authors.initials: Y
authors.lastname: Özsoy
authors.affiliation: Department of Reproduction and Artificial Insemination, Faculty of Veterinary Medicine, Dicle University, 21280 Campus/Diyarbakır, Turkey.
authors.forename: Ümüt
authors.initials: Ü
authors.lastname: Cirit
authors.affiliation: Biopharm Aşı İlaç San. ve Tic. Ltd. Şti., Dolayoba cad. Tolga Sok. No: 3, 34896 Pendik, Istanbul, Turkey.
authors.forename: Süleyman
authors.initials: S
authors.lastname: Bacınoğlu
authors.affiliation: Department of Chemical Engineering, Faculty of Engineering, Istanbul University, 34320 Avcilar, Istanbul, Turkey. Electronic address: saadetk@istanbul.edu.tr.
authors.forename: Saadet
authors.initials: S
authors.lastname: Özgümüş
authors.affiliation: Department of Reproduction and Artificial Insemination, Faculty of Veterinary Medicine, Istanbul University, 34320 Avcilar, Istanbul, Turkey.
authors.forename: Serhat
authors.initials: S
authors.lastname: Pabuccuoğlu
mesh_terms: D003545:Cysteine / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D005260:Female; D006801:Humans; D013213:Starch / Q000031:analogs & derivatives* / Q000737:chemistry; D013864:Thioglycolates / Q000737:chemistry*; D014621:Vagina
chemical_list: D004337:Drug Carriers; D013864:Thioglycolates; C017487:2-mercaptoacetate; D013213:Starch; C043831:starch polyacrylate; D003545:Cysteine
keywords: Mucoadhesion; Starch; Thioglycolic acid; Thiolation; Vaginal tablet; l-Cysteine