Abstract
We developed novel poly(l-lysine) [poly(Lys)] derivative nanogels with smart drug release properties. Poly(Lys) derivative was prepared after the chemical reaction of poly(Lys) and 3-diethylaminopropyl isothiocyanate (DEAP), and was coupled with poly(ethylene glycol) (PEG). The obtained poly(Lys-DEAP)-b-PEG was crosslinked by genipin (crosslinking agent) in an oil/water emulsion condition, producing poly(Lys) derivative nanogels. These nanogels (~95 nm in diameter, pH 7.4) showed volume expansion (~200 nm in diameter) in the endosomal pH (~pH 6.0) due to extensive proton absorption of DEAP moieties in the crosslinked nanogel core. These nanogels reversibly swelled at pH 6.0 and shrank at pH 7.4, correspond to maximized drug release at pH 6.0 and minimized drug release at pH 7.4. We conclude that this nanogel system will have great potential for tumor therapy.
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This articel does not contain any studies with human and animal subjects performed by any of the authors. These authors (M.J. Lee, N.M. Oh, K.T. Oh, Y.S. Youn, E.S. Lee) declare that they have no conflict of interest. This work was financially supported by the GRRC program of Gyeonggi province [GRRC 2013-B01, Development of industrial nano-/micro-sized biomaterials for high performance drug release control], and Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Education (NRF-2013R1A1A2004375).
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Lee, M.J., Oh, N.M., Oh, K.T. et al. Functional poly(l-lysine) derivative nanogels with acidic pH-pulsed antitumor drug release properties. Journal of Pharmaceutical Investigation 44, 351–356 (2014). https://doi.org/10.1007/s40005-014-0130-7
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DOI: https://doi.org/10.1007/s40005-014-0130-7