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estradiol (Estreva oral / Estreva / Estreva gel)

✓ Approved

Merck KGaA · ESR1 · 小分子

什么是 estradiol?

estradiol 是一种小分子,由Merck KGaA研发。该药已获批,用于治疗相关适应症,给药途径:Oral (PO)、Transdermal。

药物档案

商品名Estreva oral, Estreva, Estreva gel
公司Merck KGaA
药物类别小分子
分子靶点ESR1
给药途径Oral (PO), Transdermal
状态Approved

作用机制

分子靶点

estradiol 作用于 1 个分子靶点:

ESR1estrogen receptor 1 (ER, ESR)
需要更深入的分析?Noah AI 可解释复杂机制并与同类药物比较。

治疗适应症

estradiol 针对 1 个适应症,涉及 1 个治疗领域。

治疗领域疾病/病症分期
Surgical and medical proceduresHormone replacement therapy✓ Approved

相关研究文献

PubMedGels (Basel, Switzerland)2026-10-26

Development and Optimization of a Lupeol-Loaded Bilosomal Gel for Enhanced Topical Therapy of Imiquimod-Induced Psoriasis.

Hamza Mohammad M, Samanta Soumya S, Khan Mohammed Faheem MF, Roy Supriya S et al.

Lupeol, a naturally occurring pentacyclic triterpenoid, exhibits potent anti-inflammatory and antioxidant activities, making it a promising candidate for psoriasis treatment. However, its poor aqueous solubility and limited skin permeation restrict its therapeutic application. This study aimed to develop and optimize a lupeol-loaded bilosomal gel to enhance topical delivery and improve anti-psoriatic efficacy. Lupeol-loaded bilosomes were prepared using the thin-film hydration method and optimized through a Box-Behnken experimental design. The optimized formulation was characterized for vesicle size, entrapment efficiency, drug release, and physicochemical properties before incorporation into a Carbopol® 934P gel. The bilosomal gel was further evaluated through in vitro drug release, ex vivo skin permeation, and in vivo efficacy in an imiquimod-induced psoriasis-like mice model. The optimized bilosomes exhibited nanoscale vesicles, high drug entrapment, and sustained drug release. Incorporation into the gel produced a formulation with suitable physicochemical characteristics and significantly enhanced skin permeation compared with a conventional gel. In vivo, the bilosomal gel markedly reduced Psoriasis Area and Severity Index (PASI) scores, spleen index, and TNF-α levels while restoring normal skin histology. These findings demonstrate that bilosomal encapsulation substantially improves the topical delivery and therapeutic efficacy of lupeol, highlighting the developed bilosomal gel as a promising nanocarrier-based strategy for the topical management of psoriasis.

PMID 42929952
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PubMedCells2026-10-26

Selective Estradiol Sensitivity in 12Z Human Endometriotic Epithelial Cell Line.

Banerjee Shohini S, Chopra Esha E, Smith Ian M IM, Stroka Kimberly M KM

Estradiol (E2) is a potent estrogen molecule that plays a crucial role in regulating numerous healthy and pathophysiological processes. To model estrogen-dependent cellular activities in vitro in a physiologically meaningful way, cells chosen for experimentation should exhibit sensitivity to E2. The 12Z human endometriotic epithelial cell line is gaining attention as a model for estrogen-dependent conditions, but its functional responsiveness to E2 has not been well characterized. For the passage range in the following study, we found that E2 does not statistically significantly influence 12Z proliferation, wound closure, or single-cell migration. However, 12Zs were selectively responsive to E2 in 3D migration models where the cells were physically confined. Upregulating ESR1, the primary mediator of estrogenic action, in the 12Zs did not enhance their functional E2 sensitivity. These results highlight the importance of verifying hormone responsiveness when using 12Z cells to model estrogen-dependent processes and conditions.

PMID 42929847
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PubMedGels (Basel, Switzerland)2026-10-26

Nano-SiO2/Polymer Composite Gel Fluid-Loss Reducer for High-Temperature, Salt-Resistant Water-Based Drilling Fluids: Performance and Mechanism.

