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

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• 作者：Manveet Kaur ; Richa Kaur Bhatia ; Raghuvir R.S. Pissurlenkar ; Evans C. Coutinho ; Upendra Kumar Jain ; Om Prakash Katare ; Ramesh Ch ; ra ; Jitender Madan
• 关键词：Telmisartan ; 2-HP-尾-CD ; Complex ; In silico docking ; Solubility ; Cytotoxicity
• 刊名：Carbohydrate Polymers
• 出版年：30 January, 2014
• 年：2014
• 卷：101
• 期：Complete
• 页码：614-622
• 全文大小：1603 K

文摘

Telmisartan (TEL) requires superior bioavailability in cancer cell compartments. To meet these challenges, we have synthesized a 2-HP-尾-CD-TEL complex with stability constant (K_c) of 2.39 脳 10^鈭? mM. The absence in the FTIR spectrum of 2-HP-尾-CD-TEL complex of the characteristic peaks of TEL at 1699 cm^鈭? (carboxylic acid) and 741 and 756 cm^鈭? (1,2-disubstituted benzene ring vibrations), is indicative of the encapsulation of TEL in the 2-HP-尾-CD cavity. DSC and PXRD also confirmed the synthesis and amorphous structure of complex. The interaction of TEL with 2-HP-尾-CD was examined by NMR and 2D-ROESY which affirms the encapsulation of TEL in the 2-HP-尾-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.