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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
来源： ClinicalTrials.gov, Merck KGaA

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

PubMedFrontiers in nutrition2026-09-10

Preparation, characterization, stability, and application in curcumin of the emulsion gels stabilized with coconut cake albumin modified by ultrasonication and carboxymethylation.

Yang Yong Y, Gong Meiling M, Duan Jiapeng J

Curcumin has applications in food and medical industries, but its stability and bioaccessibility are poor. Coconut cake albumin (CCA) has potential as a component of the curcumin-loading system; however, relative data are scare. Herein, emulsion gels were formed using coconut cake albumin modified by ultrasonication and carboxymethylation (CCA-UC) in this study. The results evidenced that ultrasonication and carboxymethylation increased the emulsifying capacity (from 67.51 to 143.65 m2/g) and emulsion stability (from 70.37 to 87.18%) of CCA by improving its solubility and interface sorption capacity, enhancing the zeta potential, and reducing droplets' size (p < 0.05). CCA and CCA-UC formed compact emulsion gel when concentration was more than 10 g/100 g. Compared with the CCA-emulsion gel, CCA-UC-emulsion gel had more compact and denser gel structure, higher crystallinity (38.65%), bound water content and viscosity, and lower energy storage (G'), loss modulus (G"), and loss factor. Furthermore, CCA-UC-emulsion gel showed superior thermal and oxidative stability, and higher chewiness (35.83 g), springiness (0.90), hardness (67.44 g), and cohesiveness (0.85) than CCA-emulsion gel. Additionally, CCA-UC-emulsion gel exhibited superior intestinal digestion rate, higher curcumin encapsulation (89.64%) and loading efficiency (204.01 μg/g), better photostability, and superior bioaccessibility (49.08%). However, more specific mechanisms should be investigated in the further work. These findings revealed that ultrasonication assisted with carboxymethylation was an effective way to improve the emulsion gel properties of CCA and increase the bioaccessibility of curcumin. However, more specific mechanisms should be investigated in the further work.

PMID 42718976
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PubMedAdvanced healthcare materials2026-09-10

Water-Activated Phospholipid Phase-Separation Gel as an Immunomodulatory Anti-Adhesion Barrier for Postoperative Adhesion Prevention.

Lee Jong-Ju JJ, Sung Yulseung Y, Kim Yeji Y, Yang Heesang H et al.

Postoperative adhesions remain a major complication after abdominal surgery, and current polymeric barriers often show limited tissue retention and biocompatibility. Here, we establish a water-activated phospholipid barrier strategy for postoperative adhesion prevention by converting a depot-forming phospholipid phase-separation gel (PPSG) into a gram-scale surgical barrier. In this study, solvent identity acts as a functional design determinant rather than a passive solubilizer, governing hydration-triggered gel reinforcement, intraperitoneal residence, and tolerability. Replacing ethanol with propylene glycol strengthened the gel matrix, improved barrier activation, and enabled gram-scale administration without hepatic toxicity associated with ethanol-based PPSG. Mechanistically, the structured phospholipid barrier retained gel-state immunomodulatory activity, attenuating macrophage-driven inflammatory responses and suppressing NF-κB-associated signaling. In a rat peritoneal-cecum abrasion model, propylene glycol-based PPSG completely prevented macroscopic adhesions. Together, these findings establish a water-activated phospholipid barrier platform for converting depot-forming phospholipid systems into active surgical barriers that combine durable physical separation with local immunomodulation.

PMID 42717399
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PubMedAAPS PharmSciTech2026-09-10

Ethosomal Gel-Based Topical Delivery of Albendazole Hydrochloride for Psoriasis: In Vitro and In Vivo Evaluation.

Rençber Seda S, Karpuz Merve M, Ünlü Çakıcı Büşra B, Karayıldırım Çinel Köksal ÇK et al.

This study aimed to develop an albendazole hydrochloride (ALB)-loaded ethosomal gel for topical psoriasis treatment. ALB-loaded ethosomes were prepared and characterized to select the optimal formulation, which was subsequently incorporated into an HPMC-based hydrogel. The ethosomal gel was evaluated through physicochemical, in vitro and in vivo studies. The optimized ethosomal formulation prepared by the film hydration method exhibited a mean vesicle size of 490.00 ± 0.14 nm, polydispersity index of 0.31 ± 0.14, zeta potential of -22.85 ± 2.28 mV and encapsulation efficiency of 23.90 ± 1.43%. After incorporation into the hydrogel matrix, the Gel4-E3/ALB formulation demonstrated appropriate mechanical properties (hardness 8.42 ± 0.70 mN, adhesiveness - 16.85 ± 1.50 mN·s, elasticity 0.89 ± 0.07, cohesiveness 1.14 ± 0.09) and shear-thinning behavior, ensuring ease of application and skin retention. A controlled release pattern was observed, consistent with the controlled-release behavior expected from ethosomal hydrogel systems. Radiolabeling studies demonstrated high labeling efficiency (> 95%). In vitro cytotoxicity evaluation indicated that the optimized ethosomal gel formulation was non-toxic. In vivo studies performed in an imiquimod (IMQ)-induced psoriatic mouse model revealed significant therapeutic improvement in the Gel4-E3/ALB-treated group compared with the IMQ control, with visible reduction in erythema, scaling, and skin thickening after the fifth day of treatment. Hematological analysis showed no adverse effects associated with the formulation. Histopathological evaluation confirmed the reduction in epidermal hyperplasia and inflammatory cell infiltration in the treated group. The developed ALB-loaded ethosomal gel represents a safe and promising topical therapeutic system for psoriasis management.

