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 C_max 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.

Keywords::

• Cyclodextrin nanosponge
• Tamoxifen
• nanocarrier

Acknowledgements

Authors are also thankful to Intox Ltd, India for providing facility to conduct the pharmacokinetic studies.

Declaration of interest

Authors are thankful to Sea Marconi Technologies (Collegno, Italy), University Grant Commission (UGC) India and AICTE NAFETIC for funding the research. The authors report no conflicts of interest.