Literature DB >> 24299818

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

Manveet Kaur1, Richa Kaur Bhatia, Raghuvir R S Pissurlenkar, Evans C Coutinho, Upendra Kumar Jain, Om Prakash Katare, Ramesh Chandra, Jitender Madan.   

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.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

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

Mesh:

Substances:

Year:  2013        PMID: 24299818     DOI: 10.1016/j.carbpol.2013.09.077

Source DB:  PubMed          Journal:  Carbohydr Polym        ISSN: 0144-8617            Impact factor:   9.381


  2 in total

1.  Evolution of Choice of Solubility and Dissolution Media After Two Decades of Biopharmaceutical Classification System.

Authors:  Nadia Bou-Chacra; Katherine Jasmine Curo Melo; Ivan Andrés Cordova Morales; Erika S Stippler; Filippos Kesisoglou; Mehran Yazdanian; Raimar Löbenberg
Journal:  AAPS J       Date:  2017-05-17       Impact factor: 4.009

2.  Dissolution rate improvement of telmisartan through modified MCC pellets using 32 full factorial design.

Authors:  Hetal Patel; Hiral Patel; Mukesh Gohel; Sanjay Tiwari
Journal:  Saudi Pharm J       Date:  2015-03-23       Impact factor: 4.330

  2 in total

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