Telmisartan complex augments solubility, dissolution and drug delivery in prostate cancer cells
| Autor: | Manveet Kaur, Ramesh Chandra, Evans C. Coutinho, Richa Kaur Bhatia, Jitender Madan, Upendra Kumar Jain, Om Prakash Katare, Raghuvir R. S. Pissurlenkar |
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| Rok vydání: | 2014 |
| Předmět: |
Male
Models Molecular Polymers and Plastics Stereochemistry Molecular Conformation Beta-Cyclodextrins Benzoates In vivo Cell Line Tumor Materials Chemistry Humans Computer Simulation Telmisartan Solubility Cytotoxicity Drug Carriers Chemistry beta-Cyclodextrins Organic Chemistry Prostatic Neoplasms 2-Hydroxypropyl-beta-cyclodextrin Stability constants of complexes Drug delivery Cancer cell Benzimidazoles Drug carrier Nuclear chemistry |
| Zdroj: | Carbohydrate Polymers. 101:614-622 |
| ISSN: | 0144-8617 |
| DOI: | 10.1016/j.carbpol.2013.09.077 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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