title: Cyclodextrin-based nanosponges: effective nanocarrier for tamoxifen delivery.
abstract: The purpose of the present study was to develop Tamoxifen loaded β-cyclodextrin nanosponges for oral drug delivery. The three types of Tamoxifen loaded β-cyclodextrin nanosponges were synthesized by varying the molar ratios of β-cyclodextrin to carbonyldiimidazole as a crosslinker viz. 1:2, 1:4 and 1:8. The Tamoxifen nanosponge complex (TNC) with particle size of 400-600 nm was obtained by freeze drying method. Differential scanning calorimetry, Fourier transformed infra-red spectroscopy and X-ray powder diffraction studies confirmed the complexation of Tamoxifen with cyclodextrin nanosponge. AUC and Cmax of TNC formulation (1236.4 ± 16.12 µg · mL(-1) h, 421.156 ± 0.91 µg/mL) after gastric intubation were 1.44 fold and 1.38 fold higher than plain drug (856.079 ± 15.18 µg · mL(-1) h, 298.532 ± 1.15 µg/mL). Cytotoxic studies on MCF-7 cells showed that TNC formulation was more cytotoxic than plain Tamoxifen after 24 and 48 h of incubation.
authors.affiliation: Pharmaceutical Sciences and Technology, University Institute of Chemical Technology, Mumbai, India.
authors.forename: Satyen
authors.initials: S
authors.lastname: Torne
authors.forename: Sharad
authors.initials: S
authors.lastname: Darandale
authors.forename: Pradeep
authors.initials: P
authors.lastname: Vavia
authors.forename: Francesco
authors.initials: F
authors.lastname: Trotta
authors.forename: Roberta
authors.initials: R
authors.lastname: Cavalli
mesh_terms: D000818:Animals; D049109:Cell Proliferation / Q000187:drug effects; D003505:Cyclodextrins / Q000008:administration & dosage / Q000737:chemistry*; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry*; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D061986:MCF-7 Cells; D054118:Nanospheres / Q000008:administration & dosage / Q000737:chemistry*; D011897:Random Allocation; D051381:Rats; D013629:Tamoxifen / Q000008:administration & dosage / Q000737:chemistry*; D014961:X-Ray Diffraction
chemical_list: D003505:Cyclodextrins; D004337:Drug Carriers; D013629:Tamoxifen