Development of quercetin-loaded PVCL–PVA–PEG micelles and application in inhibiting tumor angiogenesis through the PI3K/Akt/VEGF pathway

Qi, Xueju; Gao, Cong; Yin, Chuanjin; Fan, Junting; Wu, Xiaochen; Di, Guohu; Wang, Jing; Guo, Chenglin

doi:10.1016/j.taap.2022.115889

Cited by 20 publications

(10 citation statements)

References 36 publications

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“…However, the lipophilic and hydrophobic properties of RAPA and the existence of the blood–ocular barrier and corneal barrier greatly limit its clinical application in ophthalmology [ 40 ]. Encapsulation of the hydrophobic drugs into nanoparticles has proven to be an effective strategy for improvement of their solubility, stability, and bioavailability [ 41 , 42 ]. Here, we successfully developed an ophthalmic delivery system for RAPA using PVCL-PVA-PEG, with high encapsulation efficiency, good solubility and stability, and satisfactory bioavailability.…”

Section: Discussionmentioning

confidence: 99%

Characterization and Evaluation of Rapamycin-Loaded Nano-Micelle Ophthalmic Solution

Zhang

Wei

et al. 2023

JFB

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Rapamycin-loaded nano-micelle ophthalmic solution (RAPA-NM) offers a promising application for preventing corneal allograft rejection; however, RAPA-NM has not yet been fully characterized. This study aimed to evaluate the physicochemical properties, biocompatibility, and underlying mechanism of RAPA-NM in inhibiting corneal allograft rejection. An optimized RAPA-NM was successfully prepared using a polyvinyl caprolactam–polyvinyl acetate–polyethylene glycol (PVCL-PVA-PEG) graft copolymer as the excipient at a PVCL-PVA-PEG/RAPA weight ratio of 18:1. This formulation exhibited high encapsulation efficiency (99.25 ± 0.55%), small micelle size (64.42 ± 1.18 nm), uniform size distribution (polydispersity index = 0.076 ± 0.016), and a zeta potential of 1.67 ± 0.93 mV. The storage stability test showed that RAPA-NM could be stored steadily for 12 weeks. RAPA-NM also displayed satisfactory cytocompatibility and high membrane permeability. Moreover, topical administration of RAPA-NM could effectively prevent corneal allograft rejection. Mechanistically, a transcriptomic analysis revealed that several immune- and inflammation-related Kyoto Encyclopedia of Genes and Genomes (KEGG) pathways were significantly enriched in the downregulated genes in the RAPA-NM-treated allografts compared with the rejected allogenic corneal grafts. Taken together, these findings highlight the potential of RAPA-NM in treating corneal allograft rejection and other ocular inflammatory diseases.

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Section: Discussionmentioning

confidence: 99%

Characterization and Evaluation of Rapamycin-Loaded Nano-Micelle Ophthalmic Solution

Zhang

Wei

et al. 2023

JFB

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“…The particle size, zeta potential, and polydispersity index of PTE-MMs were analyzed using a Zetasizer (Malvern MS2000, UK). The morphology of the PTE-MMs was evaluated by transmission electron microscopy (TEM) using a JEM-1200EX microscope (JEOL Ltd., Tokyo, Japan) …”

Section: Methodsmentioning

confidence: 99%

“…The morphology of the PTE-MMs was evaluated by transmission electron microscopy (TEM) using a JEM-1200EX microscope (JEOL Ltd., Tokyo, Japan). 16 2.5. In Vitro Release Study.…”

Section: Characterization Of Pte-mmsmentioning

confidence: 99%

Pterostilbene-Loaded Soluplus/Poloxamer 188 Mixed Micelles for Protection against Acetaminophen-Induced Acute Liver Injury

