Influence of Structural Features on the Cellular Uptake Behavior of Non-Targeted Polyester-Based Nanocarriers

Castro, Carlos E. de; Bonvent, Jean-Jacques; Silva, Maria C. C. da; Castro, Fabiane Lucy Ferreira; Giacomelli, Fernando C.

doi:10.1002/mabi.201600138

Cited by 9 publications

(15 citation statements)

References 32 publications

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“…However, we also found out that there should be a compromise between protein adsorption and cellular uptake since the latter correlates inversely with the shell thickness. 15 These experimental evidences agree well with conclusions based on computer simulations. 16 We have also evidenced that cellular uptake depends on the chemical nature of the core where nanoparticles comprising a highly hydrophobic inner compartment are more efficiently internalized.…”

Section: ■ Introductionsupporting

confidence: 85%

Nanoparticle–Cell Interactions: Surface Chemistry Effects on the Cellular Uptake of Biocompatible Block Copolymer Assemblies

et al. 2018

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The development of nanovehicles for intracellular drug delivery is strongly bound to the understating and control of nanoparticles cellular uptake process, which in turn is governed by surface chemistry. In this study, we explored the synthesis, characterization, and cellular uptake of block copolymer assemblies consisting of a pH-responsive poly[2-(diisopropylamino)ethyl methacrylate] (PDPA) core stabilized by three different biocompatible hydrophilic shells (a zwitterionic type poly(2-methacryloyloxyethyl phosphorylcholine) (PMPC) layer, a highly hydrated poly(ethylene oxide) (PEO) layer with stealth effect, and an also proven nontoxic and nonimmunogenic poly(N-(2-hydroxypropyl)methacrylamide) (PHPMA) layer). All particles had a spherical core-shell structure. The largest particles with the thickest hydrophilic stabilizing shell obtained from PMPC-b-PDPA were internalized to a higher level than those smaller in size and stabilized by PEO or PHPMA and produced from PEO-b-PDPA or PHPMA-b-PDPA, respectively. Such a behavior was confirmed among different cell lines, with assemblies being internalized to a higher degree in cancer (HeLa) as compared to healthy (Telo-RF) cells. This fact was mainly attributed to the stronger binding of PMPC to cell membranes. Therefore, cellular uptake of nanoparticles at the sub-100 nm size range may be chiefly governed by the chemical nature of the stabilizing layer rather than particles size and/or shell thickness.

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Section: ■ Introductionsupporting

confidence: 85%

Nanoparticle–Cell Interactions: Surface Chemistry Effects on the Cellular Uptake of Biocompatible Block Copolymer Assemblies

et al. 2018

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“…This indeed seems to be a more general phenomenon. We have particularly measured negative ζ-potentials for many different nonionic particles. − …”

Section: Resultsmentioning

confidence: 99%

“…We have particularly measured negative -potentials for many different non-ionic particles. [35][36][37]…”

Section: Manufacturing and Characterization Of The Block Copolymer Assembliesmentioning

confidence: 99%

Polyglycidol-Stabilized Nanoparticles as a Promising Alternative to Nanoparticle PEGylation: Polymer Synthesis and Protein Fouling Considerations

Oliveira

Albuquerque

et al. 2020

Langmuir

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We herein demonstrate the outstanding protein-repelling characteristic of starlike micelles and polymersomes manufactured from amphiphilic block copolymers made by poly(butylene oxide) (PBO) hydrophobic segments and polyglycidol (PGL) hydrophilic outer shells. Although positively charged proteins (herein modeled by lysozyme) may adsorb onto the surface of micelles and polymersomes where the assemblies are stabilized by short PGL chains (degree of polymerization smaller then 15), the protein adsorption vanishes when the degree of polymerization of the hydrophilic segment (PGL) is higher than ~ 20, regardless the morphology. This has been probed by using three different model proteins which are remarkable different concerning molecular weight, size and zeta potential (bovine serum albumin -BSA, lysozyme and immunoglobulin G -IgG). Indeed, the adsorption of the most abundant plasma protein (herein modeled as BSA) is circumvented even by using very short PGL shells due to the highly negative zeta potential of the produced assemblies which presumably promotes protein-nanoparticle electrostatic repulsion. The highly negative zeta potential, on the other hand, enables lysozyme adsorption and the phenomenon is governed by electrostatic forces as evidenced by isothermal titration calorimetry.Nevertheless, the protein coating can be circumvented by slightly increasing the degree of polymerization of the hydrophilic segment. Notably, the PGL length required to circumvent protein fouling is significantly smaller than the one required for PEO. This feature and the safety concerns regarding the synthetic procedures on the preparation of poly(ethylene oxide)-based amphiphilic copolymers might make polyglycidol a promising alternative towards the production of non-fouling particles.

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“…The organic solution was transferred to a syringe and afterward added dropwise into 5 mL of water solution and then removed by evaporation. For the PEO 113 - b -PCL 118 nanoparticles, acetone was used to completely dissolve the polymeric chains [ 6 , 22 ]. For the CIP-loaded micelles, CIP was weighed and solubilized in ethanol according to the desired feeding and was mixed with the polymeric organic solution before the addition to the aqueous phase.…”

Section: Methodsmentioning

confidence: 99%

Ciprofibrate-Loaded Nanoparticles Prepared by Nanoprecipitation: Synthesis, Characterization, and Drug Release

et al. 2021

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Ciprofibrate (CIP) is a highly lipophilic and poorly water-soluble drug, typically used for dyslipidemia treatment. Although it is already commercialized in capsules, no previous studies report its solid-state structure; thus, information about the correlation with its physicochemical properties lacking. In parallel, recent studies have led to the improvement of drug administration, including encapsulation in polymeric nanoparticles (NPs). Here, we present CIP’s crystal structure determined by PDRX data. We also propose an encapsulation method for CIP in micelles produced from Pluronic P123/F127 and PEO-b-PCL, aiming to improve its solubility, hydrophilicity, and delivery. We determined the NPs’ physicochemical properties by DLS, SLS, ELS, and SAXS and the loaded drug amount by UV-Vis spectroscopy. Micelles showed sizes around 10–20 nm for Pluronic and 35–45 nm for the PEO-b-PCL NPs with slightly negative surface charge and successful CIP loading, especially for the latter; a substantial reduction in ζ-potential may be evidenced. For Pluronic nanoparticles, we scanned different conditions for the CIP loading, and its encapsulation efficiency was reduced while the drug content increased in the nanoprecipitation protocol. We also performed in vitro release experiments; results demonstrate that probe release is driven by Fickian diffusion for the Pluronic NPs and a zero-order model for PEO-b-PCL NPs.

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Influence of Structural Features on the Cellular Uptake Behavior of Non-Targeted Polyester-Based Nanocarriers

Cited by 9 publications

References 32 publications

Nanoparticle–Cell Interactions: Surface Chemistry Effects on the Cellular Uptake of Biocompatible Block Copolymer Assemblies

Nanoparticle–Cell Interactions: Surface Chemistry Effects on the Cellular Uptake of Biocompatible Block Copolymer Assemblies

Polyglycidol-Stabilized Nanoparticles as a Promising Alternative to Nanoparticle PEGylation: Polymer Synthesis and Protein Fouling Considerations

Ciprofibrate-Loaded Nanoparticles Prepared by Nanoprecipitation: Synthesis, Characterization, and Drug Release

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