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Preparation of p H ‐ R esponsive Polymer Core– S hell Nanospheres for Delivery of Hydrophobic Antineoplastic Drug Ellipticine
Author(s) -
Wang Hui,
Yang Lijuan,
Rempel Garry L.
Publication year - 2014
Publication title -
macromolecular bioscience
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.924
H-Index - 105
eISSN - 1616-5195
pISSN - 1616-5187
DOI - 10.1002/mabi.201300333
Subject(s) - chemistry
Antineoplastic drug ellipticine and its derivatives are used in human cancer therapy. However, their clinical applications have been limited by its great hydrophobicity and severe side effects. An efficient delivery system is therefore very desirable. In this research, an ellipticine‐loaded core–shell structured nanosphere namely poly(DEAEMA)‐poly(PEGMA) is designed as a drug carrier and prepared via a two‐step semibatch emulsion polymerization method where DEAEMA and PEGMA represent 2‐(diethylamino)ethyl methacrylate and poly(ethylene glycol) methacrylate, respectively. The in‐vitro release profiles of ellipticine towards the different pH liposome vesicles are recorded as a function of time at 37 °C. It is found that release of ellipticine from the core‐shell polymer matrix is a pH‐responsive and controlled release process. The three pH's of 3, 4, and 5 trigger a significant ellipticine release of 88% after 98 h, 83% after 98 h, and 79% after 122 h, respectively. The release mechanism of ellipticine from the core‐shell polymer matrix under acidic conditions is explored. The synthesis and encapsulation process developed herein provides a new perspective for the development of appropriate delivery systems to deliver the ellipticine and its analogues, as well as other types of hydrophobic drugs to a given target cell or tumor tissue.