Page 57 - _NIPER-G Annual Report 2019-201

Research Area-7

Formulation and evaluation of cyclodextrin complexes for improved anticancer activity
of repurposed drug: Niclosamide (Collaboration with NIPER Hyderabad)
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.

Lodagekar A, Borkar RM, Thatikonda S, Chavan RB, Naidu VG, Shastri NR, Srinivas R, Chella
N. Formulation and evaluation of cyclodextrin complexes for improved anticancer activity of
repurposed drug: Niclosamide. Carbohydrate polymers. 2019 May 15; 212:252-9.

Graphical Abstract

Figure A and B: Effect of formulations 1:1 and plain niclosamide on morphological changes after
treatment at concentrations of 0.1, 0.2, 0.4, 0.6 μg/ml for 24 h A) NCI-H460 cell line and B) HCT-116
cell line fluorescent images.

54 NIPER-G