IMR Press / FBL / Volume 26 / Issue 9 / DOI: 10.52586/4964
Open Access Original Research
PLA-based core-shell structure stereocomplexed nanoparticles with enhanced loading and release profile of paclitaxel
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1 State Key Laboratory of Pollution Control and Resources Reuse, National Engineering Research Center for Organic Pollution Control and Resource Reuse, School of the Environment, Nanjing University, 210023 Nanjing, Jiangsu, China
*Correspondence: jiangwei@nju.edu.cn (Wei Jiang)
Front. Biosci. (Landmark Ed) 2021, 26(9), 517–532; https://doi.org/10.52586/4964
Submitted: 8 July 2021 | Revised: 5 August 2021 | Accepted: 27 August 2021 | Published: 30 September 2021
(This article belongs to the Special Issue Biomacromolecules, Biomaterials, Biosensors, and Biomedical Devices)
Copyright: © 2021 The Author(s). Published by BRI.
This is an open access article under the CC BY 4.0 license (https://creativecommons.org/licenses/by/4.0/).
Abstract

Purpose: In the present study, to achieve high paclitaxel (PTX) loading in a conjugated drug delivery system with minimal long-term side effects, we formulated a novel degradable stereocomplexed micelle-like particle with a core-shell structure. Materials and methods: In this system, methoxy polyethylene glycol (MPEG) acted as the hydrophilic shell, and the stereocomplex of polylactic acid with PTX (SCPLA-PTX) acted as the hydrophobic core. The MPEG-SCPLA-PTX micelle-like particles were synthesized via the self-assembly of a MPEG-poly L-lactic acid (PLLA) copolymer with a PTX-poly D-lactic acid-PTX copolymer. The resultant copolymers and their intermediates were characterized using 1H nuclear magnetic resonance and GPC. Micelle-like particles with different molecular weight ratios of MPEG and PLLA were synthesized to demonstrate the functions of both components. Results: PTX loading into MPEG2000Da-PLLA6000Da particles reached as high as 20.11%. At 216 h, the cumulative release from MPEG5000Da-PLLA6000Da, MPEG2000Da-PLLA6000Da, and MPEG5000Da-PLLA22000Da particles were 51.5%, 37.7%, and 52.0%, respectively. Conclusions: According to the cell uptake experiments, inhibition of tumor cell growth was satisfactory, indicating that the stereocomplexed particles developed in the present study can be employed as a promising nanocarrier for PTX delivery.

Keywords
Paclitaxel
MPEG-PLLA
Stereocomplex
Nanoparticles
Controllable drug loading
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