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AuthorPraphakar R.A.
AuthorJeyaraj M.
AuthorMehnath S.
AuthorHiguchi A.
AuthorPonnamma D.
AuthorSadasivuni K.K.
AuthorRajan M.
Available date2019-11-04T05:19:30Z
Publication Date2018
Publication NameJournal of Materials Chemistry B
AbstractThe physiological environment is a crucial factor in biomedical systems, which can be regulated with relative ease both in vitro and in vivo. Control of pH has emerged as a powerful strategy in cancer therapy because pH has a profound effect on the interaction of a polymeric-based drug delivery system with tumor cells. In this regard, the enhancement of pH response capability was demonstrated with a 5-flourouracil (5-FU)-loaded guar gum (GG)-grafted-lysine-?-cyclodextrin (L-?-CD) drug carrier. The size, charge, morphology, and encapsulation efficiency of the 5-FU-loaded polymeric carrier were characterized for the control and sustained release of the drug. In a specific cancer pH environment, 5-FU-loaded GG-g-L-?-CD could rapidly swallow, disassemble, and release 5-FU by accepting or losing electrons. In vitro observations indicate that GG-g-L-?-CD dramatically releases 5-FU in an acidic environment rather than in a basic environment. In vitro antitumor activity tests showed that 5-FU-loaded GG-g-L-?-CD had a higher cytotoxicity against KB cells, with an IC50 value of 1.38 ?g ml-1. The reactive oxygen species (ROS) generated by 5-FU in the KB cells showed efficient suppression of tumour cell growth. The Hoechst assay revealed the active nature of 5-FU in the cell nucleus of the KB cells. The potential mitochondrial damage by apoptosis in KB cells greatly increased cell death. Therefore, due to its active nature, the pH-sensitive 5-FU-loaded GG-g-L-?-CD carrier is a potential drug delivery system for safe and effective cancer therapy, and it can be useful for inhibiting tumour cell growth.
SponsorMR acknowledges the major financial support received from the University Grants Commission (UGC), Government of India, for financial support under the plan of ‘‘UGC-MRP’’ (F. No. 43-187/ 2014) (SR) and Department of Science and Technology, Science and Engineering Research Board (Ref: YSS/2015/001532; New Delhi, India), ‘‘EMEQ’’ (F. No. – SB/EMEQ-241-2014) and also acknowledges the PURSE program for the purchase of SEM and FT-IR and UPE programs for the purchase of TEM.
PublisherRoyal Society of Chemistry
TitleA pH-sensitive guar gum-: Grafted -lysine-?-cyclodextrin drug carrier for the controlled release of 5-flourouracil into cancer cells
Issue Number10
Volume Number6

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