| Literature DB >> 30832855 |
Anurag Lodagekar1, Roshan M Borkar2, Sowjanya Thatikonda3, Rahul B Chavan4, V G M Naidu3, Nalini R Shastri4, R Srinivas2, Naveen Chella5.
Abstract
Niclosamide, previously used as an anthelmintic drug is currently being repurposed for its anticancer activity. Niclosamide is a brick like biopharmaceutical classification system (BCS) class II drug with poor aqueous solubility and dissolution consequently leading to low bioavailability. By considering the physicochemical properties and geometry of niclosamide, inclusion complex with cyclodextrin was prepared by freeze drying method and characterized using FT-IR, DSC, PXRD, and 1HNMR. In silico molecular modeling study was performed to study the possible interactions between niclosamide and cyclodextrin. The anticancer activity of niclosamide formulation was evaluated through in vitro cell cytotoxicity study using various cancer cell lines. The potential of niclosamide complex for improvement of the bioavailability was evaluated in male BALB/c mice. In vitro cytotoxicity studies indicated significantly higher cytotoxicity at lower concentrations and the pharmacokinetic studies showed significant improvement in Cmax and Tmax of niclosamide from cyclodextrin complex in comparison to pure niclosamide alone.Entities:
Keywords: Analytical method by LC–MS; Bioavailability; Hydroxypropyl-β-cyclodextrin; Inclusion complex; Molecular modeling
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Year: 2019 PMID: 30832855 DOI: 10.1016/j.carbpol.2019.02.041
Source DB: PubMed Journal: Carbohydr Polym ISSN: 0144-8617 Impact factor: 9.381