Amorphous Nanosuspensions Aggregated from Paclitaxel–Hemoglobulin Complexes with Enhanced Cytotoxicity

Qin, Chao; Xin, Xiaoqing; Xue, Ping; Yin, Lifang; He, Wei

doi:10.3390/pharmaceutics10030092

Cited by 4 publications

(5 citation statements)

References 29 publications

(33 reference statements)

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“…In addition, the improvement in dissolution may be associated with the crystal form of the nanoparticles. Previous studies have reported that formulations with amorphous forms revealed a higher dissolution than crystalline formulations [31].…”

Section: Resultsmentioning

confidence: 84%

“…The high cytotoxicity of nanosuspensions compared with pure isoliquiritigenin may be ascribed to higher internalization of nanosuspensions into cells by phagocytosis, owing to their small particle size [32]. In addition, nanoparticles have greater adhesion to cell membranes than free drugs [33], and nanosuspensions can rapidly release large amounts of drug into cells, thus improving cytostatic activity [31]. An insignificant difference in cytotoxicity was obtained with high concentrations of nanosuspensions and cells incubated for long times, as also found in previous studies [34], possibly because the nanoparticles reached saturation in cells under high concentrations and incuba- tion times.…”

Section: Resultsmentioning

confidence: 99%

“…Thus, the nanosuspension had better cell apoptosis induction ability than the isoliquiritigenin solution, as confirmed by many studies [30,35] and in accordance with the cytotoxicity results. Qin et al [31] reported that an amorphous nanosuspension induces apoptosis of cells with higher efficiency than a crystalline nanosuspension; the greater ability of PVP K30-ISL-NS to induce cell apoptosis may be due to its partially amorphous form.…”

Section: Resultsmentioning

confidence: 99%

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Isoliquiritigenin Nanosuspension Enhances Cytostatic Effects in A549 Lung Cancer Cells

et al. 2020

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Isoliquiritigenin, a flavonoid extracted from licorice root, has been shown to be active against most cancer cells; however, its antitumor activity is limited by its poor water solubility. The aim of this study was to develop a stable isoliquiritigenin nanosuspension for enhanced solubility and to evaluate its in vitro cytostatic activity in A549 cells. The nanosuspension of isoliquiritigenin was prepared through wet media milling with HPC SSL (hydroxypropyl cellulose-SSL) and PVP K30 (polyinylpyrrolidone-K30) as stabilizers, and the samples were then characterized according to particle size, zeta-potential, SEM (scanning electron microscopy), TEM (transmission electron microscopy), DSC (differential scanning calorimetry), XRPD (X-ray powder diffraction), FTIR (Fourier transform infrared spectroscopy), XPS (X-ray photoelectron spectroscopy), and in vitro release. The isoliquiritigenin nanosuspension prepared with HPC SSL and PVP K30 had particle sizes of 238.1 ± 4.9 nm and 354.1 ± 9.1 nm, respectively. Both nanosuspensions showed a surface charge of approximately − 20 mV and a lamelliform or ellipse shape. The dissolution of isoliquiritigenin from the 2 nanosuspensions was markedly higher than that of free isoliquiritigenin. In vitro studies on A549 cells indicated that the cytotoxicity and cellular uptake significantly improved after treatment with both nanosuspensions in comparison to the isoliquiritigenin solution. Furthermore, cell apoptosis analysis showed a 7.5 – 10-fold increase in the apoptosis rate induced by both nanosuspensions compared with pure drug. However, the cytotoxicity of pure drug and nanosuspension on normal cells (HELF) was lower, which indicated both isoliquiritigenin nanosuspensions have low toxicity to normal cells. Therefore, the isoliquiritigenin nanosuspension prepared with HPC SSL and PVP K30 as stabilizers may be a promising approach to improve the solubility and cytostatic activity of isoliquiritigenin.

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Section: Resultsmentioning

confidence: 84%

Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

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Isoliquiritigenin Nanosuspension Enhances Cytostatic Effects in A549 Lung Cancer Cells

et al. 2020

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“…Since the binding of the SrtA protein is static quenching, the binding constant K A can be calculated according to the static quenching formula Lg[(F 0 -F)/F] = Lg K A + nlg Q. The binding constant (K A ) of SrtA after the addition of isosakuranetin was calculated to be 3.88 × 10 4 L/mol, which is greater than 10 4 L/mol and is considered a strong interaction [ 39 ], indicating that isosakuranetin binds to SrtA ( Figure 5b ).…”

