Temperature Responsive Nanoparticles Based on PEGylated Polyaspartamide Derivatives for Drug Delivery.

Guangyan Zhang,Xulin Jiang

doi:10.3390/polym11020316

Guangyan Zhang, Xulin Jiang

Open Access

https://doi.org/10.3390/polym11020316

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Journal: Polymers	Publication Date: Feb 13, 2019
Citations: 18	License type: CC BY 4.0

Affiliation: Hubei University of Technology, Wuhan University

Abstract

The temperature responsive PEGylated polyaspartamide derivative, denoted as mPEG-PAAHP, was synthesized by the click reaction. FTIR and 1H NMR were adopted to characterize and confirm the chemical structures of the obtained mPEG-PAAHPs. The temperature responsive behavior investigated by transmittance and dynamic light scattering showed that some of the obtained mPEG-PAAHPs exhibited obvious temperature responsiveness and could be used to prepare nanoparticles by quickly heating. Drug paclitaxel can be encapsulated into mPEG-PAAHP based nanoparticles with a high encapsulation efficiency up to 99% (corresponding to a drug loading content of around 9.9%). Dynamic light scattering results showed that the PTX-loaded nanoparticles had a mean size around 80 nm (PDI<0.2) and good stability in PBS with 150 mM ionic strength. In vitro cytotoxicity results showed that mPEG-PAAHP did not show any toxicity to HeLa cells, but the PTX-loaded nanoparticles based on mPEG-PAAHP exhibited obvious anti-cancer activity. Thus, the temperature responsive PEGylated polyaspartamide derivative mPEG-PAAHP may be a promising drug delivery system.

Highlights

Polymeric drug carriers with various stimuli responsiveness have attracted great attention in the past two decades [1,2]
P(Asp-Az)-HPA was availed as a template to synthesize temperature responsive polymers by introducing hydrophobic moieties via the click reaction with a high reaction efficiency [29,34]
PEGylated temperature responsive polyaspartamide derivatives containing pendant hydrophobic aromatic moieties were synthesized as illustrated in Scheme 1 to investigate their properties for drug delivery

Summary

Introduction

Polymeric drug carriers with various stimuli responsiveness have attracted great attention in the past two decades [1,2]. These stimuli-responsive drug carriers usually can self-adjust their aggregation states or change their chemical structures when the external environment is changed [3,4], so the external environmental conditions, such as temperature [5,6] and pH [7,8,9], can be chosen as a key to implement drug loading or controlled drug release conveniently. Temperature responsive polymers exhibit great potential and prospects in drug delivery [11,12].

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