title: Synthesis, characterization of thiolated karaya gum and evaluation of effect of pH on its mucoadhesive and sustained release properties.
abstract: Present study aims at synthesis and characterization of thiolated gum karaya by reacting karaya gum with 80% thioglycolic acid resulting in esterification and immobilization of thiol groups on polymeric backbone. Immobilized thiol groups were found to be 5.026 mM/g determined by Ellman's method. It was characterized by FTIR, DSC and XRD. Directly compressible tablets prepared using thiolated gum displayed more disintegration time, swelling and mucoadhesion with increase in pH of medium simulating gastric and intestinal environment than plain gum. Controlled drug release for more than 24h by Fickian diffusion following Korsemeyer-Peppas model was observed with Metoprolol Succinate as a model drug as compared to plain gum which released more than 90% of the drug within 2h. Synthesized thiomer showed no cytotoxicity determined using HepG2 cell line. According to these results, thiolated gum karaya seems to be promising excipient for the development of mucoadhesive drug delivery systems.
authors.affiliation: Department of Pharmaceutics, Sinhgad Technical Education Society's Smt. Kashibai Navale College of Pharmacy, Kondhwa(Bk), Pune, 411038, India. Electronic address: swati.bahulkar@gmail.com.
authors.forename: Swati S
authors.initials: SS
authors.lastname: Bahulkar
authors.affiliation: Department of Pharmaceutics, Sinhgad Technical Education Society's Smt. Kashibai Navale College of Pharmacy, Kondhwa(Bk), Pune, 411038, India. Electronic address: nehamunot@yahoo.com.
authors.forename: Neha M
authors.initials: NM
authors.lastname: Munot
authors.affiliation: Physical and Material Chemistry Division, CSIR-National Chemical Laboratory, Dr. Homi Bhabha Road, Pune, 411008, India. Electronic address: sachingcopk@gmail.com.
authors.forename: Sachin S
authors.initials: SS
authors.lastname: Surwase
mesh_terms: D000818:Animals; D002152:Calorimetry, Differential Scanning; D003692:Delayed-Action Preparations / Q000737:chemistry; D016503:Drug Delivery Systems; D005079:Excipients / Q000737:chemistry*; D056945:Hep G2 Cells / Q000187:drug effects; D006801:Humans; D006863:Hydrogen-Ion Concentration; D007413:Intestinal Mucosa; D007618:Karaya Gum / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D017550:Spectroscopy, Fourier Transform Infrared; D013438:Sulfhydryl Compounds / Q000737:chemistry; D013607:Tablets / Q000737:chemistry*; D014961:X-Ray Diffraction
chemical_list: D003692:Delayed-Action Preparations; D005079:Excipients; D013438:Sulfhydryl Compounds; D013607:Tablets; D007618:Karaya Gum
keywords: Cytotoxicity; Ellman's method; Metoprolol succinate; Mucoadhesion; Thiolated gum karaya