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Delivering Volume 15: welcome to another year of Therapeutic Delivery! 交付》第 15 卷:欢迎来到《治疗交付》的又一年!
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-12-20 DOI: 10.4155/tde-2023-0126
Rebecca Turner
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引用次数: 0
A narrative review on Naringin and Naringenin as a possible bioenhancer in various drug-delivery formulations. 关于柚皮苷和柚皮苷在各种给药配方中可能用作生物增效剂的综述。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-12-01 Epub Date: 2023-12-13 DOI: 10.4155/tde-2023-0086
Pradeepti Ganesh, Vanishree Suresh, Manoj Kumar Narasimhan, Sarvesh Sabarathinam

Naringenin belongs to the flavanones and is mainly found in fruits (grapefruit and oranges) and vegetables. Naringenin exhibits lipid-lowering and insulin-like characteristics and is used to treat osteoporosis, cancer and cardiovascular disorders. Their incorporation into drug formulations offers several advantages, including enhanced solubility, improved bioavailability and targeted delivery. Naringin-based formulations are beneficial in cancer, for example controlling breast and prostate cancer by inhibition of CYP19. Naringin suppresses the PI3K/AKT signalling pathway, it triggers autophagy, which effectively halts the proliferation of gastric cancer cells. Naringin and naringenin co-administration or pre-administration has enhanced the target drug's potency and produced a synergistic effect. This published study demonstrates the potential applications of Naringin and Naringenin as recognized bio-enhancers.

柚皮苷属于黄烷酮类化合物,主要存在于水果(柚子和橘子)和蔬菜中。柚皮苷具有降血脂和类胰岛素的特性,可用于治疗骨质疏松症、癌症和心血管疾病。将柚皮苷添加到药物制剂中具有多种优势,包括提高溶解度、改善生物利用度和靶向给药。基于柚皮苷的制剂对癌症有益,例如通过抑制 CYP19 来控制乳腺癌和前列腺癌。柚皮苷能抑制 PI3K/AKT 信号通路,引发自噬,从而有效阻止胃癌细胞的增殖。柚皮苷和柚皮甙联合给药或预给药可增强靶向药物的效力,产生协同效应。这项已发表的研究证明了柚皮苷和柚皮甙作为公认的生物增强剂的潜在应用价值。
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引用次数: 0
Nanoparticle-based delivery platforms for the enhanced oral delivery of peptides/proteins. 基于纳米颗粒的递送平台,用于增强多肽/蛋白质的口服递送。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-12-01 Epub Date: 2023-12-19 DOI: 10.4155/tde-2023-0048
Sara Salatin, Soheila Montazersaheb, Afsaneh Farjami, Samin Hamidi

Biopharmaceutical products are currently well-established in nearly all branches of medicine and are believed to have great potential for the treatment of a broad spectrum of diseases. Peptide/protein drugs exhibit a predominant class of new biopharmaceuticals coming on the market in recent years. Oral delivery of peptides/proteins as a non-invasive therapeutic technique has become an appealing alternative to the parenteral route. However, the efficient oral delivery of peptides/proteins is limited because of their high molecular weight, poor stability and low biodistribution. Nanoparticles (NPs) have shown excellent results in peptide/protein delivery research. In this paper, the use of NPs as delivery systems for peptides/proteins and their ability to be efficiently delivered via the oral route have been described.

目前,生物制药产品在几乎所有医学领域都得到了广泛应用,并被认为在治疗各种疾病方面具有巨大潜力。肽/蛋白质药物是近年来上市的新型生物制药的主要类别。多肽/蛋白质口服给药作为一种非侵入性治疗技术,已成为肠外给药途径的一种有吸引力的替代方法。然而,由于多肽/蛋白质分子量高、稳定性差、生物分布低,其高效口服给药受到了限制。纳米颗粒(NPs)在多肽/蛋白质给药研究中取得了卓越的成果。本文介绍了 NPs 作为肽/蛋白质给药系统的用途及其通过口服途径高效给药的能力。
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引用次数: 0
Engineered exosomes: a promising vehicle in cancer therapy. 工程外泌体:一种前景广阔的癌症治疗工具。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-12-01 Epub Date: 2023-12-20 DOI: 10.4155/tde-2023-0131
Farkhondeh Pooresmaeil, Sahar Andi, Behnam Hasannejad-Asl, Shahla Takamoli, Azam Bolhassani

During the past few decades, researchers have attempted to discover an effective treatment for cancer. Exosomes are natural nanovesicles released by various cells and play a role in communication between cells. While natural exosomes have high clinical potential, their inherent limitations have prompted researchers to design exosomes with improved therapeutic properties. To achieve this purpose, researchers have undertaken exosome engineering to modify the surface properties or internal composition of exosomes. After these modifications, engineered exosomes can be used as carriers for delivery of chemotherapeutic agents, targeted drug delivery or development of cancer vaccines. The present study provides an overview of exosomes, including their biogenesis, biological functions, isolation techniques, engineering methods, and potential applications in cancer therapy.

