Inclusion complex of novel curcumin analogue CDF and β-cyclodextrin (1:2) and its enhanced in vivo anticancer activity against pancreatic cancer.
OBJECTIVE
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-β-cyclodextrin inclusion complex (1:2) (CDFCD).


METHODS
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.


RESULTS
CDF-β-cyclodextrin was found to lower IC(50) value by half when tested against multiple cancer cell lines. It preferentially accumulated in the pancreas, where levels of CDF-β-cyclodextrin in mice were 10 times higher than in serum, following intravenous administration of an aqueous CDF-β-cyclodextrin preparation.


CONCLUSIONS
Novel curcumin analog CDF preferentially accumulates in the pancreas, leading to its potent anticancer activity against pancreatic cancer cells. Synthesis of such CDF-β-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.
ISTRA, Department of Chemistry, MCE Society's Abeda Inamdar Senior College of Arts, Science and Commerce, Pune 411001, India.
Prasad R
PR
Dandawate
Alok
A
Vyas
Aamir
A
Ahmad
Sanjeev
S
Banerjee
Jyoti
J
Deshpande
K Venkateswara
KV
Swamy
Abeda
A
Jamadar
Anne Catherine
AC
Dumhe-Klaire
Subhash
S
Padhye
Fazlul H
FH
Sarkar
D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D030024:Curcuma / Q000737:chemistry; D003474:Curcumin / Q000008:administration & dosage* / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology; D004337:Drug Carriers / Q000737:chemistry*; D005260:Female; D054879:Halogenation; D006801:Humans; D051379:Mice; D008958:Models, Molecular; D010179:Pancreas / Q000187:drug effects / Q000378:metabolism; D010190:Pancreatic Neoplasms / Q000188:drug therapy* / Q000378:metabolism; D012995:Solubility; D047392:beta-Cyclodextrins / Q000737:chemistry*
D000970:Antineoplastic Agents; D004337:Drug Carriers; D047392:beta-Cyclodextrins; D003474:Curcumin