Construction of paclitaxel-loaded poly (2-hydroxyethyl methacrylate)-g-poly (lactide)- 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine copolymer nanoparticle delivery system and evaluation of its anticancer activity
Xiaowei Ma*, Huan Wang*, Shubin Jin, Yan Wu, Xing-Jie Liang
Laboratory of Nanomedicine and Nanosafety, Division of Nanomedicine and Nanobiology, National Center for Nanoscience and Technology, People’s Republic of China; and CAS Key Laboratory for Biomedical Effects of Nanomaterials and Nanosafety, Chinese Academy of Sciences, Beijing, People’s Republic of China
*These authors contributed equally to this work
Background: There is an urgent need to develop drug-loaded biocompatible nanoscale packages with improved therapeutic efficacy for effective clinical treatment. To address this need, a novel poly (2-hydroxyethyl methacrylate)-poly (lactide)-1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine [PHEMA-g-(PLA-DPPE)] copolymer was designed and synthesized to enable these nanoparticles to be pH responsive under pathological conditions.
Methods: The structural properties and thermal stability of the copolymer was measured and confirmed by Fourier transform infrare d spectroscopy, nuclear magnetic resonance, and thermogravimetric analysis. In order to evaluate its feasibility as a drug carrier, paclitaxel-loaded PHEMA-g-(PLA-DPPE) nanoparticles were prepared using the emulsion-solvent evaporation method.
Results: The PHEMA-g-(PLA-DPPE) nanoparticles could be efficiently loaded with paclitaxel and controlled to release the drug gradually and effectively. In vitro release experiments demonstrated that drug release was faster at pH 5.0 than at pH 7.4. The anticancer activity of the PHEMA-g-(PLA-DPPE) nanoparticles was measured in breast cancer MCF-7 cells in vivo and in vitro. In comparison with the free drug, the paclitaxel-loaded PHEMA-g-(PLA-DPPE) nanoparticles could induce more significant tumor regression.
Conclusion: This study indicates that PHEMA-g-(PLA-DPPE) nanoparticles are promising carriers for hydrophobic drugs. This system can passively target cancer tissue and release drugs in a controllable manner, as determined by the pH value of the area in which the drug accumulates.
Keywords: poly (2-hydroxyethyl methacrylate), controlled release, biocompatibility, antitumor activity, 1,2-dipalmitoyl-sn-glycero-3-phosphoethanolamine, nanoparticles
This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution - Non Commercial (unported, v3.0) License. The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. Permissions beyond the scope of the License are administered by Dove Medical Press Limited. Information on how to request permission may be found at: http://www.dovepress.com/permissions.php
Readers of this article also read:
Soosay Raj TA, Smith AM, Moore AS
Published Date: 6 November 2013
Safety of besifloxacin ophthalmic suspension 0.6% in refractive surgery: a retrospective chart review of post-LASIK patients
Nielsen SA, McDonald MB, Majmudar PA
Published Date: 15 April 2013
Bimatoprost ophthalmic solution 0.03% lowered intraocular pressure of normal-tension glaucoma with minimal adverse events. [Corrigendum]
Tsumura T, Yoshikawa K, Suzumura H, Kimura T, Sasaki S, Kimura I, Takeda R
Published Date: 16 January 2013
Kawaji H, Ishii M, Tamaki Y, Sasaki K, Takagi M
Published Date: 8 November 2012
Efficacy of the anti-VZV (anti-HSV3) vaccine in HSV1 and HSV2 recurrent herpes simplex disease: a prospective study
Le Goaster J, Gonzalo S, Bouree P, Tangy F, Haenni AL
Published Date: 30 July 2012
Published Date: 27 July 2012
Published Date: 21 June 2012
Abelson R, Lane KJ, Rodriguez J, Johnston P, Angjeli E, Ousler G, Montgomery D
Published Date: 24 April 2012
Chen ZQ, Liu Y, Zhao JH, Wang L, Feng NP
Published Date: 30 March 2012
Espandar L, Sikder S, Moshirfar M
Published Date: 6 February 2011