title: New Insight into a Cancer Theranostic Probe: Efficient Cell-Specific Delivery of SN-38 Guided by Biotinylated Poly(vinyl alcohol).
abstract: An optically modulated "turn-on" theranostic prodrug TP1 has been explored and formulated with biotinylated poly(vinyl alcohol) (biotinPVA) to obtain desired pharmacokinetics. TP1, consisting of the antineoplastic camptothecin analogue SN-38, and the fluorescent dye rhodol green have been covalently conjugated through a disulfide bond. Glutathione triggering the release of drug and fluorophore has been well established by UV-vis measurements through mass spectral analysis in physiological conditions. The biocompatible biotinPVA formulated prodrug (PTP1) showed remarkably higher stability against blood serum and cell-specific activation in contrast to that of TP1. Significantly, PTP1 permits monitoring of the delivery and release of well-known topoisomerase I inhibitor SN-38 by modulating fluorescence signal at λem550 nm within intracellular milieus. Moreover, theranostic probe PTP1 exhibited dose-dependent antiproliferative activity against receptor-positive HeLa cells, whereas it did not show such an effect against receptor-negative NIH3T3 cells. Finally, the cell-specific antiproliferative activity of PTP1 via the apoptotic pathway is an efficient approach in cancer theranostics. Thus, futuristic PTP1 could be a promising agent in which diagnostic and prognostic data will be monitored synergistically.
authors.affiliation: Amrita Centre for Industrial Research and Innovation, Amrita School of Engineering, Amrita University , Coimbatore 64112, India.
authors.forename: Debabrata
authors.initials: D
authors.lastname: Dutta
authors.affiliation: Chemical Sciences & Technology Division, CSIR-National Institute for Interdisciplinary Science and Technology (CSIR-NIIST) , Industrial Estate, Pappanamcode, Thiruvananthapuram, Kerala 695019, India.
authors.forename: Susan M
authors.initials: SM
authors.lastname: Alex
authors.affiliation: Amrita Centre for Industrial Research and Innovation, Amrita School of Engineering, Amrita University , Coimbatore 64112, India.
authors.forename: Kondapa Naidu
authors.initials: KN
authors.lastname: Bobba
authors.affiliation: Chemical Sciences & Technology Division, CSIR-National Institute for Interdisciplinary Science and Technology (CSIR-NIIST) , Industrial Estate, Pappanamcode, Thiruvananthapuram, Kerala 695019, India.|Academy of Scientific and Innovative Research, AcSIR, CSIR-NIIST , Thiruvananthapuram, Kerala 695019, India.
authors.forename: Kaustabh Kumar
authors.initials: KK
authors.lastname: Maiti
authors.affiliation: Amrita Centre for Industrial Research and Innovation, Amrita School of Engineering, Amrita University , Coimbatore 64112, India.|Department of Chemical Engineering and Materials Science, Amrita School of Engineering, Amrita University , Coimbatore 641112, India.
authors.forename: Sankarprasad
authors.initials: S
authors.lastname: Bhuniya
mesh_terms: D000818:Animals; D002166:Camptothecin / Q000031:analogs & derivatives; D002460:Cell Line; D006801:Humans; D000077146:Irinotecan; D051379:Mice; D000068936:Theranostic Nanomedicine
chemical_list: D000077146:Irinotecan; D002166:Camptothecin
keywords: SN-38; antiproliferative; biocompatible; blood serum; poly(vinyl alcohol); theranostic