Repeated treatment with VEGF receptor inhibitors induces phenotypic changes in endothelial cells and pericytes in the rat retina DOI

Ayuki Nakano,

T Kawada,

Akane Morita

et al.

Microvascular Research, Journal Year: 2024, Volume and Issue: unknown, P. 104756 - 104756

Published: Oct. 1, 2024

Language: Английский

Recent development of VEGFR small molecule inhibitors as anticancer agents: A patent review (2021–2023) DOI
Jing Zeng,

Qichuan Deng,

Zheng Chen

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 146, P. 107278 - 107278

Published: March 9, 2024

Language: Английский

Citations

14

Co-delivery of antioxidants and siRNA-VEGF: promising treatment for age-related macular degeneration DOI
Marina França Dias, Estael Luzia Coelho da Cruz-Cazarim, Frederico Pittella

et al.

Drug Delivery and Translational Research, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 3, 2025

Language: Английский

Citations

1

Topical Ophthalmic Liposomes Dual-Modified with Penetratin and Hyaluronic Acid for the Noninvasive Treatment of Neovascular Age-Related Macular Degeneration DOI Creative Commons
Chen Sun, Shuyue Zhang, Nan Xu

et al.

International Journal of Nanomedicine, Journal Year: 2024, Volume and Issue: Volume 19, P. 1887 - 1908

Published: Feb. 1, 2024

Introduction: Since intrinsic ocular barrier limits the intraocular penetration of therapeutic protein through eye drops, repeated intravitreal injections anti-vascular endothelial growth factor (anti-VEGF) agents are standard therapy for neovascular age-related macular degeneration (nAMD), which highly invasive and may cause particular complications, leading to poor patient compliance. Methods: Using Penetratin (Pen) as enhancer hyaluronic acid (HA) retina-targeting ligand, a dual-modified ophthalmic liposome (Penetratin acid-liposome/Conbercept, PenHA-Lip/Conb) drop was designed non-invasively penetrate deliver anti-VEGF targeted tissue. Results: PenHA-Lip effectively penetrates targets retinal pigment epithelium via corneal non-corneal pathways. After single topical administration conbercept-loaded (PenHA-Lip/Conb), concentration conbercept peaked at 18.74 ± 1.09 ng/mL 4 h, is 11.55-fold higher than unmodified conbercept. In laser-induced choroidal neovascularization (CNV) mouse model, PenHA-Lip/Conb drops three times daily seven days inhibited CNV formation progression without any significant tissue toxicity achieved an equivalent effect injection. Conclusion: efficiently safely delivered posterior segment be promising noninvasive option nAMD. Keywords: drug delivery, liposomes, Penetratin, acid,

Language: Английский

Citations

7

Theranostic role of 89Zr- and 177Lu-labeled aflibercept in breast cancer DOI
Qi Yang, Zhao Chen,

Yongkang Qiu

et al.

European Journal of Nuclear Medicine and Molecular Imaging, Journal Year: 2023, Volume and Issue: 51(5), P. 1246 - 1260

Published: Dec. 23, 2023

Language: Английский

Citations

12

The Diagnosis and Treatment of Branch Retinal Vein Occlusions: An Update DOI Creative Commons

Diana‐Maria Dărăbuş,

Rodica Georgiana Dărăbuș,

Mihnea Munteanu

et al.

Biomedicines, Journal Year: 2025, Volume and Issue: 13(1), P. 105 - 105

Published: Jan. 5, 2025

Branch retinal vein occlusion (BRVO) is a common vascular condition and significant contributor to vision loss worldwide, particularly in middle-aged elderly populations. This review synthesizes current knowledge on the epidemiology, pathogenesis, clinical features of BRVO, alongside recent advancements diagnostic therapeutic strategies. BRVO approximately four times more prevalent than central (CRVO) often leads impairment. By focusing this aims address specific challenges its diagnosis management. The pathophysiology complex, involving factors such as venous compression, inflammation, increased levels endothelial growth factor (VEGF). Diagnostic approaches optical coherence tomography (OCT) fluorescein angiography are highlighted for their roles assessing disease severity guiding treatment decisions. Therapeutic interventions, including laser photocoagulation, anti-VEGF therapy, intravitreal corticosteroids, critically evaluated, emphasizing emerging treatments gene peptide-based agents, small-molecule inhibitors. Despite management strategies, recurrence macular edema resistance remain challenges. Continued research essential refine protocols improve long-term visual outcomes patients with BRVO.

Language: Английский

Citations

0

A Bifunctional Peptide with Penetration Ability for Treating Retinal Angiogenesis via Eye Drops DOI
Jing Liao, Lin Zhao, Hongyuan Chen

et al.

