Application of flash nanoprecipitation to fabricate poorly water-soluble drug nanoparticles

Tao, Jinsong; Chow, Shing Fung; Zheng, Ying

doi:10.1016/j.apsb.2018.11.001

Cited by 153 publications

(116 citation statements)

References 142 publications

(235 reference statements)

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“…All NPs showed to be amorphous, however, ethylcellulose characteristic peak showed an observable intensity that can be also seen in ethylcellulose NPs and loaded ethylcellulose NPs. Results reported by Tao et al [ 50 ] revealed that nanoparticles produced by nanoprecipitation were usually amorphous and less stable during storage compared to their crystalline counterpart. Since amorphous compounds easily recrystallise in water, and therefore increase aggregation, a desirable solution is to freeze-dry the samples for an improved stability.…”

Section: Resultsmentioning

confidence: 99%

Bio-Based Nanoparticles as a Carrier of β-Carotene: Production, Characterisation and In Vitro Gastrointestinal Digestion

et al. 2020

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β-carotene loaded bio-based nanoparticles (NPs) were produced by the solvent-displacement method using two polymers: zein and ethylcellulose. The production of NPs was optimised through an experimental design and characterised in terms of average size and polydispersity index. The processing conditions that allowed to obtain NPs (<100 nm) were used for β-carotene encapsulation. Then β-carotene loaded NPs were characterised in terms of zeta potential and encapsulation efficiency. Transmission electron microscopy, Fourier transform infrared spectroscopy and X-ray diffraction analysis were performed for further morphological and chemical characterisation. In the end, a static in vitro digestion following the INFOGEST protocol was performed and the bioaccessibility of β-carotene encapsulated in both NPs was determined. Results show that the best conditions for a size-controlled production with a narrow size distribution are lower polymer concentrations and higher antisolvent concentrations. The encapsulation of β-carotene in ethylcellulose NPs resulted in nanoparticles with a mean average size of 60 ± 9 nm and encapsulation efficiency of 74 ± 2%. β-carotene loaded zein-based NPs resulted in a mean size of 83 ± 8 nm and encapsulation efficiency of 93 ± 4%. Results obtained from the in vitro digestion showed that β-carotene bioaccessibility when encapsulated in zein NPs is 37 ± 1%, which is higher than the value of 8.3 ± 0.1% obtained for the ethylcellulose NPs.

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Section: Resultsmentioning

confidence: 99%

Bio-Based Nanoparticles as a Carrier of β-Carotene: Production, Characterisation and In Vitro Gastrointestinal Digestion

et al. 2020

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“…32,33 Importantly, PMMA-based NPs can be loaded by various active compounds and contrast agents (including drugs). 34,35 Therefore, dye-loaded PMMA NPs appear as highly promising candidate for in vivo imaging down to single-particle sensitivity, but this would require rendering them "stealth" properties.…”

Section: Meaningful Monitoring Of the Behavior Of Single Nps In Vivo mentioning

confidence: 99%

Ultrabright Fluorescent Polymeric Nanoparticles with a Stealth Pluronic Shell for Live Tracking in the Mouse Brain

Khalin¹,

Heimburger

Melnychuk

et al. 2020

ACS Nano

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The inability to visualize single organic nanoparticles (NPs) in vivo is an unsolved issue in the field of nanomedicine. To enable high single particle fluorescence, we loaded polymer poly(methyl methacrylate)-sulfonate (PMMA-SO3H) NPs with octadecyl rhodamine B together with hydrophobic counter-ions as a fluorophore insulator to prevent aggregation-induced quenching. To create NPs with stealth properties we used the amphiphilic block copolymers pluronic F-127 and F-68. Fluorescence correlation spectroscopy (FCS) and Förster resonance energy transfer (FRET) showed that pluronics remain at the NP surface after dialysis (density: one amphiphile per 5.5 nm 2) and protected NPs from degradation by serum proteins and surfactants. Single particle brightness was increased 150-fold as compared to commercially available preparations by increasing dye loading to 20 wt% and optimizing particle size. Added to primary cultured neurons, these NPs were stable and interacted with dendrites and axons. After intravenous injection in mice, NPs could be tracked in cerebral vessels for at least 1h by in vivo two-photon microscopy. Following brain injury or neuroinflammation, NPs extravasated from meningeal vessels, were taken up by meningeal macrophages, and entered the brain parenchyma. In summary, we developed biocompatible NPs suitable for drug delivery with in vitro and in vivo stealth properties and extremely bright fluorescence. Thus, individual NPs could be tracked in mouse brain and their dynamics visualized with subcellular resolution. Using superbright NPs may thus open new avenues for the investigation of NPs in living organisms.