在过去的几十年里,研究人员一直试图找到一种有效的癌症治疗方法。外泌体是由各种细胞释放的天然纳米颗粒,在细胞之间的交流中发挥着作用。虽然天然外泌体具有很高的临床潜力,但其固有的局限性促使研究人员设计出具有更好治疗特性的外泌体。为此,研究人员开展了外泌体工程研究,以改变外泌体的表面特性或内部组成。经过这些改造后,工程外泌体可用作载体,用于递送化疗药物、靶向药物递送或开发癌症疫苗。本研究概述了外泌体,包括其生物发生、生物功能、分离技术、工程方法以及在癌症治疗中的潜在应用。
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引用次数: 0
Quality by design-assisted development of D-α-tocopherol polyethylene glycol 1000 succinate-incorporated gefitinib-loaded cationic liposome(s). 通过设计辅助开发D-α-生育酚聚乙二醇1000琥珀酸-吉非替尼负载阳离子脂质体的质量。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-12-01 Epub Date: 2023-11-29 DOI: 10.4155/tde-2023-0075
Lopamudra Mishra, Shuvadip Bhowmik, Rajveer Singh, Preeti Patel, Ghanshyam Das Gupta, Balak Das Kurmi

Aim: Gefitinib-loaded D-α-tocopherol polyethylene glycol 1000 succinate (TPGS)-coated cationic liposomes (GEF-TPGS-LIPO+) were developed and optimized by the quality by design (QbD) approach for its potential anticancer effect. Methods/materials: Box-Behnken design (BBD) a systematic design of experiments was added to screen and optimize the formulation variables. Results: GEF-TPGS-LIPO+ shows vesicle size (210 ± 4.82 nm), polydispersity index (0.271 ± 0.002), zeta potential (22.2 ± 0.84 mV) and entrapment efficiency (82.3 ± 1.95). MTT result shows the enhanced cytotoxicity and higher intracellular drug uptake with highest and lowest levels of the reactive oxygen species and NF-κB expressions on A549 lung cancer cells, determined by fluorescence-activated cell sorting flow cytometry. Conclusion: Potential anticancer effect on A549 cells might be found due to cationic liposomal interaction with cancer cells.

目的:研制吉非替尼负载D-α-生育酚聚乙二醇1000琥珀酸酯(TPGS)包被阳离子脂质体(GEF-TPGS-LIPO+),并采用质量设计(QbD)方法对其潜在的抗癌作用进行优化。方法/材料:采用Box-Behnken设计(BBD),采用系统的实验设计对配方变量进行筛选和优化。结果:GEF-TPGS-LIPO+的囊泡大小为210±4.82 nm,多分散性指数为0.271±0.002,zeta电位为22.2±0.84 mV,包封效率为82.3±1.95。MTT结果显示,A549肺癌细胞的细胞毒性增强,细胞内药物摄取增加,活性氧和NF-κB的表达水平最高和最低。结论:阳离子脂质体可能与癌细胞相互作用,对A549细胞具有潜在的抗癌作用。
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引用次数: 0
On the role of nanocarriers in oral drug delivery. 纳米载体在口服给药中的作用。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-12-01 Epub Date: 2023-12-13 DOI: 10.4155/tde-2023-0117
Qin Yu, Wei Wu
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引用次数: 0
Anthocyanin-enriched extract from Ribes nigrum inhibits triglyceride and cholesterol accumulation in adipocytes. 富含花青素的黑肋提取物抑制甘油三酯和胆固醇在脂肪细胞中的积累。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-11-01 Epub Date: 2023-11-29 DOI: 10.4155/tde-2023-0018
Laura Montaldo, Alicia Gallo, Gabriela Rocha, Cecilia Csernoch, Mauricio De Marzi, Liliana N Guerra

Aim: Obesity is a chronic pathology of epidemic proportions. Mature adipocytes from a 3T3-L1 cell line were used as in vitro obesity model to test different bioactive compounds. We aim to evaluate cassis (Ribes nigrum) extract antioxidant activity and its antiadipogenic effect on mature adipocytes. Results: We produced an extract by using enzyme that combines cellulase and pectinase; we obtained high yield of the bioactive compound anthocyanin. Extract showed high antioxidant capacity. We conducted in vitro assays by adding the extract to adipocytes culture medium. Extract reduced intracellular levels of triglyceride by 62% and cholesterol by 32%. Conclusion: Enzymatic extract's high antioxidant activity was likely attributable to its high concentration of anthocyanin. This extract inhibits lipid accumulation in adipocytes.

