Drug Database
FL

flurbiprofen (Yakuban Tape)

✓ Approved

Kaken Pharmaceutical · PTGS1 · Small Molecule

What is flurbiprofen?

flurbiprofen is a small molecule developed by Kaken Pharmaceutical. It is approved for therapeutic indications via transdermal.

Drug Profile

Brand NamesYakuban Tape
CompanyKaken Pharmaceutical
Drug ClassSmall Molecule
Molecular TargetPTGS1, PTGS2
RouteTransdermal
StatusApproved

Mechanism of Action

Molecular Targets

flurbiprofen acts on 2 molecular targets:

PTGS1prostaglandin-endoperoxide synthase 1 (COX3, PCOX1)
PTGS2prostaglandin-endoperoxide synthase 2 (GRIPGHS, hCox-2)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

flurbiprofen is developed for 5 unique indications across 3 therapeutic areas.

Therapeutic AreaConditionPhase
Gastrointestinal disordersAbdominal pain✓ Approved
Injury, poisoning and procedural complicationsEpicondylitis✓ Approved
Musculoskeletal and connective tissue disordersMusculoskeletal pain✓ Approved
Musculoskeletal and connective tissue disordersOsteoarthritis✓ Approved
Musculoskeletal and connective tissue disordersTendonitis✓ Approved

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Park Chaeheon C, Lee Seungchan S, Jung Seung Oh SO, Lee Yujin Y et al.

Despite its potent anti-aging efficacy, the practical application of retinol (ROH) remains highly restricted by its poor photostability, low aqueous solubility, and concentration-dependent cytotoxicity. Herein, we report the synthesis of a hyaluronic acid-retinol (HA-ROH) conjugate to overcome these limitations and improve transdermal delivery. The successful conjugation was confirmed via proton nuclear magnetic resonance (1H NMR) spectroscopy, high-performance liquid chromatography (HPLC) and Fourier-transform infrared spectroscopy (FT-IR). Notably, the HA-ROH conjugate exhibited remarkable photostability under UVA irradiation compared to free retinol. HA-ROH presented a sustained, hyaluronidase-responsive ROH release profile, indicating its potential as an enzyme-responsive controlled delivery system. Furthermore, the conjugation significantly mitigated the cytotoxicity of retinol in both HaCaT keratinocytes and human dermal fibroblasts. The conjugate suppressed matrix metalloproteinase-1 (MMP-1) expression more effectively than free ROH. In vitro cellular uptake and ex vivo skin permeation studies demonstrated enhanced transdermal delivery of the HA-ROH conjugate. Taken together, these results suggest that the HA-ROH conjugate is a highly promising, stable, and safe candidate for advanced dermatologic and cosmetic applications.

PubMedJournal of nanobiotechnology2026-10-21

A programmable nanoplatform for inflammatory-state reprogramming in psoriasis treatment.

Chen Zhihua Z, Zhao Jinyu J, Huang Shiqi S, Lou Ge G et al.

Psoriasis is a chronic, immune-mediated inflammatory skin disease. Although current treatments alleviate symptoms, they primarily focus on inflammation suppression through single-target approaches, which fail to comprehensively address the complex pathological imbalances. To overcome this limitation, we developed a programmable delivery system based on a nanocomposite material composed of Tannic acid (TA), Cerium (Ce), and Luteolin (Lut), integrated into an in situ gelling hydrogel platform (TA-Ce-Lut-Gel), enabling multi-dimensional treatment strategy for psoriasis by precisely modulating oxidative stress, immune responses, and skin microbiota. The TA-Ce-Lut metal-polyphenol nanoparticles, constructed through coordination bonds, exhibited a size of 177.30 ± 0.55 nm and high encapsulation efficiency of 72.89 ± 5.32%. Upon incorporation into the hydrogel, this system provided a localized and sustained drug depot. In an imiquimod-induced mouse model of psoriasis (both ear and back), TA-Ce-Lut-Gel significantly reduced skin inflammation, improved skin thickness, erythema, and scaling, showing superior efficacy compared to traditional anti-inflammatory treatments. This system alleviated ROS levels, regulated macrophage M2 polarization, and reshaped the immune response, while also modulating the TRAF6/NF-κB/STAT3 signaling pathway to significantly inhibit pro-inflammatory cytokine secretion. Additionally, combined with NIR irradiation, TA-Ce-Lut-Gel enhanced transdermal drug delivery and antioxidant activity, further enhancing therapeutic effects and promoting skin microbiota recovery. This study presents an effective platform for localized precise treatment of psoriasis, overcoming the limitations of traditional single-target anti-inflammatory therapies and offering a potential strategy for the treatment of other immune-mediated diseases, with broad clinical application prospects.

PubMedBioImpacts : BI2026-10-20

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Kavathekar Prajakta Kirankumar PK, Pawar Pravin K PK

Recent advances in nanotechnology have positioned solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) as promising platforms for dermal and transdermal drug delivery. This review critically highlights emerging breakthroughs that go beyond the conventional advantages of lipid nanoparticles. SLNs, composed of physiologically compatible solid lipids, provide improved drug stability and controlled release; however, their clinical utility is often constrained by limited drug loading, drug expulsion during storage, and highly ordered crystalline structures. To overcome these drawbacks, second-generation NLCs incorporate both solid and liquid lipids, creating an imperfect lipid matrix that significantly enhances loading capacity, minimizes drug leakage, and enables tunable release kinetics. Recent formulation innovations including precision high-pressure homogenization, microfluidic-assisted production, and optimized hot/cold homogenization approaches have enabled tighter particle size control, improved batch reproducibility, and better long-term stability. In parallel, surface engineering strategies such as ligand functionalization, polymer coating, and incorporation of natural bioactives have demonstrated enhanced skin targeting, deeper stratum corneum penetration, and prolonged dermal retention. Notably, recent preclinical and translational studies report improved therapeutic outcomes in acne, psoriasis, fungal infections, inflammatory disorders, wound healing, hyperpigmentation, and melanoma-related skin conditions when compared with conventional topical systems. Despite these advances, important translational gaps remain, including large-scale manufacturing challenges, regulatory uncertainties, and limited clinical validation. By integrating recent technological breakthroughs with application-focused evidence, this review provides a forward-looking perspective on the evolving role of SLNs and NLCs as next-generation lipid nanocarriers for dermatological therapy and advanced skin care.

