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Industry Update, May 2024. 行业最新情况,2024 年 5 月。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-08-08 DOI: 10.1080/20415990.2024.2383162
Elaine Harris
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引用次数: 0
Development and optimization of guaifenesin sustained release mini-tablets for adult and geriatric patients. 开发和优化用于成人和老年患者的愈创木酚缓释小药片。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-10-03 DOI: 10.1080/20415990.2024.2406216
Mahshid Samadi, Mitra Jelvehgari, Sara Salatin

Aim: The main aim of this study was to formulate and optimize sustained release mini-tablets of guaifenesin.Materials & methods: Guaifenesin granules were successfully prepared using different blend ratios of carnauba wax to drug by melt granulation method. The properties of granules were further modified by combining them with ethyl cellulose. The obtained granules were then mixed and compressed into mini-tablets using a tablet press machine. The resulting mini-tablets were characterized in terms of weight, thickness, hardness, drug content and in vitro drug release.Results: Mini-tablets with 1:6 carnauba wax to drug ratio showed superior physicochemical characteristics, releasing about 100.03% of guaifenesin over 8 h. Ethyl cellulose offers a great potential to accurately control drug release from mini-tablets.Conclusion: The prepared mini-tablets seem to be a very promising alternative to guaifenesin conventional formulations and can be used in adults and elderly people.

目的:本研究的主要目的是配制和优化愈创甘油醚缓释小药片:采用不同的棕榈蜡与药物混合比例,通过熔融造粒法成功制备了愈创木酚颗粒。通过与乙基纤维素结合,进一步改变了颗粒剂的性质。然后将得到的颗粒混合并用压片机压制成小药片。对所得迷你药片的重量、厚度、硬度、药物含量和体外药物释放进行了表征:结果:棕榈蜡与药物比例为 1:6 的迷你药片显示出优异的理化特性,在 8 小时内释放了约 100.03% 的愈创木酚:所制备的迷你片剂似乎是一种非常有前景的瓜奈酚传统制剂替代品,可用于成人和老年人。
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引用次数: 0
Industry updates in the field of therapeutic delivery in June 2024. 2024 年 6 月治疗给药领域的行业动态。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-10-11 DOI: 10.1080/20415990.2024.2408214
Mengistie Diress, Armin Mooranian, Hani Al-Salami
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引用次数: 0
Nanotechnology-assisted combination drug delivery: a progressive approach for the treatment of acute myeloid leukemia. 纳米技术辅助联合给药:治疗急性髓性白血病的渐进方法。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-09-13 DOI: 10.1080/20415990.2024.2394012
Neelam Poonia, Nikita Vijay Jadhav, Davuluri Mamatha, Manoj Garg, Atul Kabra, Amit Bhatia, Shreesh Ojha, Viney Lather, Deepti Pandita

Acute myeloid leukemia (AML), a heterogeneous hematopoietic cancer prevalent in adults, has been a leading cause of leukemia-associated deaths for decades. Despite advancements in understanding its pathology and pharmacological targets, therapeutic strategies have seen minimal change. The standard treatment, combining cytarabine and anthracycline, has persisted, accompanied by challenges such as pharmacokinetic issues and non-specific drug delivery, leading to severe side effects. Nanotechnology offers a promising solution through combination drug delivery. FDA-approved CPX351 (VYXEOS™) a liposomal formulation delivering doxorubicin and cytarabine, exemplifies enhanced therapeutic efficacy. Ongoing research explores various nanocarriers for delivering multiple bioactives, addressing drug targeting, pharmacokinetics and chemoresistance. This review highlights nanotechnology-based combination therapies for the effective management of AML, presenting a potential breakthrough in leukemia.

