4.5 Article

Inclusion Complex of Novel Curcumin Analogue CDF and β-Cyclodextrin (1:2) and Its Enhanced In Vivo Anticancer Activity Against Pancreatic Cancer

期刊

PHARMACEUTICAL RESEARCH
卷 29, 期 7, 页码 1775-1786

出版社

SPRINGER/PLENUM PUBLISHERS
DOI: 10.1007/s11095-012-0700-1

关键词

CDF; curcumin analog; CDF-beta-Cyclodextrin; pancreatic cancer

资金

  1. CSIR, New Delhi, INDIA

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Several formulations have been proposed to improve the systemic delivery of novel cancer therapeutic compounds, including cyclodextrin derivatives. We aimed to synthesize and characterize of CDF-beta-cyclodextrin inclusion complex (1:2) (CDFCD). The compound was characterized by Fourier transform infrared, differential scanning calorimetry, powder X-ray diffraction studies, H1 & C13 NMR studies and scanning electron microscopic analysis. Its activity was tested against multiple cancer cell lines, and in vivo bioavailability was checked. CDF-beta-cyclodextrin was found to lower IC50 value by half when tested against multiple cancer cell lines. It preferentially accumulated in the pancreas, where levels of CDF-beta-cyclodextrin in mice were 10 times higher than in serum, following intravenous administration of an aqueous CDF-beta-cyclodextrin preparation. Novel curcumin analog CDF preferentially accumulates in the pancreas, leading to its potent anticancer activity against pancreatic cancer cells. Synthesis of such CDF-beta-cyclodextrin self-assembly is an effective strategy to enhance its bioavailability and tissue distribution, warranting further evaluation for CDF delivery in clinical settings for treatment of human malignancies.

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