PubMedACS biomaterials science & engineering2026-10-20

Potentiated Skin Permeation and Antitumor Efficacy of Fulvestrant-Loaded High-Permeation Vesicles for Localized Breast Cancer Treatment.

Akhtar Junia J, Saren Brojendra Nath BN, Yadav Vivek V, Bhardwaj Smriti S et al.

Fulvestrant (FLV) is a selective estrogen receptor degrader used for hormone receptor-positive breast cancer. Nevertheless, its delivery is limited by low aqueous solubility and repeated intramuscular administration. Considering these drawbacks, a high-permeation vesicle-in-gel system (HPV-gel) was explored as a localized transdermal approach for FLV and evaluated for its physicochemical, permeation, cellular, pharmacokinetic, antitumor, and safety performance. Accordingly, FLV/HPVs were prepared using soya phosphatidylcholine and a ternary permeation-enhancer combination of sodium oleate (SO), diethylene glycol monoethyl ether (DEGEE), and propylene glycol (PG). Enhancer proportions were optimized using a D-optimal mixture design based on vesicle size, PDI, and entrapment efficiency. The optimized composition contained 80% phospholipid and 20% of a permeation enhancer mixture, comprising SO, DEGEE, and PG in a ratio of 6:1.5:2.5. FLV/HPVs showed a particle size of 94.02 ± 1.10 nm, a PDI of 0.241 ± 0.029, a zeta potential of -38.6 ± 1.2 mV, an entrapment efficiency of 85.79 ± 3.72%, a practical drug loading of 8.58 ± 0.16%, and a deformability index of 1.62 ± 0.08. The optimized vesicles were incorporated into a 1.5% w/v Carbopol 934P gel and compared with FLV-gel and FLV/Lipo-gel with the same gel base and an equivalent FLV amount. FLV/HPVs-gel showed sustained drug release and increased FLV permeation by nearly 8-fold and 3-fold compared with FLV-gel and FLV/Lipo-gel, respectively, with higher intradermal retention and deeper dermal distribution. Following topical administration, FLV/HPVs-gel increased Cmax by ∼8.3- and ∼2-fold and AUC0-168 h by ∼8.1- and ∼2.6-fold compared with FLV-gel and FLV/Lipo-gel, respectively, while showing plasma concentration-time profile closer to FLV (i.m.). In 4T1 tumor-bearing mice, FLV/HPVs-gel showed the strongest tumor-suppressive effect, accompanied by greater intratumoral penetration, while biochemical parameters, major organ histology, TEWL, and skin histology indicated acceptable systemic and local safety. Overall, FLV/HPVs-gel improved skin permeation, drug exposure, and antitumor activity, suggesting its potential as a noninvasive transdermal approach for FLV in breast cancer therapy.

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Testosterone, widely known as the male hormone, is also produced naturally in women and plays an important role throughout their lifespan. There has been a growing use of testosterone for a range of symptoms in menopausal women, including low sexual desire, low mood, fatigue, poor memory, and heart and bone health. This review brings together the current evidence and guidelines on testosterone as part of hormone replacement therapy (HRT) in menopausal women, including its impact on reproductive and non-reproductive tissues; when it is indicated to be prescribed and in what forms; safety and gaps in existing evidence. We found that there is high-quality evidence to support the use of testosterone for low sexual desire where conventional HRT has not helped. Transdermal preparations are recommended with no serious side effects at testosterone levels normally found in women. There is insufficient evidence to support its use for brain, heart and bone health. This represents an area of focus for future research.

PubMedBioImpacts : BI2026-10-20

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Skin cancer is one of the most prevalent malignancies worldwide, with incidence increasing by approximately 2-3% annually due to prolonged ultraviolet radiation exposure, genetic predisposition, and an ageing population. Conventional treatments, including oral, injectable, and topical therapies, are often limited by poor skin permeability, first-pass metabolism, systemic toxicity, and inadequate tumor targeting. This review systematically examines ethosomal drug delivery systems, focusing on their composition, mechanism of skin permeation, and formulation strategies. Key aspects such as phospholipid composition, ethanol concentration (20-45% w/w), preparation techniques, and interaction with tumor-altered skin barriers are critically analyzed. Ethosomes, as deformable lipid vesicles, enhance transdermal drug delivery by fluidizing stratum corneum lipid lamellae, enabling deeper dermal penetration. Studies demonstrate improved drug localization, controlled release, and enhanced therapeutic efficacy in various skin cancers, including melanoma, basal cell carcinoma, and squamous cell carcinoma. Applications in chemotherapy, photodynamic therapy, and immunotherapy show promising preclinical outcomes. Despite significant advancements and encouraging preclinical results, challenges such as formulation stability, scalability, regulatory considerations, and long-term safety must be addressed before ethosomal systems can achieve successful clinical translation in skin cancer therapy.

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