title: Fabrication, characterization and bioevaluation of silibinin loaded chitosan nanoparticles.
abstract: Silibinin is reported to possess multiple biological activities. However, its hydrophobic nature limits its bioavailability compromising in vivo biological activities. Nanoparticles-based delivery of such molecules has emerged as new technique to resolve these issues. Bio-degradable, compatible and adhesive nature of chitosan has recently attracted its suitability as a carrier for biologically active molecules. This study presents fabrication and characterization of chitosan-tripolyphosphate based encapsulation of silibinin. Various preparations of silibinin encapsulated chitosan-tripolyphosphate nanoparticles were studied for particle size, morphology, zeta-potential, and encapsulation efficiencies. Preparations were also evaluated for cytotoxic activities in vitro. The optimized silibinin loaded chitosan nanoparticles were of 263.7±4.1nm in particle size with zeta potential 37.4±1.57mV. Nanoparticles showed high silibinin encapsulation efficiencies (82.94±1.82%). No chemical interactions between silibinin and chitosan were observed in FTIR analysis. Powder X-ray diffraction analysis revealed transformed physical state of silibinin after encapsulation. Surface morphology and thermal behaviour were determined using TEM and DSC analysis. Encapsulated silibinin displayed increased dissolution and better cytotoxicity against human prostate cancer cells (DU145) than silibinin alone.
authors.affiliation: Medicinal Chemistry & Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, India.
authors.forename: Deep
authors.initials: D
authors.lastname: Pooja
authors.affiliation: Medicinal Chemistry & Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, India.
authors.forename: Dileep J
authors.initials: DJ
authors.lastname: Babu Bikkina
authors.affiliation: Medicinal Chemistry & Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, India; IICT-RMIT Research Centre, CSIR-Indian Institute of Chemical Technology, Hyderabad, India. Electronic address: hiteshkulhari@gmail.com.
authors.forename: Hitesh
authors.initials: H
authors.lastname: Kulhari
authors.affiliation: Medicinal Chemistry & Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, India.
authors.forename: Nalla
authors.initials: N
authors.lastname: Nikhila
authors.affiliation: Toxicology Unit, Biology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, India.
authors.forename: Srinivas
authors.initials: S
authors.lastname: Chinde
authors.affiliation: Crop Protection Chemical Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, India.
authors.forename: Y M
authors.initials: YM
authors.lastname: Raghavendra
authors.affiliation: Inorganic and Physical Chemistry Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, India.
authors.forename: B
authors.initials: B
authors.lastname: Sreedhar
authors.affiliation: Medicinal Chemistry & Pharmacology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, India. Electronic address: tiwari@iict.res.in.
authors.forename: Ashok K
authors.initials: AK
authors.lastname: Tiwari
mesh_terms: D000284:Administration, Oral; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D055598:Chemical Phenomena; D048271:Chitosan / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry*; D006801:Humans; D008297:Male; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D011471:Prostatic Neoplasms / Q000473:pathology; D000077385:Silybin; D012838:Silymarin / Q000008:administration & dosage / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D012838:Silymarin; D000077385:Silybin; D048271:Chitosan
keywords: Characterization; Chitosan nanoparticles; Cytotoxicity; Dissolution; Silibinin