急性髓性白血病(AML)是一种多发于成人的异质性造血癌症,几十年来一直是白血病相关死亡的主要原因。尽管人们对其病理和药理靶点的认识不断进步,但治疗策略的改变却微乎其微。将阿糖胞苷和蒽环类药物结合使用的标准治疗方法一直沿用至今,但却面临着药代动力学问题和非特异性给药等挑战,导致严重的副作用。纳米技术通过联合给药提供了一种前景广阔的解决方案。美国食品和药物管理局批准的 CPX351(VYXEOS™)是一种可递送多柔比星和阿糖胞苷的脂质体制剂,是提高疗效的典范。目前正在进行的研究探索了多种纳米载体,用于递送多种生物活性物质,解决药物靶向、药代动力学和化疗耐药性等问题。本综述重点介绍了有效治疗急性髓细胞性白血病的纳米技术联合疗法,为白血病领域带来了潜在的突破。
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引用次数: 0
Therapeutic delivery of siRNA for the management of breast cancer and triple-negative breast cancer. 将 siRNA 用于治疗乳腺癌和三阴性乳腺癌。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-09-25 DOI: 10.1080/20415990.2024.2400044
Boya Manasa Sai, Yirivinti Hayagreeva Dinakar, Hitesh Kumar, Rupshee Jain, Sharyu Kesharwani, Siddharth S Kesharwani, Shyam Lal Mudavath, Ajmeer Ramkishan, Vikas Jain

Breast cancer is the leading cause of cancer-related deaths among women globally. The difficulties with anticancer medications, such as ineffective targeting, larger doses, toxicity to healthy cells and side effects, have prompted attention to alternate approaches to address these difficulties. RNA interference by small interfering RNA (siRNA) is one such tactic. When compared with chemotherapy, siRNA has several advantages, including the ability to quickly modify and suppress the expression of the target gene and display superior efficacy and safety. However, there are known challenges and hurdles that limits their clinical translation. Decomposition by endonucleases, renal clearance, hydrophilicity, negative surface charge, short half-life and off-target effects of naked siRNA are obstacles that hinder the desired biological activity of naked siRNA. Nanoparticulate systems such as polymeric, lipid, lipid-polymeric, metallic, mesoporous silica nanoparticles and several other nanocarriers were used for effective delivery of siRNA and to knock down genes involved in breast cancer and triple-negative breast cancer. The focus of this review is to provide a comprehensive picture of various strategies utilized for delivering siRNA, such as combinatorial delivery, development of modified nanoparticles, smart nanocarriers and nanocarriers that target angiogenesis, cancer stem cells and metastasis of breast cancer.

乳腺癌是全球妇女因癌症死亡的主要原因。抗癌药物存在靶向性不强、剂量较大、对健康细胞有毒性和副作用等问题,这促使人们关注其他方法来解决这些难题。通过小干扰 RNA(siRNA)进行 RNA 干扰就是其中一种方法。与化疗相比,siRNA 具有多种优势,包括能够快速改变和抑制靶基因的表达,并显示出卓越的疗效和安全性。然而,已知的挑战和障碍限制了其临床转化。裸 siRNA 被内切酶分解、肾脏清除、亲水性、表面负电荷、半衰期短以及脱靶效应等都是阻碍裸 siRNA 发挥预期生物活性的障碍。纳米颗粒系统,如聚合物、脂质、脂聚合、金属、介孔二氧化硅纳米颗粒和其他一些纳米载体,被用于有效递送 siRNA 并敲除乳腺癌和三阴性乳腺癌的相关基因。本综述的重点是全面介绍用于递送 siRNA 的各种策略,如组合递送、开发改性纳米颗粒、智能纳米载体以及针对乳腺癌血管生成、癌症干细胞和转移的纳米载体。
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引用次数: 0
Targeted drug delivery to the thrombus by fusing streptokinase with a fibrin-binding peptide (CREKA): an in silico study. 通过融合链激酶和纤维蛋白结合肽(CREKA)向血栓靶向给药:一项硅学研究。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-04-30 DOI: 10.4155/tde-2023-0107
Mohammad Soroosh Hajizade, Mohammad Javad Raee, Seyed Nooreddin Faraji, Fakhrossadat Farvadi, Maryam Kabiri, Sedigheh Eskandari, Ali Mohammad Tamaddon