Liu Luman L, Liu Jingping J, Geng Yuan Y, Wang Ren R et al.

Polymeric gel fluid-loss reducers for water-based drilling fluids often undergo performance deterioration under combined high-temperature and high-salinity conditions. In this study, an organic-inorganic nanocomposite gel fluid-loss reducer, SiO2@P-DAS, was synthesized through aqueous free-radical polymerization using N,N-dimethylacrylamide, 2-acrylamido-2-methylpropane sulfonic acid, sodium styrene sulfonate, and KH-570-modified nano-SiO2. The corresponding polymer gel without nano-SiO2, P-DAS, was used as the control. FTIR results were consistent with the presence of modified nano-SiO2 in the composite gel. Thermogravimetric analysis showed that its initial decomposition temperature increased from 245 °C for P-DAS to 252 °C for SiO2@P-DAS. At a concentration of 3.0 wt%, the post-aging API filtrate volume of SiO2@P-DAS was 3.8 mL, compared with 4.8 mL for P-DAS after aging at 220 °C for 16 h. Under HTHP conditions of 220 °C and 3.5 MPa, the corresponding filtrate volumes were 33.33 and 49.67 mL, respectively. SiO2@P-DAS also maintained lower fluid loss under NaCl and CaCl2 contamination. At 5 wt% CaCl2, its post-aging API filtrate volume was 6.8 mL, 58.0% lower than that of P-DAS. In weighted drilling fluids with densities of 1.4-2.0 g/cm3, the post-aging API and HTHP filtrate volumes remained within 2.4-3.2 and 24.6-26.2 mL, respectively. Zeta-potential, particle-size, and filter-cake observations suggest that polymer adsorption and hydration, together with the contribution of modified nano-SiO2 to particle packing and filter-cake continuity, improve filtration control. These results demonstrate the potential of SiO2@P-DAS as a nanocomposite gel fluid-loss reducer for high-temperature and salt-contaminated water-based drilling fluids.

PMID 42929929
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PubMedGels (Basel, Switzerland)2026-10-26

Research Progress of Polyacrylamide Gels for Oilfield Applications: A Systematic Review.

Dong Ruiqiang R, Chen Guanyu G, Li Daoyong D, Cui Xinyue X et al.

In the middle-to-late stage of reservoir development, widespread high-permeability channeling exacerbates ineffective water circulation and impairs crude oil recovery. This work explores polyacrylamide (PAM) gels intended for oilfield profile control and water shut-off. It comprehensively compares gelation behaviors and performance metrics of diverse cross-linking and modification strategies, and pinpoints critical unresolved research gaps. Four representative PAM-gel systems are analyzed in detail, including organic-crosslinked, metal-crosslinked, nano-composite-modified, and delayed-crosslinker formulations. The results show that polyethyleneimine (PEI) cross-linked gels achieve a storage modulus of 780 kPa at 110 °C, which is superior to the conventional hydroquinone-hexamethylenetetramine (HQ-HMTA) system. Metal-crosslinked gels are prone to syneresis and structural instability above 70 °C. Nanocomposite modification significantly enhances gel comprehensive properties: nano-silica improves thermal resistance to 155.5 °C; modified nano-graphite doubles storage modulus (G'), shortens gelation time by half, and maintains 76.5% of initial modulus after 60-day aging at 130 °C; TOCN-reinforced gels preserve structural integrity under high-salinity environments at 140 °C for 108 h. Delayed-release cross-linkers can extend gelation time up to 17 days to meet the demands of deep in situ profile control. Furthermore, the emerging data-driven paradigm of artificial-intelligence-assisted gel optimization is also reviewed, together with its current limitations. Future research priorities cover intelligent responsive gel materials, environmentally benign cross-linkers, and unified evaluation specifications for heterogeneous reservoirs. This paper reviews over 100 core publications from 2000 to 2026 based on the Web of Science and Engineering Village databases. Different from existing studies, this work emphasizes the molecular crosslinker mechanisms, nanomodification reinforcement, and field performance variations of PAM gel systems, and concludes the major technical bottlenecks for their application in harsh reservoirs. Meanwhile, it quantitatively compares the performance of modified PAM gel formulations and clarifies the applicable temperature ranges of different crosslinker schemes, providing technical references for the development of PAM plugging agents for complex oil reservoirs.

