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Carbohydr Polym. 2014 Jan 30;101:614-22. doi: 10.1016/j.carbpol.2013.09.077. Epub 2013 Sep 30.

Telmisartan complex augments solubility, dissolution and drug delivery in prostate cancer cells.

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1
Department of Pharmaceutics, Chandigarh College of Pharmacy, Mohali, Punjab, India.

Abstract

Telmisartan (TEL) requires superior bioavailability in cancer cell compartments. To meet these challenges, we have synthesized a 2-HP-β-CD-TEL complex with stability constant (Kc) of 2.39 × 10(-3)mM. The absence in the FTIR spectrum of 2-HP-β-CD-TEL complex of the characteristic peaks of TEL at 1,699 cm(-1) (carboxylic acid) and 741 and 756 cm(-1) (1,2-disubstituted benzene ring vibrations), is indicative of the encapsulation of TEL in the 2-HP-β-CD cavity. DSC and PXRD also confirmed the synthesis and amorphous structure of complex. The interaction of TEL with 2-HP-β-CD was examined by NMR and 2D-ROESY which affirms the encapsulation of TEL in the 2-HP-β-CD cavity in at least two orientations with equal binding energies. The complex also exhibited its superiority in both in vitro release and cytotoxicity experiments on prostate cancer, PC-3 cells as compared to free drug. These data warrant an in depth in vivo to scale-up the technology for the management of prostate cancer.

KEYWORDS:

2-HP-β-CD; Complex; Cytotoxicity; In silico docking; Solubility; Telmisartan

PMID:
24299818
DOI:
10.1016/j.carbpol.2013.09.077
[Indexed for MEDLINE]
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