Aim: Streptokinase has poor selectivity and provokes the immune response. In this study, we used in silico studies to design a fusion protein to achieve targeted delivery to the thrombus. Materials & methods: Streptokinase was analyzed computationally for mapping. The fusion protein modeling and quality assessment were carried out on several servers. The enzymatic activity and the stability of the fusion protein and its complex with plasminogen were assessed through molecular docking analysis and molecular dynamics simulation respectively. Results: Physicochemical properties analysis, protein quality assessments, protein-protein docking and molecular dynamics simulations predicted that the designed fusion protein is functionally active. Conclusion: Our results showed that this fusion protein might be a prospective candidate as a novel thrombolytic agent with better selectivity.

目的:链激酶的选择性较差,会引起免疫反应。在本研究中,我们利用硅学研究设计了一种融合蛋白,以实现对血栓的靶向给药。材料与方法:通过计算分析链激酶的图谱。在多个服务器上进行了融合蛋白建模和质量评估。通过分子对接分析和分子动力学模拟,分别评估了融合蛋白的酶活性和稳定性及其与纤溶酶原的复合物。结果理化性质分析、蛋白质质量评估、蛋白质-蛋白质对接和分子动力学模拟预测所设计的融合蛋白质具有功能活性。结论我们的研究结果表明,这种融合蛋白可能是一种具有更好选择性的新型溶栓药物。
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引用次数: 0
Development of fexofenadine self-microemulsifying delivery systems: an efficient way to improve intestinal permeability. 开发非索非那定自微乳化给药系统:改善肠道渗透性的有效方法。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-06-28 DOI: 10.1080/20415990.2024.2363635
Ziba Islambulchilar, Ashkan Barfar, Shahla Mirzaeei

Aim: The present study aimed to prepare and evaluate fexofenadine self-microemulsifying drug-delivery systems (SMEDDS) formulation and to determine and compare its intestinal permeability using in situ single-pass intestinal perfusion (SPIP) technique.Methods: Fexofenadine-loaded SMEDDS were prepared and optimized. Droplet size, polydispersity index, zeta potential, drug release and intestinal permeability were evaluated.Results: Optimized formulation consisted of 15% oil, 80% surfactant and 5% cosolvent. Droplet size and drug loading of optimized formulation was 13.77 nm and 60 mg/g and it has released 90% of its drug content. Intestinal permeability of fexofenadine was threefold enhanced in SMEDDS compared with free fexofenadine.Conclusion: The results of our study revealed that SMEDDS could be a promising tool for oral delivery of fexofenadine with enhanced dissolution rate and intestinal permeability.

目的:本研究旨在制备和评估非索非那定自微乳化给药系统(SMEDDS)制剂,并采用原位单通道肠道灌注(SPIP)技术测定和比较其肠道渗透性。研究方法制备并优化了负载非索非那定的 SMEDDS。对液滴大小、多分散指数、ZETA电位、药物释放和肠道渗透性进行了评估。结果显示优化配方由 15%的油、80% 的表面活性剂和 5% 的共溶剂组成。优化配方的液滴大小和载药量分别为 13.77 纳米和 60 毫克/克,释放了 90% 的药物成分。与游离非索非那定相比,SMEDDS 中非索非那定的肠道渗透性提高了三倍。结论我们的研究结果表明,SMEDDS 可以提高非索非那定的溶出率和肠道渗透性,是一种很有前途的口服给药工具。
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引用次数: 0
March Industry News. 三月行业新闻。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-06-28 DOI: 10.1080/20415990.2024.2365621
Fiona McCartney
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引用次数: 0
Role of EYP-1901 in neovascular age-related macular degeneration and diabetic eye diseases: review of Phase I/II trials. EYP-1901 在新生血管性老年黄斑变性和糖尿病眼病中的作用:I/II 期试验回顾。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-10-03 DOI: 10.1080/20415990.2024.2406226
Abrahem Sayed, Pranesh Ravichandran, Cecilia Canizela, Rehan M Hussain

