Novel Dithranol Loaded Cyclodextrin Nanosponges for Augmentation of Solubility, Photostability and Cytocompatibility

Abstract

Background: Drug loaded β-cyclodextrin based nanosponges (CDNS) are of special interest for the entrapment of moieties with the view to address their physicochemical challenges, and to improve their delivery characteristics and utility. Dithranol (DTH), the standard drug for psoriasis, has poor stability and solubility, which limit its pharmaceutical applications. Objective: The objective of the current study was to entrap DTH in CDNS in order to alleviate the above-mentioned challenges. Methods: To synthesize CDNS, β-cyclodextrin was treated with diphenyl carbonate in various molar ratios. The obtained placebo CDNS were loaded with DTH by lyophilisation. The particle size of the DTH loaded CDNS was found to lie between 150 and 450 nm, with a narrow polydispersity index range. Fourier transform infrared spectroscopy, thermal analysis, X-ray diffraction, zeta potential and electron microscopy with energy dispersive spectroscopy (EDS) were conducted for characterization of DTH-CDNS. Results: Findings from spectral examinations confirmed the formation of inclusion complexes. Solubilisation efficiency of DTH (in distilled water) was found augmented 4.54 folds with optimized CDNS. The cytocompatibility study was performed by the MTT assay employing THP1 cell lines. A remarkable amelioration in stability and photostability of DTH was also observed by its inclusion in nanosponges. Conclusion: In a nutshell, we report the rational engineering and characterization of DTH loaded cyclodextrin-based nanosponges, and subsequently, their stepwise screening for photostability, in vitro release, in vitro cytocompatibility, in vitro antioxidant and in vitro inflammatory activity in a top-down manner, yielding the best carrier for this drug.