Molecular Pharmaceutics, Journal Year: 2025, Volume and Issue: unknown

Published: Jan. 14, 2025

Numerous diseases, such as diabetic retinopathy and age-related macular degeneration, can lead to retinal neovascularization, which seriously impair the visual function potentially result in blindness. The presence of blood–retina barrier makes it challenging for ocularly administered drugs penetrate physiological barriers reach ocular posterior segments, including retina choroid. Herein, we developed an innovative bifunctional peptide, Tat-C-RP7, exhibits excellent penetration capabilities antiangiogenic properties aimed at treating neovascularization diseases. RP7 is NRP-1 targeting peptide that blocks vascular endothelial growth factor receptor-2 (VEGFR-2) signaling inhibits angiogenesis, while Tat facilitates delivery various cargoes across biological barriers, barrier. By combining these attributes, Tat-C-RP7 anticipated traverse via topical administration exert its effects segment. Experimental results demonstrated significantly inhibited proliferation migration rat microvascular cells effectively reduced tubule formation vitro. Its activity was confirmed zebrafish. outstanding penetrative FITC-labeled have been validated through cell uptake assays, vitro models, ex-vivo tissues, vivo studies. Besides, half-life longer than RP7. In oxygen-induced model, shown reduce area angiogenesis following administration. Additionally, produced no irritating on eyes rabbits. Overall, demonstrates penetrability represents a promising therapeutic option

Language: Английский

Citations

0

Protective Role and Enhanced Intracellular Uptake of Curcumin in Retinal Cells Using Self-Emulsifying Drug Delivery Systems (SNEDDS) DOI Creative Commons
Elide Zingale,

Sebastiano Masuzzo,

Tatu Lajunen

et al.

Pharmaceuticals, Journal Year: 2025, Volume and Issue: 18(2), P. 265 - 265

Published: Feb. 17, 2025

Background: Sirtuin-1 (SIRT1), a histone deacetylase enzyme expressed in ocular tissues with intracellular localization, plays critical protective role against various degenerative diseases. The link between reduced SIRT1 levels and diabetic retinopathy (DR) has prompted the exploration of natural therapeutic compounds that act as agonists. Curcumin (CUR), which been shown to upregulate expression, is one such promising compound. However, effective delivery CUR deeper tissues, particularly retina, remains challenge due its poor solubility limited penetration following topical administration. Within this context, development self-nanoemulsifying drug systems (SNEDDS) for represents novel approach. Methods: In accordance our prior research, optimized SNEDDS loaded were developed characterized post-reconstitution simulated tear fluid (STF) at 1:10 ratio, showing suitable physicochemical technological parameters delivery. Results: An entrapment efficiency (EE%) approximately 99% an absence precipitation noticed upon resuspension STF. CUR-SNEDDS resulted better stability release profile than free under conditions. vitro analysis mucoadhesive properties revealed CUR-SNEDDS, modified cationic lipid, demonstrated enhanced interactions mucin, indicating potential improved retention. Cytotoxicity tests did not affect viability human corneal epithelial (HCE) cells up concentrations 3 μM displayed superior antioxidant activity compared oxidative stress model using retinal pigment (ARPE-19) exposed hydroquinone (HQ). Cell uptake studies confirmed accumulation within exposure neat CUR. lower concentrations, found effectively induce expression. Conclusions: cytocompatibility, properties, cellular suggest these hold promise formulations retina.

Language: Английский

Citations

0

Targeting endothelial glycolytic reprogramming by tsRNA-1599 for ocular anti-angiogenesis therapy DOI Creative Commons
Xiaoyan Han, Lingjie Kong, Duo Li

et al.

Theranostics, Journal Year: 2024, Volume and Issue: 14(9), P. 3509 - 3525

Published: Jan. 1, 2024

Current treatments for ocular angiogenesis primarily focus on blocking the activity of vascular endothelial growth factor (VEGF), but unfavorable side effects and unsatisfactory efficacy remain issues. The identification novel targets anti-angiogenic treatment is still needed.

Language: Английский

Citations

3

Novel artemisinin derivative P31 inhibits VEGF-induced corneal neovascularization through AKT and ERK1/2 pathways DOI Creative Commons
Wen Ding,

Yingxue Su,

Jianshan Mo

et al.

Heliyon, Journal Year: 2024, Volume and Issue: 10(8), P. e29984 - e29984

Published: April 1, 2024

Corneal neovascularization (CoNV)is a major cause of blindness in many ocular diseases. Substantial evidence indicates that vascular endothelial growth factor (VEGF) plays an important role the pathogenesis corneal neovascularization. Previous showed artemisinin may inhibit angiogenesis through down regulation VEGF receptors. We designed and synthesized derivatives, validated their inhibitory effect on cell animal models, explored mechanisms by which they exert CoNV. Among these P31 demonstrated significant anti-angiogenic effects vivo vitro. Besides, inhibited VEGF-induced HUVECs rabbit model via AKT ERK pathways. Moreover, alleviated angiogenic inflammatory responses suture cornea. In conclusion, as novel derivative, attenuates has promising application

Language: Английский

Citations

1

Development of dual drug loaded-hydrogel scaffold combining microfluidics and coaxial 3D-printing for intravitreal implantation DOI Creative Commons
Elide Zingale, Edward M. Weaver, Pietro Maria Bertelli

et al.

International Journal of Pharmaceutics, Journal Year: 2024, Volume and Issue: unknown, P. 124700 - 124700

Published: Sept. 1, 2024

Language: Английский

Citations

1