title: Use of xanthan and its binary blends with synthetic polymers to design controlled release formulations of buccoadhesive nystatin tablets.
abstract: Various buccoadhesive nystatin tablets formulations containing xanthan, carbopols (934P, 971P, 974P), PVP K30 or PEG 6000 or their binary blends were prepared. The powders were compressed into tablets at a constant compression pressure. Drug release behaviour, swelling and erosion indices and strength of bioadhesion in vitro to a biological membrane were investigated. The interaction between nystatin and polymers was investigated by DSC and FT-IR. Tablets containing the different types of carbopol alone consistently showed an initial burst release of drug, whereas this was not observed for matrices containing xanthan or xanthan-carbopol. The presence of PEG in xanthan-containing formulations induced an increase in dissolution rate; however, in the absence of xanthan the amount of drug release from a PEG matrix was reduced to < 15% over 8 h dissolution. The presence of PVP increased the dissolution rate of nystatin due to the relative hydrophilicity of PVP. The presence of calcium ions induced a more rigid gel in the xanthan matrix as a result of interaction between the polymer and calcium ions. Xanthan can be used in potential mucoadhesive formulations containing nystatin to produce a controlled release of the drug and the outcomes of this work may provide a suitable strategy for matrix selection to provide more efficacious treatment alternatives for candidiasis and other disease processes for significant patient populations.
authors.affiliation: Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Damascus University, Syria.
authors.forename: Khalil
authors.initials: K
authors.lastname: Sakeer
authors.forename: Hind
authors.initials: H
authors.lastname: Al-Zein
authors.forename: Issa
authors.initials: I
authors.lastname: Hassan
authors.forename: Gary P
authors.initials: GP
authors.lastname: Martin
authors.forename: Ali
authors.initials: A
authors.lastname: Nokhodchi
mesh_terms: D000268:Adhesiveness; D000278:Administration, Buccal; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage / Q000737:chemistry; D002118:Calcium / Q000378:metabolism; D002152:Calorimetry, Differential Scanning; D003692:Delayed-Action Preparations; D005079:Excipients / Q000737:chemistry*; D009061:Mouth Mucosa / Q000378:metabolism; D009761:Nystatin / Q000008:administration & dosage* / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D011135:Polysaccharides, Bacterial / Q000737:chemistry*; D011817:Rabbits; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013607:Tablets
chemical_list: D000935:Antifungal Agents; D003692:Delayed-Action Preparations; D005079:Excipients; D011108:Polymers; D011135:Polysaccharides, Bacterial; D013607:Tablets; D009761:Nystatin; D002118:Calcium; C002563:xanthan gum