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“…The supersaturation required for homogeneous nucleation is much higher than for heterogeneous nucleation. In addition, heterogeneous nucleation can occur because the formed nuclei can reduce the critical free energy for nucleation formulation and it can occur at a lower supersaturation condition [70]. Thus, nanocrystallization of rifampicin can be feasible, even if the homogenous saturation conditions were not achieved.…”

Section: Study Of Rifampicin Loading and Entrapment Efficiency By Batmentioning

confidence: 99%

Microflow Nanoprecipitation of Positively Charged Gastroresistant Polymer Nanoparticles of Eudragit® RS100: A Study of Fluid Dynamics and Chemical Parameters

et al. 2020

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The objective of the present work was to produce gastroresistant Eudragit® RS100 nanoparticles by a reproducible synthesis approach that ensured mono-disperse nanoparticles under the size of 100 nm. Batch and micromixing nanoprecipitation approaches were selected to produce the demanded nanoparticles, identifying the critical parameters affecting the synthesis process. To shed some light on the formulation of the targeted nanoparticles, the effects of particle size and homogeneity of fluid dynamics, and physicochemical parameters such as polymer concentration, type of solvent, ratio of solvent to antisolvent, and total flow rate were studied. The physicochemical characteristics of resulting nanoparticles were studied applying dynamic light scattering (DLS) particle size analysis and electron microscopy imaging. Nanoparticles produced using a micromixer demonstrated a narrower and more homogenous distribution than the ones obtained under similar conditions in conventional batch reactors. Besides, fluid dynamics ensured that the best mixing conditions were achieved at the highest flow rate. It was concluded that nucleation and growth events must also be considered to avoid uncontrolled nanoparticle growth and evolution at the collection vial. Further, rifampicin-encapsulated nanoparticles were prepared using both approaches, demonstrating that the micromixing-assisted approach provided an excellent control of the particle size and polydispersity index. Not only the micromixing-assisted nanoprecipitation promoted a remarkable control in the nanoparticle formulation, but also it enhanced drug encapsulation efficiency and loading, as well as productivity. To the best of our knowledge, this was the very first time that drug-loaded Eudragit® RS100 nanoparticles (NPs) were produced in a continuous fashion under 100 nm (16.5 ± 4.3 nm) using microreactor technology. Furthermore, we performed a detailed analysis of the influence of various fluid dynamics and physicochemical parameters on the size and uniformity of the resulting nanoparticles. According to these findings, the proposed methodology can be a useful approach to synthesize a myriad of nanoparticles of alternative polymers.

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Application of flash nanoprecipitation to fabricate poorly water-soluble drug nanoparticles

Cited by 153 publications

References 142 publications

Bio-Based Nanoparticles as a Carrier of β-Carotene: Production, Characterisation and In Vitro Gastrointestinal Digestion

Bio-Based Nanoparticles as a Carrier of β-Carotene: Production, Characterisation and In Vitro Gastrointestinal Digestion

Ultrabright Fluorescent Polymeric Nanoparticles with a Stealth Pluronic Shell for Live Tracking in the Mouse Brain

Microflow Nanoprecipitation of Positively Charged Gastroresistant Polymer Nanoparticles of Eudragit® RS100: A Study of Fluid Dynamics and Chemical Parameters

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