Stable Polymer Nanoparticles with Exceptionally High Drug Loading by Sequential Nanoprecipitation

Liu, Yun; Yang, Guangze; Baby, Thejus; Tengjisi,; Chen, Dong; Weitz, David A.; Zhao, Chun‐Xia

doi:10.1002/ange.201913539

Cited by 55 publications

(42 citation statements)

References 38 publications

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“…The decrease of interfacial tension between the two phases, caused by rapid diffusion of solvent into non-solvent phase, results in the increase of surface area and leads to the formation of nanoparticles. As Liu et al reported in 2020 [35], simple and robust sequential nanoprecipitation is a suitable method for enhancing drug loading and produces a stable drug-core polymer shell PNPs with high amount of loaded drug (up to 58.5%).…”

Section: Preparation Structure and Properties Of Polymer Nanoparticlesmentioning

confidence: 99%

Polymer Nanoparticles and Nanomotors Modified by DNA/RNA Aptamers and Antibodies in Targeted Therapy of Cancer

2021

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Polymer nanoparticles and nano/micromotors are novel nanostructures that are of increased interest especially in the diagnosis and therapy of cancer. These structures are modified by antibodies or nucleic acid aptamers and can recognize the cancer markers at the membrane of the cancer cells or in the intracellular side. They can serve as a cargo for targeted transport of drugs or nucleic acids in chemo- immuno- or gene therapy. The various mechanisms, such as enzyme, ultrasound, magnetic, electrical, or light, served as a driving force for nano/micromotors, allowing their transport into the cells. This review is focused on the recent achievements in the development of polymer nanoparticles and nano/micromotors modified by antibodies and nucleic acid aptamers. The methods of preparation of polymer nanoparticles, their structure and properties are provided together with those for synthesis and the application of nano/micromotors. The various mechanisms of the driving of nano/micromotors such as chemical, light, ultrasound, electric and magnetic fields are explained. The targeting drug delivery is based on the modification of nanostructures by receptors such as nucleic acid aptamers and antibodies. Special focus is therefore on the method of selection aptamers for recognition cancer markers as well as on the comparison of the properties of nucleic acid aptamers and antibodies. The methods of immobilization of aptamers at the nanoparticles and nano/micromotors are provided. Examples of applications of polymer nanoparticles and nano/micromotors in targeted delivery and in controlled drug release are presented. The future perspectives of biomimetic nanostructures in personalized nanomedicine are also discussed.

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Section: Preparation Structure and Properties Of Polymer Nanoparticlesmentioning

confidence: 99%

Polymer Nanoparticles and Nanomotors Modified by DNA/RNA Aptamers and Antibodies in Targeted Therapy of Cancer

2021

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“…The results of the ANOVA test (Table 4) showed that the P-value was lower than 0.05 for all responses and P for the lack of fit was greater than 0.05 for all responses, confirming that the proposed model is adequate, reliable, and has a good predictive power. (1) Regression coefficient; (2) predictive power of the model; (3) degrees of freedom; (4) sum of squares; (5) mean of square (variance); (6) Fisher's ratio; (7) probability; (8) particle size (µm); (9) particle size distribution (%); (10) drug loading (%); (11) entrapment efficiency (%); (12) yield (%); (13)(14)(15)(16)(17) percentage of curcumin released after 2 h, 4 h, 6 h, 12 h, and 24 h (%).…”

Section: Summary Of Fitmentioning

confidence: 99%

“…CQA (1) Predicted (1) Critical quality attribute; (2) particle size (%); (3) particle size distribution (%); (4) drug loading (%); (5) entrapment efficiency (%); (6)(7)(8)(9) percentage of curcumin released after 2 h, 4 h, 6 h, and 12 h (%).…”

Section: Establishment Of the Design Space And Validation Of The Modelmentioning

confidence: 99%

“…The main strategies are based on loading the compound in micro-and nanocarriers (e.g., pellets, polymeric microparticles, liposomes, polymeric nanoparticles, or micelles) which are able to deliver curcumin to colitis tissue and improve its solubility, protect it from degradation, and facilitate its delivery by specifically targeting the inflamed colon [1][2][3]. The development of curcumin-loaded micro-and nanocarriers is used not only in colon-specific drug delivery systems, but in all the delivery systems pursuing the improvement of curcumin bioavailability, drug loading, stability, and programmed release [5,6].…”