PMID 42717176
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PubMedVascular health and risk management2026-09-10

Short-Term Efficacy and Safety of Topical Sirolimus Gel in Pediatric Superficial Microcystic Lymphatic Malformations: A Single-Center Interventional Study of 30 Patients.

Xu Weiyang W, Ding Yu Y, Zhao Lei L, Pi Mengqi M et al.

To evaluate the efficacy and safety of 0.2% topical sirolimus gel for pediatric superficial microcystic lymphatic malformations (LMs). This single-center interventional study included 30 pediatric patients (14 males and 16 females; aged 2-15 years) with superficial microcystic lymphatic malformations. All patients received 0.2% topical sirolimus gel twice daily for 12 weeks according to a predefined treatment and follow-up protocol. Clinical efficacy was assessed at baseline and week 12 using clinical examination, standardized photography, symptom scores, and available imaging findings, together with a four-grade physician-assessed response scale. Adverse events were monitored throughout treatment, and blood sirolimus concentrations were measured at weeks 4 and 12. All patients showed lesion reduction, with an overall response rate of 96% (29/30). At week 12, efficacy was graded as IV in 10 patients, III in 11, II in 8, and I in 1. Among patients with pain symptoms, pain scores decreased significantly after treatment (2.88 ± 0.78 vs 1.18 ± 0.88; P < 0.05). In 10 patients with measurable lesions, maximum lesion diameter decreased significantly from 3.22 ± 1.36 cm to 1.89 ± 1.33 cm (P < 0.05). Only mild local adverse effects were observed, and blood sirolimus concentrations remained below 2.0 ng/mL in all patients. Topical sirolimus gel demonstrated favorable efficacy and safety for pediatric superficial microcystic LMs.

PMID 42718634
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PubMedAAPS PharmSciTech2026-09-10

From Liquid to Gel: Multifunctional Stimuli-responsive Polymers for Targeted Oral Drug Delivery.

Mishra Manoj Kumar MK, Shukla Divaker D, Sharma Shalini S, Sharma Jyoti Nanda JN et al.

Oral drug delivery is the delivery method of choice, as it is non-invasive and patients will comply with the delivery method, but many contemporary therapeutics, such as poorly soluble, permeable, and unstable drugs, fail because of rapid gastrointestinal absorption, enzyme degradation, and non-targetability. The in-situ gelling systems are now considered paradigms that no longer exist as liquids; instead, they form a depot in the gastrointestinal tract and transform into a gel in response to physiological signals such as pH, ions, or enzymes. This review will discuss how these so-called smart polymers have developed over the years, starting as simple gel-forming systems and evolving into the multifunctional platforms that are also designed to have a pointed and sustained action. Next generation in situ gels combine bioadhesion, permeation enhancement, and active targeting ligands to overcome sequential barriers to delivery transit, permeability, stability, and cellular uptake. We critically assess the chemistry, mechanisms, formulation strategies, and therapeutic use of these systems, including gastro-retention and localized therapy, as well as oral delivery of biologics. Despite encouraging preclinical results, we touch on translational issues of scalability, manufacturing, and regulatory pathways. Multifunctional stimuli-responsive polymers, which actively traverse the gastrointestinal environment, are the future of oral drug delivery because they provide precision, bioavailability, and improved patient outcomes.

PMID 42717126
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PubMedAnnals of translational medicine2026-09-10

A comprehensive longitudinal study quantifying the systemic effects associated with ovariectomy and high-dose corticosteroids in a sheep model of osteoporosis.

Bisazza Katie T KT, Nelson Brad B BB, Anthony Russell V RV, Goodrich Laurie R LR et al.

The sheep is a common preclinical model for osteoporosis in humans and allows for robust longitudinal studies. Appropriate characterization of large animal models is necessary prior to selection for preclinical studies. We sought to comprehensively characterize the process of bone loss in a 12-month sheep model of osteoporosis, and report on the sheep clinical pathologies throughout osteoporosis model development. We induced osteoporotic bone loss in 10 sheep via ovariectomy and corticosteroid administration. Over a 12-month period, we performed serial bone density scanning, bone biopsy for microarchitecture and histomorphometry assessment, clinical assessments, and evaluated systemic levels of steroid hormones, as well as hematological and biochemical values. Statistical analysis was performed to compare the outcomes of osteoporotic sheep to healthy age-matched control sheep over time. We successfully induced osteoporotic-like bone loss in the experimental group by observing decreased bone density in the lumbar spine and tibia by 6 months, including changes to bone microarchitecture (i.e., trabecular thinning, decreasing bone volume) and histomorphometry (i.e., decreased trabecular bone ratio) indicative of bone remodeling disruption. We also reported comprehensive systemic changes in the same animals over time. Compared to control animals, we observed a significant disruption to clinical pathology parameters and steroid hormone production in osteoporotic sheep. Osteoporotic model development induced hematological and serological disruptions at 3 months, including neutrophilia, immune cell suppression, electrolyte and protein imbalances, hyperphosphatemia, and elevated liver enzymes. Additionally, administration of corticosteroids appeared to suppress cortisol production over the course of model development, followed by a surge of endogenous cortisol following cessation of corticosteroid treatment. Estradiol surprisingly did not drop to significantly lower levels than controls for the duration of the experiment, suggesting that there are extragonadal sources of estradiol production or dietary sources of phytoestrogens in the sheep differing from humans. Bone loss was induced in sheep within 3-6 months, and the most significant systemic disruptions appear to correlate with timing of high-dose corticosteroids. These findings offer a detailed characterization of the sheep model of osteoporosis, enabling investigators to distinguish the effects of treatment administration from those arising solely from model development.

PMID 42718873
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