Fabrication, characterization and bioevaluation of silibinin loaded chitosan nanoparticles

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...

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Bibliographic Details
Published in:International journal of biological macromolecules 2014-08, Vol.69, p.267-273
Main Authors: Pooja, Deep, Babu Bikkina, Dileep J., Kulhari, Hitesh, Nikhila, Nalla, Chinde, Srinivas, Raghavendra, Y.M., Sreedhar, B., Tiwari, Ashok K.
Format: Article
Language:English
Subjects:
Administration, Oral
Antineoplastic Agents - administration & dosage
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Cell Line, Tumor
Characterization
Chemical Phenomena
Chitosan - chemistry
Chitosan nanoparticles
Cytotoxicity
Dissolution
Drug Carriers - chemistry
Humans
Male
Nanoparticles - chemistry
Particle Size
Prostatic Neoplasms - pathology
Silibinin
Silymarin - administration & dosage
Silymarin - chemistry
Silymarin - pharmacology
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Summary: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.
ISSN:0141-8130
1879-0003
DOI:10.1016/j.ijbiomac.2014.05.035