Section: Resultsmentioning

confidence: 99%

Exploring the modulatory impact of isosakuranetin on Staphylococcus aureus : Inhibition of sortase A activity and α-haemolysin expression

Tian,

Wang,

Yang

et al. 2023

Virulence

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The ubiquity of methicillin-resistant Staphylococcus aureus (MRSA) and the mounting prevalence of antibiotic resistance necessitate the identification of novel therapeutic approaches to reduce the selective pressure of antibiotics. Targeting bacterial virulence factors, such as the pivotal Sortase A (SrtA) in S. aureus for adhesion and invasion, and the salient toxin α-Hemolysin (Hla), offers a sophisticated approach to attenuate pathogenicity without bacterial elimination. Herein, we report the discovery of a flavonoid, isosakuranetin, which inhibits the activity of S. aureus SrtA. A fluorescence resonance energy transfer assay revealed that isosakuranetin exhibited a low IC 50 of 21.20 μg/mL. Furthermore, isosakuranetin significantly inhibited SrtA-related virulence properties, such as bacterial adhesion to fibrinogen, biofilm formation, and invasion of A549 cells. We employed fluorescence quenching and molecular docking to determine the interactions between isosakuranetin and SrtA, revealing the key amino acid sites for binding. Importantly, isosakuranetin inhibited the haemolytic activity of S. aureus in vitro at a concentration of 32 μg/mL. Moreover, isosakuranetin effectively suppressed the transcription and expression of Hla in a dose-dependent manner and regulated the transcription of RNAIII , the upstream operator of Hla. Notably, isosakuranetin demonstrated in vivo efficacy in a mouse model of S. aureus -induced pneumonia by significantly improving survival rates and reducing lung damage. This is a valuable finding, as isosakuranetin’s dual inhibitory effects on SrtA and haemolytic activity, as well as its anti-virulence activity against MRSA, make it an excellent candidate for therapeutic development.

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“…Generally, nanocrystals do not use carriers, have few excipients, are simple to prepare, and have a high drug load. If the drug nanocrystals are controlled by particle size or modified by surface, they can also target specific parts, such as the liver, spleen, brain, or tumor tissues ( Qin et al, 2018 ). In addition, studies have shown that nanocrystals can improve the uptake of insoluble drugs in Caco-2 cells and the transmembrane transport rate ( Di Costanzo and Angelico, 2019 ).…”

Section: Review Of Ua Nanoformulationsmentioning

confidence: 99%

Nanoformulations of Ursolic Acid: A Modern Natural Anticancer Molecule

et al. 2021

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Background: Ursolic acid (UA) is a natural pentacyclic triterpene derived from fruit, herb, and other plants. UA can act on molecular targets of various signaling pathways, inhibit the growth of cancer cells, promote cycle stagnation, and induce apoptosis, thereby exerting anticancer activity. However, its poor water-solubility, low intestinal mucosal absorption, and low bioavailability restrict its clinical application. In order to overcome these deficiencies, nanotechnology, has been applied to the pharmacological study of UA.Objective: In this review, we focused on the absorption, distribution, and elimination pharmacokinetics of UA in vivo, as well as on the research progress in various UA nanoformulations, in the hope of providing reference information for the research on the anticancer activity of UA.Methods: Relevant research articles on Pubmed and Web of Science in recent years were searched selectively by using the keywords and subheadings, and were summarized systematically.Key finding: The improvement of the antitumor ability of the UA nanoformulations is mainly due to the improvement of the bioavailability and the enhancement of the targeting ability of the UA molecules. UA nanoformulations can even be combined with computational imaging technology for monitoring or diagnosis.Conclusion: Currently, a variety of UA nanoformulations, such as micelles, liposomes, and nanoparticles, which can increase the solubility and bioactivity of UA, while promoting the accumulation of UA in tumor tissues, have been prepared. Although the research of UA in the nanofield has made great progress, there is still a long way to go before the clinical application of UA nanoformulations.

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Amorphous Nanosuspensions Aggregated from Paclitaxel–Hemoglobulin Complexes with Enhanced Cytotoxicity

Cited by 4 publications

References 29 publications

Isoliquiritigenin Nanosuspension Enhances Cytostatic Effects in A549 Lung Cancer Cells

Isoliquiritigenin Nanosuspension Enhances Cytostatic Effects in A549 Lung Cancer Cells

Exploring the modulatory impact of isosakuranetin on Staphylococcus aureus : Inhibition of sortase A activity and α-haemolysin expression

Nanoformulations of Ursolic Acid: A Modern Natural Anticancer Molecule

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