title: Telmisartan complex augments solubility, dissolution and drug delivery in prostate cancer cells.
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.
authors.affiliation: Department of Pharmaceutics, Chandigarh College of Pharmacy, Mohali, Punjab, India.
authors.forename: Manveet
authors.initials: M
authors.lastname: Kaur
authors.forename: Richa Kaur
authors.initials: RK
authors.lastname: Bhatia
authors.forename: Raghuvir R S
authors.initials: RR
authors.lastname: Pissurlenkar
authors.forename: Evans C
authors.initials: EC
authors.lastname: Coutinho
authors.forename: Upendra Kumar
authors.initials: UK
authors.lastname: Jain
authors.forename: Om Prakash
authors.initials: OP
authors.lastname: Katare
authors.forename: Ramesh
authors.initials: R
authors.lastname: Chandra
authors.forename: Jitender
authors.initials: J
authors.lastname: Madan
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D001562:Benzimidazoles / Q000737:chemistry* / Q000494:pharmacology; D001565:Benzoates / Q000737:chemistry* / Q000494:pharmacology; D045744:Cell Line, Tumor; D003198:Computer Simulation; D004337:Drug Carriers / Q000737:chemistry*; D006801:Humans; D008297:Male; D008958:Models, Molecular; D008968:Molecular Conformation; D011471:Prostatic Neoplasms / Q000473:pathology*; D012995:Solubility; D000077333:Telmisartan; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D001562:Benzimidazoles; D001565:Benzoates; D004337:Drug Carriers; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000077333:Telmisartan
keywords: 2-HP-β-CD; Complex; Cytotoxicity; In silico docking; Solubility; Telmisartan