et al. 2023

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Excessive acetaminophen (APAP) induces excess reactive oxygen species (ROS), leading to liver damage. Pterostilbene (PTE) has excellent antioxidant and anti-inflammatory activities, but poor solubility limits its biological activity. In this study, we prepared PTE-loaded Soluplus/poloxamer 188 mixed micelles (PTE-MMs), and the protective mechanism against APAP-induced liver injury was investigated. In vitro results showed that PTE-MMs protected H 2 O 2 -induced HepG2 cell proliferation inhibition, ROS accumulation, and mitochondrial membrane potential destruction. Immunofluorescence results indicated that PTE-MMs significantly inhibited H 2 O 2 -induced DNA damage and cGAS-STING pathway activation. For in vivo protection studies, PTE-MMs (25 and 50 mg/kg) were administered orally for 5 days, followed by APAP (300 mg/kg). The results showed that APAP significantly induced injury in liver histopathology as well as an increase in serum aspartate aminotransferase and alanine aminotransferase levels. Moreover, the above characteristics of APAPinduced acute liver injury were inhibited by PTE-MMs. In addition, APAP-induced changes in the activities of antioxidant enzymes such as SOD and GSH in liver tissue were also inhibited by PTE-MMs. Immunohistochemical results showed that PTE-MMs inhibited APAP-induced DNA damage and cGAS-STING pathway activation in liver tissues. For in vivo therapeutic effect study, mice were first given APAP (300 mg/kg), followed by oral administration of PTE-MMs (50 mg/kg) for 3 days. The results showed that PTE-MMs exhibited promising therapeutic effects on APAP-induced acute liver injury. In conclusion, our study shows that the Soluplus/poloxamer 188 MM system has the potential to enhance the biological activity of PTE in the protection and therapeutic of liver injury.

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“…In this study, we used cou6-loaded HS15 (HS15-cou6) nanomicelles to study cell uptake in HS15 delivery systems. To study the localization of HS15 nanomicelles in HK-2 cells, we used fluorescent labeling of lysosomes and mitochondria in HK-2 cells . Briefly, HK-2 cells were stained with 100 nM Lyso-Tracker and 1 μM Mito-Tracker for 20 min.…”

Section: Methodsmentioning

confidence: 99%

“…To study the localization of HS15 nanomicelles in HK-2 cells, we used fluorescent labeling of lysosomes and mitochondria in HK-2 cells. 23 Briefly, HK-2 cells were stained with 100 nM Lyso-Tracker and 1 μM Mito-Tracker for 20 min. After that, cells were treated with HS15-cou6 nanomicelles for 5 min.…”

Section: Measurement Of Antioxidant Activity In Vitromentioning

confidence: 99%

Myricetin-Loaded Nanomicelles Protect against Cisplatin-Induced Acute Kidney Injury by Inhibiting the DNA Damage-cGAS–STING Signaling Pathway

Wang

Fei

et al. 2022

Mol. Pharmaceutics

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Acute kidney injury (AKI) is the most common side effect of the anti-cancer drug cisplatin, and currently, no effective preventive measures are available in clinical practice. Oxidative stress and DNA damage mechanisms may be involved in cisplatin-induced AKI. In this study, we prepared Kolliphor HS15-based myricetin-loaded (HS15-Myr) nanomicelles and explored the mechanism of protection against cisplatininduced AKI. In vitro results showed that the HS15-Myr nanomicelles enhanced the antioxidant activity of myricetin (Myr) and inhibited cisplatin-induced proliferation inhibition of HK-2 cells. Moreover, the HS15-Myr nanomicelles inhibited cisplatin-induced reactive oxygen species accumulation, mitochondrial membrane potential reduction, and DNA damage, which might be related to the inhibition of the cyclic GMP−AMP synthase (cGAS)�stimulating interferon gene (STING) signaling pathway. In vivo results in mice showed that the significant reductions in body weight and renal indices and the increased blood urea nitrogen and serum creatinine levels induced by cisplatin could be significantly reversed by pretreating with the HS15-Myr nanomicelles. Furthermore, nanomicelle pretreatment significantly altered the activities of antioxidant enzymes (e.g., GSH, MDA, and SOD) induced by cisplatin. In addition, cisplatin-induced inflammatory responses in mouse kidney tissue were found to be inhibited by pretreatment with HS15-Myr nanomicelles, such as IL-1β and TNF-α expression. The nanomicelles also significantly inhibited cisplatin-induced activation of the DNA damage-cGAS−STING pathway in kidney tissues. Together, our findings suggest that Myr-loaded nanomicelles are potential nephroprotective drugs.

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Development of quercetin-loaded PVCL–PVA–PEG micelles and application in inhibiting tumor angiogenesis through the PI3K/Akt/VEGF pathway

Cited by 20 publications

References 36 publications

Characterization and Evaluation of Rapamycin-Loaded Nano-Micelle Ophthalmic Solution

Characterization and Evaluation of Rapamycin-Loaded Nano-Micelle Ophthalmic Solution

Pterostilbene-Loaded Soluplus/Poloxamer 188 Mixed Micelles for Protection against Acetaminophen-Induced Acute Liver Injury

Myricetin-Loaded Nanomicelles Protect against Cisplatin-Induced Acute Kidney Injury by Inhibiting the DNA Damage-cGAS–STING Signaling Pathway

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