目的:肥胖是一种具有流行性的慢性疾病。采用3T3-L1细胞系成熟脂肪细胞作为体外肥胖模型,检测不同生物活性化合物。本研究旨在评价黑醋栗提取物的抗氧化活性及其对成熟脂肪细胞的抗脂作用。结果:采用纤维素酶和果胶酶相结合的酶制得提取物;我们获得了高收率的生物活性化合物花青素。提取物具有较高的抗氧化能力。我们将提取液加入到脂肪细胞培养液中进行体外实验。提取物使细胞内甘油三酯水平降低62%,胆固醇水平降低32%。结论:酶提物具有较高的抗氧化活性可能与酶提物中花青素含量较高有关。这种提取物抑制脂肪细胞中的脂质积累。
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引用次数: 0
September industry news update. 9月行业新闻更新。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-11-01 Epub Date: 2023-12-07 DOI: 10.4155/tde-2023-0120
Fiona McCartney
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引用次数: 0
Characteristics and release of isoniazid from inhalable alginate/carrageenan microspheres. 可吸入海藻酸/卡拉胶微球中异烟肼的特性和释放。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-11-01 Epub Date: 2023-12-12 DOI: 10.4155/tde-2023-0064
Yotomi Desia Eka Rani, Mahardian Rahmadi, Dewi Melani Hariyadi

Aim: Inhalable microspheres made of polymers as a targeted drug delivery system have been developed to overcome the limitation of current treatments in Tuberculosis. Materials & methods: Isoniazid inhalable microspheres were created using a gelation ionotropic method with sodium alginate, carrageenan and calcium chloride in four different formulations. Result: The particle morphology has smooth surfaces and round spherical shapes with sizes below 5 μm; good flowability. The drug loading and entrapment efficiency values ranged from 1.69 to 2.75% and 62.44 to 85.30%, respectively. The microspheres drug release followed the Korsmeyer-Peppas model, indicating Fickian diffusion. Conclusion: Isoniazid inhalable microspheres achieved as targeted lung delivery for tuberculosis treatment.

目的:为了克服目前治疗结核病的局限性,我们开发了由聚合物制成的可吸入微球,作为一种靶向给药系统。材料与方法:使用海藻酸钠、卡拉胶和氯化钙四种不同配方的凝胶电离法制作异烟肼吸入微球。研究结果颗粒形态表面光滑,呈圆球形,大小低于 5 μm,流动性良好。药物载量和包埋效率值分别为 1.69% 至 2.75% 和 62.44% 至 85.30%。微球的药物释放遵循 Korsmeyer-Peppas 模型,表明其具有 Fickian 扩散作用。结论异烟肼可吸入微球实现了肺部靶向给药治疗结核病。
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引用次数: 0
Microemulsions, nanoemulsions and emulgels as carriers for antifungal antibiotics. 微乳剂、纳米乳剂和乳剂作为抗真菌抗生素的载体。
IF 4.2 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-11-01 Epub Date: 2023-11-28 DOI: 10.4155/tde-2023-0076
Annapurna Padaraju, Falguni Dwivedi, Gautam Kumar

According to estimates, up to 25% of the world's population has fungal skin diseases, making them the most prevalent infectious disease. Several chemical classes of antifungal drugs are available to treat fungal infections. However, the major challenges of conventional formulations of antifungal drugs include poor pharmacokinetic profiles like solubility, low permeability, side effects and decreased efficacy. Novel drug delivery is a promising approach for overcoming pharmacokinetic limitations and increasing the effectiveness of antibiotics. In this review, we have shed light on microemulsions, nanoemulsions, and emulgels as novel drug delivery approaches for the topical delivery of antifungal antibiotics. We believe these formulations have potential translational value and could be developed for treating fungal infections in humans.

据估计,世界上高达25%的人口患有真菌性皮肤病,使其成为最普遍的传染病。几种化学类型的抗真菌药物可用于治疗真菌感染。然而,传统抗真菌药物配方的主要挑战包括药物动力学特征差,如溶解度、低渗透性、副作用和疗效下降。新型药物递送是克服药代动力学限制和提高抗生素有效性的一种很有前途的方法。在这篇综述中,我们阐明了微乳液、纳米乳液和乳液作为局部给药抗真菌抗生素的新型给药途径。我们相信这些配方具有潜在的转化价值,可以开发用于治疗人类真菌感染。
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Therapeutic delivery
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