Size-dependent cellular uptake and sustained drug release of PLGA particles (Open Access)--颗粒学报PARTICUOLOGY

Sun, R., Liu, X., Zhang, Y., Li, Q., Zhu, Y., & Fan, C. (2023). Size-dependent cellular uptake and sustained drug release of PLGA particles. Particuology, 73, 1-7. https://doi.org/10.1016/j.partic.2022.03.003

Size-dependent cellular uptake and sustained drug release of PLGA particles (Open Access)

Rui Sun^{a c 1}, Xia Liu^{a c 1}, Yu Zhang^{a b *}, Qian Li^d, Ying Zhu^{a b}, Chunhai Fan^d *

a Division of Physical Biology, CAS Key Laboratory of Interfacial Physics and Technology, Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Shanghai 201800, China
b The Interdisciplinary Research Center, Shanghai Synchrotron Radiation Facility, Zhangjiang Laboratory, Shanghai Advanced Research Institute, Chinese Academy of Sciences, Shanghai 201210, China
c University of Chinese Academy of Sciences, Beijing 100049, China
d School of Chemistry and Chemical Engineering, Frontiers Science Center for Transformative Molecules and National Center for Translational Medicine, Shanghai Jiao Tong University, Shanghai 200240, China

10.1016/j.partic.2022.03.003

Volume 73, February 2023, Pages 1-7

Received 24 January 2022, Revised 14 March 2022, Accepted 17 March 2022, Available online 17 April 2022, Version of Record 10 May 2022.

E-mail: zhangyu@sari.ac.cn; fanchunhai@sjtu.edu.cn

Highlights

• Drug loading of micrometer DEX-loaded PLGA particles (DPs) was higher than that of submicrometer DPs.

• At submicrometer scale, 500 nm DPs showed a better sustained release profile.

• 500 nm DPs had sustained anti-inflammatory efficacy in lipopolysaccharide-induced RAW 264.7 cells model.

Abstract

Poly (lactic-co-glycolic) acid (PLGA) particles have become a commonly used drug delivery strategy in the pharmaceutical industry. In this work, we aim to investigate the size-dependent cellular internalization of PLGA particles and its effects on sustained drug release. We prepared three different-sized particles using PLGA (200, 500 and 2000 nm) ranging from submicrometer to micrometer. Dexamethasone (DEX) with excellent anti-inflammatory properties was used as a model drug to prepare DEX-loaded PLGA particles (DPs). We comprehensively investigated the encapsulation efficiency, cellular uptake and in vitro drug release profile. Pharmacodynamic assessment revealed that, in the lipopolysaccharide (LPS)-induced RAW 264.7 cells model, 500 nm DPs showed sustained anti-inflammatory efficacy. This work provides important information for designing PLGA-based drug delivery systems for biomedical applications.

Graphical abstract

Keywords

DEX-loaded PLGA particles (DPs); Sustained release; Anti-inflammatory efficacy

文章导读