EYP-1901 (Duravyu) has demonstrated promising outcomes in Phases I and II clinical trials for the treatment of neovascular age-related macular degeneration (nAMD) and diabetic macular edema (DME)/diabetic retinopathy. This innovative treatment capitalizes on the potent anti-angiogenic properties of vorolanib, an inhibitor that targets all isoforms of VEGF, effectively mitigating the pathological neovascularization and vascular permeability that underpin these retinal conditions. EYP-1901 is integrated with the Durasert drug delivery system to administer a sustained release of vorolanib directly to the posterior segment of the eye. This delivery system ensures a consistent therapeutic effect over an extended period and significantly reduces the frequency of clinical interventions required, offering a more convenient treatment regimen while maintaining patient safety.

EYP-1901(Duravyu)在治疗新生血管性老年性黄斑变性(nAMD)和糖尿病性黄斑水肿(DME)/糖尿病视网膜病变的 I 期和 II 期临床试验中取得了良好的疗效。Vorolanib 是一种针对血管内皮生长因子所有异构体的抑制剂,这种创新疗法利用了 Vorolanib 的强效抗血管生成特性,有效缓解了支撑这些视网膜病变的病理性新生血管和血管通透性。EYP-1901 与 Durasert 给药系统集成,可直接向眼球后段持续释放沃罗来尼。这种给药系统可确保长期持续的治疗效果,并大大减少所需的临床干预频率,在保证患者安全的同时提供更方便的治疗方案。
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引用次数: 0
Antimicrobial peptide-fibrin glue mixture for treatment of methicillin-resistant Staphylococcus aureus-infected wounds. 用于治疗耐甲氧西林金黄色葡萄球菌感染伤口的抗菌肽-纤维蛋白胶混合物。
IF 3 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2024-01-01 Epub Date: 2024-07-16 DOI: 10.1080/20415990.2024.2369497
Mehran Bahreini, Mehrdad Moosazadeh Moghaddam, Masoud Ghorbani, Mohammad Reza Nourani, Reza Mirnejad

Aim: This study was conducted to investigate the effect of fibrin glue-CM11 antibacterial peptide mixture (FG-P) on the healing of infected wounds in vivo.Materials & methods: We formulated a mixture of FG-P and evaluated its antimicrobial activity in vitro against multidrug-resistant (MDR) bacteria involved in wound infection as well as its healing effect on wound infected by methicillin-resistant S. aureus (MRSA) in vivo.Results: The peptide had an MIC of 8 μg/ml against all bacteria isolates. Growth inhibition zones were evident for FG-P compared with FG. The in vivo study showed that the FG-P could be significantly effective in healing the MRSA-infected wound.Conclusion: The use of FG-P mixture is a very suitable option for treating infected wounds.

目的:本研究旨在探讨纤维蛋白胶-CM11 抗菌肽混合物(FG-P)对体内感染伤口愈合的影响。材料与方法:我们配制了一种 FG-P 混合物,并在体外评估了它对伤口感染中的多重耐药(MDR)细菌的抗菌活性,以及在体内评估了它对耐甲氧西林金黄色葡萄球菌(MRSA)感染伤口的愈合效果。研究结果该肽对所有细菌分离物的 MIC 均为 8 μg/ml。与 FG 相比,FG-P 的生长抑制区明显。体内研究表明,FG-P 对愈合 MRSA 感染的伤口有显著效果。结论使用 FG-P 混合物治疗受感染的伤口是一种非常合适的选择。
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引用次数: 0
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Therapeutic delivery
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