A method to Quantify the Affinity of Cabazitaxel for PLA-PEG Nanoparticles and Investigate the Influence of the Nano-Assembly Structure on the Drug/Particle Association

Diou, Odile; Greco, Stéphanie; Beltran, Thierry; Lairez, D.; Authelin, Jean‐René; Bazile, Didier

doi:10.1007/s11095-015-1696-0

Cited by 19 publications

(8 citation statements)

References 34 publications

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“…The GM diameter decreased whereas EE and DLE increased as the concentration of the nonionic surfactant Tween 80 increased (Figures 3(b) and 4(b)). These results agree with previous studies [36,37] and indicate that Tween 80, which is widely used as a wetting agent, emulsifier, lubricant, and diffusion agent in pharmaceutical excipients, may help form GMs.…”

Section: Synthesis and Characterization Of Gmssupporting

confidence: 93%

Preparation and Characterization of PEG-PLA Genistein Micelles Using a Modified Emulsion-Evaporation Method

Cheng

Qin

et al. 2020

Journal of Nanomaterials

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The objective of this study is to improve the bioavailability of genistein by encapsulation with polyethylene glycol-polylactic acid (PEG-PLA) copolymers. Genistein micelles (GMs) prepared using a modified emulsion-evaporation method were more stable than those made with the original method. The effect of polyvinyl alcohol, Tween 80, sonication time, PEG-PLA/genistein ratio, and organic phase (acetone)/H2O ratio on the size, polydispersity index, encapsulation efficiency, and drug loading efficiency of GMs was investigated. GMs were obtained and characterized under optimal experimental conditions. For long-term storage, GMs were lyophilized by freeze drying with trehalose to produce genistein lyophilized powder (GLP). The analysis of GLP by Fourier-transform infrared spectroscopy and differential scanning calorimetry showed that genistein was successfully incorporated into the micellar structure. In vitro release experiments revealed that the incorporation of genistein into PEG-PLA copolymers significantly improved its solubility and bioavailability. GLP was more potent in inhibiting the proliferation of HSC-T6 cells than genistein. Treatment with GLP at 10–20 μg/mL for 48 h significantly inhibited the protein expression of α-smooth muscle actin and collagen I in HSC-T6 cells compared with the control. These data demonstrated that the improved solubility and bioavailability of genistein in the form of GLP enhanced its antifibrotic effect in vitro.

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Section: Synthesis and Characterization Of Gmssupporting

confidence: 93%

Preparation and Characterization of PEG-PLA Genistein Micelles Using a Modified Emulsion-Evaporation Method

Cheng

Qin

et al. 2020

Journal of Nanomaterials

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“…Previous studies have reported that bulk PEG chain conformations in di-block copolymers change depending on their crystalline temperature [ 31 , 32 ]. Moreover, it was also reported that PLA-PEG or PLGA-PEG NPs prepared by anti-solvent precipitation feature embedded PEG chains in the core [ 33 , 34 ].…”

Section: Discussionmentioning

confidence: 99%

Processing Parameters and Ion Excipients Affect the Physicochemical Characteristics of the Stereocomplex-Formed Polylactide-b-Polyethylene Glycol Nanoparticles and Their Pharmacokinetics

et al. 2022

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To optimize the characteristics of stereocomplex polylactide-b-polyethylene glycol nanoparticles (SC-PEG NPs) in terms of pharmacokinetics (PK), we chose continuous anti-solvent precipitation with a T-junction as a preparation method and investigated the effect of using solvents containing an ion excipient (lithium bromide, LiBr) on the characteristics of SC-PEG NPs by changing the processing temperature and total flow rate (TFR). Processing temperatures above the melting temperature (Tm) of the PEG domain produced a sharper polydispersity and denser surface PEG densities of SC-PEG NPs than those produced by processing temperatures below the Tm of the PEG domains. Response surface analysis revealed that a higher LiBr concentration and slower TFR resulted in larger and denser hydrodynamic diameters (Dh) and surface PEG densities, respectively. However, a high concentration (300 mM) of LiBr resulted in a decreased drug loading content (DLC). 14C-tamoxifen-loaded 111In-SC-PEG NPs with larger Dh and denser surface PEG densities showed a prolonged plasma retention and low tissue distribution after intravenous injection in mice. These results indicate that the novel strategy of using solvents containing LiBr at different processing temperatures and TFR can broadly control characteristics of SC-PEG NPs, such as Dh, surface PEG densities, and DLC, which alter the PK profiles and tissue distributions.

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“…between the various entities (small molecules, nucleic acids, peptides, proteins) and nanomedicines. A methodology to calculate the fraction of nano-encapsulated drug after manufacturing, and after the dilution in blood following intravenous administration was developed and applied to the anticancer drug cabazitaxel encapsulated in Poly(lactic)-Polyethylen glycol (PLA-PEG) NPs (Diou et al, 2015; Lakkireddy and Bazile, 2016).…”

Section: Critical Quality Attributesmentioning

confidence: 99%

Bridging communities in the field of nanomedicine

Halamoda-Kenzaoui

Baconnier

Bastogne

et al. 2019

Regulatory Toxicology and Pharmacology

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An early dialogue between nanomedicine developers and regulatory authorities are of utmost importance to anticipate quality and safety requirements for these innovative health products. In order to stimulate interactions between the various communities involved in a translation of nanomedicines to clinical applications, the European Commission's Joint Research Centre hosted a workshop titled “Bridging communities in the field of Nanomedicine” in Ispra/Italy on the 27th −28th September 2017. Experts from regulatory bodies, research institutions and industry came together to discuss the next generation of nanomedicines and their needs to obtain regulatory approval. The workshop participants came up with recommendations highlighting methodological gaps that should be addressed in ongoing projects addressing the regulatory science of nanomedicines. In addition, individual opinions of experts relevant to progress of the regulatory science in the field of nanomedicine were summarised in the format of a survey.

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A method to Quantify the Affinity of Cabazitaxel for PLA-PEG Nanoparticles and Investigate the Influence of the Nano-Assembly Structure on the Drug/Particle Association

Abstract: The methodological tool described here showed that the difference in cabazitaxel/nanoparticle association between aggregates and micelles could be attributed to the difference in PLA-PEG chains packing.

Cited by 19 publications

References 34 publications

Preparation and Characterization of PEG-PLA Genistein Micelles Using a Modified Emulsion-Evaporation Method

Preparation and Characterization of PEG-PLA Genistein Micelles Using a Modified Emulsion-Evaporation Method

Processing Parameters and Ion Excipients Affect the Physicochemical Characteristics of the Stereocomplex-Formed Polylactide-b-Polyethylene Glycol Nanoparticles and Their Pharmacokinetics

Bridging communities in the field of nanomedicine

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