PMID 42929937
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PubMedGels (Basel, Switzerland)2026-10-26

Recent Advances in Novel Adsorbents Prepared by the Sol-Gel Method for the Removal of Uranium and Strontium from Radioactive Wastewater: A Review.

Jiang Jiayi J, Zhao Jiaxue J, Chen Miaoling M, Chen Diyun D et al.

Uranium- and strontium-containing wastewater from nuclear industries poses a threat to the environment and human health. The sol-gel method, with its tunable composition and synthetic flexibility, is widely used to fabricate novel and high-performance adsorbents. This review covers recent progress in the sol-gel fabrication of UO22+ and Sr2+ adsorbents, including both inorganic and organic-inorganic hybrid materials. Reported adsorption capacities typically range from about 40 to 670 mg/g for UO22+ and from about 40 to 370 mg/g for Sr2+, with a few systems achieving even higher values under optimized conditions. Titanates and titanosilicates exhibit outstanding selectivity toward Sr2+, whereas phosphate-based materials and amidoxime-functionalized hybrids show strong affinity for UO22+. However, practical application is still hampered by high precursor costs, poor shapeability, limited long-term stability, harsh regeneration conditions, and interference from coexisting ions. Future efforts should focus on low-cost materials and shaping processes to promote the engineering applications of tailored materials via the sol-gel method.

PMID 42929925
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PubMedGels (Basel, Switzerland)2026-10-26

Preparation of a Lotus-Leaf-Inspired PVA-Grape Seed Extract Biomimetic Gel Film and Its Application in Active Packaging for the Postharvest Preservation of Agaricus bisporus.

Wang Liyan L, Sun Lingyu L, Zhang Yixuan Y, Cong Mengdi M et al.

This study reports the fabrication of a biomimetic PVA-GSE film featuring a lotus-leaf-like hierarchical micro/nanostructure, and its application as a gel-based active packaging material for the post-harvest preservation of Agaricus bisporus (A. bisporus). A lotus-leaf negative template was prepared using soft etching and a polydimethylsiloxane (PDMS) secondary transfer method; the PVA/GSE solution was then cast onto this template and subjected to repeated freeze-thaw cycles for physical cross-linking to induce PVA hydrogelation. The resulting biomimetic gel film reproduces the hierarchical lotus-leaf surface morphology and forms a continuous polymer gel network composed of interconnected gel pores, which serve as reservoirs for grape seed extract (GSE). This gel network structure enhances the properties of PVA. Although BPG-40 exhibited the strongest preservation performance during storage owing to its highest GSE loading, BPG-30 was selected as the optimal formulation, because it achieved the best overall balance of mechanical strength, water-vapour barrier and optical quality while retaining 91-93% of the BPG-40 antioxidant and antibacterial activity; beyond 30% loading, the marginal gains in bioactivity were outweighed by a 12.6% decrease in tensile strength, severe colour darkening (L* = 6.07) and surface cracks observed by SEM. An experiment was conducted to evaluate the effects of the biomimetic composite film on A. bisporus over a 12 days storage period at 4 °C. Storage results demonstrate that this film effectively reduces the weight loss rate of A. bisporus, lowers their respiration rate, enhances the polyphenol retention rate, and significantly extends the storage life of A. bisporus. This study simulates the surface structural regulation mechanism of lotus leaves and represents an innovative approach that synergistically integrates active ingredients with material structure for use in fresh-keeping packaging materials.

PMID 42929915
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