Biocompatibility Profile and In Vitro Cellular Uptake of Self-assembled Alginate Nanoparticles.

Pei Zhang,Yan Yang,Huan Wang,Chenguang Liu,Yaoyao Yu,Shirui Zhao

doi:10.3390/molecules24030555

Abstract

Polymeric nanoparticles could offer promising controlled drug delivery. The biocompatibility is of extreme importance for future applications in humans. Self-assembled polymeric nanoparticles based on phenylalanine ethyl ester (PAE)-modified alginate (Alg) had been successfully prepared and characterized in our lab. However, little is known about their interaction with cells and other biological systems. In this study, nanoparticles (NPs) based on PAE-Alg conjugates (PEA-NPs) with different degree of substitution (DS) were prepared and investigated. Our results showed that PEA-NPs had no effects on the proliferation of the human intestinal epithelial Caco-2 cells at concentrations up to 1000 μg/mL. Furthermore, the in vitro cellular uptake profile of PEA-NPs, concerning several parameters involved in the application of therapeutic or diagnostic NPs, such as NPs concentration, time and temperature, was described. Different NPs have been adopted for cellular uptake studies and the NPs internalized into Caco-2 cells were quantified. Cellular uptake efficiency could reach 60% within 4 h. PEA-NPs also showed greater cell permeability than oleoyl alginate ester nanoparticles (OAE-NPs) previously prepared in our lab. Our studies reveal that NPs based on PEA conjugate are promising nanosystems for cellular delivery.

Highlights

In the last two decades it has been found that amphiphilic block or graft copolymers can form self-assembled, nanosize aggregates [1]
We reported that Alg hydrophobically modified with oleic acid can load water insoluble vitamins into the hydrophobic cores of nanosized particles
The mean hydrodynamic diameters of the particles decreased from 425.3 ± 5.7 nm to 226.7 ± 4.0 nm with increased degree of substitution (DS) of PEA conjugate (PEA1 = 3.49, PEA2 = 4.18 and PEA3 = 4.67) [27]

Summary

Introduction

In the last two decades it has been found that amphiphilic block or graft copolymers can form self-assembled, nanosize aggregates [1]. Comprehensive research has been conducted on the feasibility for self-assembled nanoparticles (NPs) to be used for targeted drug delivery and other biomedical applications, such as suitable properties for potential use PDT [4], affecting immune responses [5,6], delivery of proteomics or genomics used in ligand-targeted therapeutics [7], delivery of anticancer and antifungal drugs approved for clinical use [8]. Because of their special physicochemical properties, such as size and surface area, self-assembled NPs have shown great advantages in targeted therapy and delivery [9].

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Discussion

Conclusion