PMID- 24907761 OWN - NLM STAT- MEDLINE DCOM- 20150127 LR - 20231213 IS - 1873-0191 (Electronic) IS - 0928-4931 (Linking) VI - 41 DP - 2014 Aug 1 TI - Enhanced cytotoxicity and apoptosis-induced anticancer effect of silibinin-loaded nanoparticles in oral carcinoma (KB) cells. PG - 274-82 LID - S0928-4931(14)00248-3 [pii] LID - 10.1016/j.msec.2014.04.056 [doi] AB - Silibinin (SIL) is a plant derived flavonoid isolated from the fruits and seeds of the milk thistle (Silybum marianum). Silibinin possesses a wide variety of biological applications including anticancer activities but poor aqueous solubility and poor bioavailability limit its potential and efficacy at the tumor sites. In the present study, silibinin was encapsulated in Eudragit(R) E (EE) nanoparticles in the presence of stabilizing agent polyvinyl alcohol (PVA) and its anticancer efficacy in oral carcinoma (KB) cells was studied. Silibinin loaded nanoparticles (SILNPs) were prepared by nanoprecipitation technique and characterized in terms of size distribution, morphology, surface charge, encapsulation efficiency and in vitro drug release. MTT assay revealed higher cytotoxic efficacy of SILNPs than free SIL in KB cells. Meanwhile, reactive oxygen species (ROS) determination revealed the significantly higher intracellular ROS levels in SILNPs treated cells compared to free SIL treated cells. Therefore, the differential cytotoxicity between SILNPs and SIL may be mediated by the discrepancy of intracellular ROS levels. Moreover, acridine orange (AO) and ethidium bromide (EB) dual staining and reduced mitochondrial membrane potential (MMP) confirmed the induction of apoptosis with nanoparticle treatment. Further, the extent of DNA damage (evaluated by comet assay) was significantly increased in SILNPs than free SIL in KB cells. Taken together, the present study suggests that silibinin-loaded nanoparticles can be used as an effective drug delivery system to produce a better chemopreventive response for the treatment of cancer. CI - Copyright (c) 2014 Elsevier B.V. All rights reserved. FAU - Gohulkumar, M AU - Gohulkumar M AD - Department of Physics, Annamalai University, Annamalainagar 608 002, Tamilnadu, India. FAU - Gurushankar, K AU - Gurushankar K AD - Department of Physics, Annamalai University, Annamalainagar 608 002, Tamilnadu, India. FAU - Rajendra Prasad, N AU - Rajendra Prasad N AD - Department of Biochemistry and Biotechnology, Annamalai University, Annamalainagar, 608 002, Tamilnadu, India. FAU - Krishnakumar, N AU - Krishnakumar N AD - Department of Physics, Annamalai University, Annamalainagar 608 002, Tamilnadu, India. Electronic address: nskumarphyamu@gmail.com. LA - eng PT - Journal Article DEP - 20140502 PL - Netherlands TA - Mater Sci Eng C Mater Biol Appl JT - Materials science & engineering. C, Materials for biological applications JID - 101484109 RN - 0 (Antineoplastic Agents) RN - 0 (Reactive Oxygen Species) RN - 0 (Silymarin) RN - 4RKY41TBTF (Silybin) RN - 9002-89-5 (Polyvinyl Alcohol) SB - IM MH - Antineoplastic Agents/*chemistry/pharmacology MH - Apoptosis/drug effects MH - Cell Line, Tumor MH - DNA Damage/drug effects MH - Humans MH - Membrane Potential, Mitochondrial/drug effects MH - Silybum marianum/chemistry/metabolism MH - Nanoparticles/*chemistry MH - Polyvinyl Alcohol/chemistry MH - Reactive Oxygen Species/metabolism MH - Silybin MH - Silymarin/*chemistry/*pharmacology OTO - NOTNLM OT - Apoptosis OT - Cytotoxicity OT - KB cells OT - Nanoparticles OT - Silibinin EDAT- 2014/06/09 06:00 MHDA- 2015/01/28 06:00 CRDT- 2014/06/09 06:00 PHST- 2013/12/02 00:00 [received] PHST- 2014/03/09 00:00 [revised] PHST- 2014/04/23 00:00 [accepted] PHST- 2014/06/09 06:00 [entrez] PHST- 2014/06/09 06:00 [pubmed] PHST- 2015/01/28 06:00 [medline] AID - S0928-4931(14)00248-3 [pii] AID - 10.1016/j.msec.2014.04.056 [doi] PST - ppublish SO - Mater Sci Eng C Mater Biol Appl. 2014 Aug 1;41:274-82. doi: 10.1016/j.msec.2014.04.056. Epub 2014 May 2.