Roche · FKBP1A
tacrolimus 是一种治疗药物，由Roche研发。该药已获批，用于治疗相关适应症，给药途径：Topical。
| 商品名 | Protopic, tacrolimus, topical, M 1151C2 |
| 公司 | Roche |
| 分子靶点 | FKBP1A |
| 给药途径 | Topical |
| 状态 | Approved |
tacrolimus 作用于 1 个分子靶点：
| FKBP1A | FKBP prolyl isomerase 1A (FKBP-12, FKBP12) |
tacrolimus 针对 3 个适应症，涉及 1 个治疗领域。
| 治疗领域 | 疾病/病症 | 分期 |
|---|---|---|
| Skin and subcutaneous tissue disorders | Dermatitis allergic | ✓ Approved |
| Skin and subcutaneous tissue disorders | Dermatitis atopic | ✓ Approved |
| Skin and subcutaneous tissue disorders | Psoriasis | Phase II |
Oualid D D, Lheure C C, Louchez A A, Tancrede-Bohin E E et al.
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.
Mamizadeh Hamed H, Herizchi Ghadim Hamideh H, Pourasghary Sajjad S
To evaluate whether adding topical 5% caffeine to fluocinolone acetonide 0.025% cream (FAC) improves short-term clinical outcomes compared with FAC alone in patients with chronic plaque psoriasis. This randomized, parallel-group, masked, active-controlled clinical trial included 40 patients with chronic plaque psoriasis treated at the dermatology outpatient clinic of Sina Hospital, Tabriz, Iran. Participants were randomly allocated in a 1:1 ratio to receive either topical 5% caffeine plus fluocinolone acetonide 0.025% (intervention group, n=20) or topical fluocinolone acetonide 0.025% alone (control group, n=20). Psoriasis severity was assessed using the Psoriasis Area and Severity Index (PASI) at baseline and weekly for four weeks. Treatment response and adverse events were also recorded. Baseline PASI scores were comparable between the intervention and control groups (3.41 ± 1.86 vs 3.79 ± 1.51, respectively; P=0.484). PASI scores were significantly lower in the intervention group at each post-treatment assessment. At week 4, mean PASI was 0.39 ± 0.17 in the intervention group and 2.29 ± 1.31 in the control group (P=0.001). The mean reduction from baseline to week 4 was 3.01 ± 1.48 with 5% caffeine plus FAC and 1.49 ± 1.01 with FAC alone (P<0.001). Complete clearance, defined as PASI=0, occurred in 14 of 20 patients (70%) in the intervention group compared with 1 of 20 (5%) in the control group (P=0.001). No adverse events were reported during the study. Adding topical 5% caffeine to FAC produced a greater short-term reduction in psoriasis severity than FAC alone. No adverse events were reported during the 4-week treatment period. Larger randomized trials with longer follow-up are warranted to confirm efficacy and characterize longer-term tolerability. Iranian Registry of Clinical Trials (IRCT), IRCT20091012002581N10, registered on October 28, 2023; https://irct.ir/trial/73367.
Brūvere Diāna D, Bārzdiņa Ance A, Broks Renārs R, Koka Rudīte R et al.
Blackcurrant (Ribes nigrum) is rich in polyphenols and is known for its antioxidant and anti-inflammatory properties, yet its processing byproducts (pomace) remain underutilized. This study aimed to develop and characterize R. nigrum pomace extract-loaded alginate-inulin hydrogel for potential topical application, thus promoting the valorization of R. nigrum pomace extract. Comparative extract analysis demonstrated that the pomace extract contained the highest levels of total polyphenols (71.0 mg GAE/g dried extract) and tannins (21.8%) and exhibited the most promising antibacterial activity (MIC 3.1-6.3 mg/mL), although its antiradical activity was relatively lower than that of juice and berry extracts. Furthermore, the obtained hydrogels were structurally stable and provided a gradual release of polyphenols at pH 5.5, with 80% released within 24 h. Incorporation of R. nigrum pomace extract increased the swelling of the hydrogels and improved viscoelastic recovery. Overall, the findings highlight the potential of R. nigrum pomace as a sustainable bioactive component in alginate-inulin hydrogel systems for potential topical applications in wound care.
