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In Vitro Anticancer Drug Delivery Using Amphiphilic Poly( N ‐vinylpyrrolidone)‐ b ‐Polyketal‐ b ‐Poly( N ‐vinylpyrrolidone) Block Copolymer as Micellar Nanocarrier
Author(s) -
Mitra Kheyanath,
Hira Sumit Kumar,
Singh Shikha,
Vishwakarma Niraj Kumar,
Vishwakarma Sambhav,
Gupta Uttam,
Manna Partha Pratim,
Ray Biswajit
Publication year - 2018
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201801399
Subject(s) - nanocarriers , copolymer , micelle , chemistry , amphiphile , polymer chemistry , drug delivery , drug carrier , nuclear chemistry , differential scanning calorimetry , biophysics , organic chemistry , aqueous solution , polymer , physics , thermodynamics , biology
We have first synthesized acid‐degradable alkyne‐terminated aliphatic polyketal and thereof synthesized novel pH‐responsive double hydrophilic amphiphilic block copolymer of poly(N‐vinyl pyrrolidone) (PNVP) and aliphatic polyketal (PK) (PNVP‐ b ‐PK‐ b ‐PNVP via click chemistry upon reaction with azide‐terminated PNVP. Formation of block copolymer is confirmed by proton nuclear magnetic resonance, gel permeation chromatography, thermogravimetry, differential scanning calorimetry, and fluorescence spectroscopy techniques. pH‐dependent degradation study of the block copolymer shows faster degradation at lower pH. Transmission electron microscopy (TEM) has revealed the formation of tiny (∼3.8 nm) micellar nanoparticles. Loading of the anticancer drugs doxorubicin (Dox) and imatinib in the micelle is confirmed from UV‐Visible, and TEM studies. Drug release study from drug‐loaded micelles has shown that imatinib is being released faster than Dox and both systems have shown higher load release at acidic pH of 6.4. Doxorubicin‐ and imatinib‐ loaded micelles demonstrate significant tumoricidal properties against parental and drug resistant human erythroleukemia K‐562 and Dalton's lymphoma cells with respect to enhanced cellular uptake, cytotoxicity and growth inhibition.