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Graphical abstract Highlights • βCD-based nanosponges (CDNSs) were prepared for curcumin (CUR) encapsulation. • The molar ratio of EPI to βCD strongly affected the CDNSs characteristics. • Free CDNSs showed no toxicity confirming their cytocompatibilty. • CUR encapsulation in CDNSs enhanced the selective toxicity against cancerous cells. • The best CUR loading and toxicity was obtained for CDNS8 having highest EPI ratio. Abstract A novel β-cyclodextrin-based nanosponge (CDNS) was proposed as curcumin (CUR) delivery system improving pharmacokinetics and anticancer activity of CUR. The effect of molar ratio of Epiclon (EPI) as cross-linker and β-cyclodextrin (βCD) on the porosity, surface area, swelling ratio, CUR solubility and loading capacity, rate of drug release and selective toxicity of the CDNSs was fully investigated. The high degree of cross-linking led to the formation of mesoporous CDNS having high specific surface area and high loading capacity. All CUR-free CDNSs showed no toxicity against MCF 10A and 4T1 cells as normal and cancerous cells, respectively. While CDNSs-CUR exhibited selective toxicity against cancerous cells. In sum, high CUR aqueous solubility, significant loading and controllable release of the CUR, outstanding and selective toxicity against cancerous cells make CDNS8-CUR (EPI/βCD = 8) as promising candidate for further study in the cancer therapy. [ABSTRACT FROM AUTHOR]

• A novel theranostic nano-system was designed based on Magnetite decorated with Gd3+ ions. • Novel polycyclodextrin was prepared for Gd3+ ions chelation and curcumin delivery. • The target system showed more toxicity against 4T1 than MCF 10A cells. • In vivo anti-tumor study confirmed capability of the system in tumor shrinking without body weight changes. • In vitro and in vivo analysis showed efficacy of the system for T 1 -T 2 dual modality MR imaging. A novel theranostic nanoplatform was prepared based on Fe 3 O 4 nanoparticles (NPs) coated with gadolinium ions decorated-polycyclodextrin (PCD) layer (Fe 3 O 4 @PCD-Gd) and employed for Curcumin (CUR) loading. The dissolution profile of CUR indicated a pH sensitive release manner. Fe 3 O 4 @PCD-Gd NPs exhibited no significant toxicity against both normal and cancerous cell lines (MCF 10A and 4T1, respectively); while the CUR-free NPs showed more toxicity against 4T1 than MCF 10A cells. In vivo anticancer study revealed appropriate capability of the system in tumor shrinking with no tissue toxicity and adverse effect on body weight. In vivo MR imaging of BALB/c mouse showed both T 1 and T 2 contrast enhancement on the tumor cells. Fe 3 O 4 @PCD-Gd/CUR NPs showed significant features as a promising multifunctional system having appropriate T 1 -T 2 dual contrast enhancement and therapeutic efficacy in cancer theranostics. [ABSTRACT FROM AUTHOR]

In an attempt to find new potent cytotoxic compounds, several mono- and bis-pyrazolophthalazines 4a-m and 6a-h were synthesized through an efficient, one-pot, three- and pseudo five-component synthetic approach. All derivatives were evaluated for their in vitro cytotoxic activities against four human cancer cell lines of A549, HepG2, MCF-7, and HT29. Compound 4e showed low toxicity against normal cell lines (MRC-5 and MCF 10A, IC 50 > 200 µM) and excellent cytotoxic activity against A549 cell line with IC 50 value of 1.25 ± 0.19 µM, which was 1.8 times more potent than doxorubicin (IC 50 = 2.31 ± 0.13 µM). In addition, compound 6c exhibited remarkable cytotoxic activity against A549 and MCF-7 cell lines (IC 50 = 1.35 ± 0.12 and 0.49 ± 0.01 µM, respectively), more than two-fold higher than that of doxorubicin. The binding properties of the best active mono- and bis-pyrazolophthalazine (4e and 6c) with HSA and DNA were fully evaluated by various techniques including UV–Vis absorption, circular dichroism (CD), Zeta potential and dynamic light scattering analyses indicating interaction of the compounds with the secondary structure of HSA and significant change of DNA conformation, presumably via a groove binding mechanism. Additionally, molecular docking and site-selective binding studies confirmed the fundamental interaction of compounds 4e and 6c with base pairs of DNA. Compounds 4e and 6c showed promising features to be considered as potential lead structures for further studies in cancer therapy. [ABSTRACT FROM AUTHOR]