Lee Seung-Min SM, Cha Sangryul S, Jeon DooLee D, Choi Wooseok W et al.
Acute ultraviolet B (UVB) exposure induces epidermal hyperplasia, pigmentation-related responses, and early extracellular matrix remodeling. Topical tyrosinase inhibitors, including arbutin and kojic acid, can have limited residence on damaged skin. Here, we evaluated a skin-conformal composite patch comprising aligned polyurethane nanofiber membranes integrated with methacrylated hyaluronic acid (MHA) hydrogel arrays loaded with arbutin or kojic acid. Seven-week-old Hairless Mouse, Strain 2 (HRM2) mice were assigned to six groups: control (CTL), UVB only (UV), UVB plus topical arbutin (UVA), UVB plus topical kojic acid (UVK), UVB plus arbutin-loaded MHA patch (UV-A-MHA), and UVB plus kojic acid-loaded MHA patch (UV-K-MHA). Dorsal skin received a single UVB dose (200 mJ/cm2), was treated immediately, and was analyzed on Day 4. Drug-loaded MHA patch treatment attenuated UVB-induced epidermal thickening and was associated with qualitative differences in dermal matrix organization, while direct comparisons with the corresponding freely applied formulations varied across endpoints. These histological findings were evaluated using hematoxylin and eosin, Masson's trichrome, Picro-Sirius Red, and Fontana-Masson staining. GFP-loaded MHA hydrogels remained detectable in the epidermis and upper dermis through Day 4, supporting local cargo retention under skin-contact conditions. Preliminary HPLC-UV analysis detected arbutin and kojic acid parent peaks in MHA formulations before and after 60 s of UV exposure. Patch treatment was associated with significant reductions in α-smooth muscle actin and vimentin, whereas effects on SMAD phosphorylation differed between the two drug formulations, without detectable changes in body weight or serum TNF-α and IL-6. Because the main experiment lacked drug-free MHA patch and bandage-only controls, scaffold-, occlusion-, and drug-specific effects could not be fully separated. These findings support aligned nanofiber-supported MHA hydrogel arrays as functional biomaterial patches for localized cutaneous delivery and modulation of acute UVB-induced remodeling-associated responses.
Andresen Amalie Kjær AK, Gaertner Emilia E, Hong Lin Marie Karen Tracy MKT, Moser Claus C et al.
Chronic wound infections are frequently associated with bacterial biofilms, which significantly reduce the efficacy of antimicrobial treatments. Conventional in vitro evaluation methods, such as disc diffusion assays and static biofilm models, lack physiological relevance, whereas more advanced wound models are often costly, complex, and difficult to reproduce. In this study, we present a cost-effective and easily applicable in vitro wound model based on gelatin-alginate hydrogels for the evaluation of topical antimicrobial therapies. Hydrogels composed of gelatin type A and sodium alginate were integrated into a transwell system and crosslinked using microbial transglutaminase and calcium ions. This configuration enables passive diffusion of simulated wound fluid from the basolateral compartment, thereby mimicking key aspects of the wound environment. The model supports the growth of Pseudomonas aeruginosa biofilms within a three-dimensional matrix. The hydrogel system supported bacterial growth and microcolony formation during 48 h of incubation at 37 °C. The system was applied in both biofilm inhibition and eradication studies using tobramycin, ε-poly-L-Lysine and the commercially available wound gel Prontosan®. Viable bacteria were quantitatively recovered through hydrogel dissolution followed by serial dilution and count of colony-forming units. Overall, the developed model provides a simple and accessible platform for quantitative evaluation of antibiofilm treatments. While not intended to fully replicate the complexity of native tissue, this system offers a practical alternative to collagen-based models and helps bridge the gap between conventional in vitro assays and more advanced wound models.
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