Section: Introductionmentioning

confidence: 99%

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Development of a Curcumin-Loaded Polymeric Microparticulate Oral Drug Delivery System for Colon Targeting by Quality-by-Design Approach

et al. 2020

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The purpose of this study was to apply the quality-by-design (QbD) approach for the development of colon-targeted curcumin-loaded polymeric microparticles (Col-CUR-MPs). The proportion of the enterosoluble polymer (Eudragit® FS) in the polymeric matrix, curcumin concentration, and the concentration of the polymer mixture (Eudragit® FS-polycaprolactone) were identified as potential risk factors for the quality of the final product following risk assessment. The influence of these variables on the critical quality attributes (CQAs) of Col-CUR-MPs was investigated. Therefore, a central composite face experimental design was used in order to determine the functional relationships between variables and product CQAs. The obtained regression model and contour plots were used to establish the design space. Finally, the model was validated by preparing two microparticulate formulations, one corresponding to the robust setpoint from within the design space and one outside the established design space, and calculating the percentage bias between the experimental and predicted values. The in vivo study, which was conducted on a fluorescein-loaded formulation that corresponded to the robust setpoint determined by QbD and that contained a mixture of polycaprolactone and Eudragit® FS (60:40, w/w), confirmed the colon-targeting qualities of this formulation.

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“…The LDBCs, coded as PEG 2k -b-dxDAP (where x is the number of peripheral DAP moieties), have been synthesized by clicking two performed blocks and using the first four generations of bis-MPA dendrons (G = 1, 2, 3, or 4) with x = 2, 4, 8, or 16 DAP units, respectively (Scheme 1). Together with their characterization, the self-assembly properties of the LDBCs using two different methodologies, nanoprecipitation [42][43][44][45] and microfluidics, are described. Microfludics provide controlled reaction conditions and then an excellent control on the assembly of organic nanomaterials due to their remarkable heat and mass transfer enhancement [46].…”

Section: Introductionmentioning

confidence: 99%

Supramolecular Functionalizable Linear–Dendritic Block Copolymers for the Preparation of Nanocarriers by Microfluidics

et al. 2021

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Hybrid linear–dendritic block copolymers (LDBCs) having dendrons with a precise number of peripheral groups that are able to supramolecular bind functional moieties are challenging materials as versatile polymeric platforms for the preparation of functional polymeric nanocarriers. PEG2k-b-dxDAP LDBCs that are based on polyethylene glycol (PEG) as hydrophilic blocks and dendrons derived from bis-MPA having 2,6-diacylaminopyridine (DAP) units have been efficiently synthesized by the click coupling of preformed blocks, as was demonstrated by spectroscopic techniques and mass spectrometry. Self-assembly ability was first checked by nanoprecipitation. A reproducible and fast synthesis of aggregates was accomplished by microfluidics optimizing the total flow rate and phase ratio to achieve spherical micelles and/or vesicles depending on dendron generation and experimental parameters. The morphology and size of the self-assemblies were studied by TEM, Cryogenic Transmission Electron Microscopy (cryo-TEM), and Dynamic Light Scattering (DLS). The cytotoxicity of aggregates synthesized by microfluidics and the influence on apoptosis and cell cycle evaluation was studied on four cell lines. The self-assemblies are not cytotoxic at doses below 0.4 mg mL–1. Supramolecular functionalization using thymine derivatives was explored for reversibly cross-linking the hydrophobic blocks. The results open new possibilities for their use as drug nanocarriers with a dynamic cross-linking to improve nanocarrier stability but without hindering disassembly to release molecular cargoes.

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Stable Polymer Nanoparticles with Exceptionally High Drug Loading by Sequential Nanoprecipitation

Cited by 55 publications

References 38 publications

Polymer Nanoparticles and Nanomotors Modified by DNA/RNA Aptamers and Antibodies in Targeted Therapy of Cancer

Polymer Nanoparticles and Nanomotors Modified by DNA/RNA Aptamers and Antibodies in Targeted Therapy of Cancer

Development of a Curcumin-Loaded Polymeric Microparticulate Oral Drug Delivery System for Colon Targeting by Quality-by-Design Approach

Supramolecular Functionalizable Linear–Dendritic Block Copolymers for the Preparation of Nanocarriers by Microfluidics

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