title: Preparation and evaluation of microspheres of xyloglucan and its thiolated xyloglucan derivative.
abstract: Xyloglucan is a natural polymer reported to possess mucoadhesive properties. To enhance the mucoadhesion potential, xyloglucan was thiolated with cysteine. The microspheres of xyloglucan were prepared using a biocompatible crosslinker sodium trimetaphosphate and it was optimized for formulation variables, namely polymer concentration, internal:external phase ratio and stirring speed using a Box-Behnken experimental design. The formulation was also optimized for performance parameters like entrapment, t80 and % mucoadhesion. The microspheres were characterized by Fourier transform infrared spectroscopy, DSC and SEM for the optimum formula and then were reproduced by replacing the xyloglucan with thiomer. The microspheres formed showed entrapment efficiency of about 80%, t80 of about 400min and % mucoadhesion of 60% while same for thiomer were 90%, 500min and 80% respectively. In oral glucose tolerance test protocol the thiomer microspheres showed significant reduction in blood glucose levels. Thus thiolated xyloglucan offers a better polymer for multiparticulate drug delivery.
authors.affiliation: Faculty of Pharmaceutical Sciences, JNTU Hyderabad, Kukatpally, Hyderabad, India; MNR College of Pharmacy, MNR Nagar, Sangareddy, India. Electronic address: savita.sonawane@rediffmail.com.
authors.forename: Savita
authors.initials: S
authors.lastname: Sonawane
authors.affiliation: AISSMS College of Pharmacy, Pune, India.
authors.forename: Mangesh
authors.initials: M
authors.lastname: Bhalekar
authors.affiliation: APL Research Centre, Aurobindo Pharma Ltd., Hyderabad, India.
authors.forename: Shamkant
authors.initials: S
authors.lastname: Shimpi
mesh_terms: D000269:Adhesives / Q000737:chemistry; D000818:Animals; D003692:Delayed-Action Preparations; D004337:Drug Carriers / Q000737:chemistry*; D005260:Female; D005913:Glipizide / Q000737:chemistry / Q000494:pharmacology; D005936:Glucans / Q000737:chemistry*; D005951:Glucose Tolerance Test; D008297:Male; D008863:Microspheres; D009092:Mucous Membrane / Q000737:chemistry; D011122:Polyphosphates / Q000737:chemistry; D051381:Rats; D013438:Sulfhydryl Compounds / Q000737:chemistry*; D013696:Temperature; D014990:Xylans / Q000737:chemistry*
chemical_list: D000269:Adhesives; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005936:Glucans; D011122:Polyphosphates; D013438:Sulfhydryl Compounds; D014990:Xylans; C029353:xyloglucan; C009293:trimetaphosphoric acid; D005913:Glipizide
keywords: Microspheres; Thiolation; Xyloglucan