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Recent Developments and Potential for Clinical Use of Casein as a Drug Carrier. 酪蛋白作为药物载体的最新进展及临床应用潜力。
IF 2.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.2174/1567201819666220513085552
Ravindra Semwal, Sunil Kumar Joshi, Ruchi Badoni Semwal, Deepak Kumar Semwal

Background: The development of drug delivery carriers is the key area of research in the field of novel drug delivery systems. To date, a long list of carriers has been identified for this purpose but the deliveries of poorly water-soluble active substances are still facing challenges and hence, such substances are pharmacologically unsafe and economically incompetent.

Objective: This article aims to review the applications of casein as a drug carrier and its potential for clinical use.

Methods: The relevant literature on the casein protein was collected from authentic online scientific databases like PubMed, Scopus and Google Scholar using different keywords including "casein", "drug delivery system", "drug carrier" and "bioavailability". The articles and books accessed online have been thoroughly reviewed and the most relevant reports on casein as a drug carrier have only been included in the present study.

Results: Casein is a milk protein that has many structural and physicochemical properties which facilitate its functionality in delivery systems. Moreover, its amphiphilic nature makes it the most suitable carrier for both hydrophobic and hydrophilic drugs without showing any toxic effects. The carriers obtained from natural sources are trustworthy over synthetic carriers and in the demand of the market due to their easy availability, low-cost factor, bio-friendly and nontoxic nature.

Conclusion: Casein was found to be an effective natural drug carrier in various delivery systems due to its unique applications in improving the bioavailability and efficacy of a drug.

背景:药物传递载体的开发是新型药物传递系统研究的重点领域。迄今为止,已经为此目的确定了一长列载体,但水溶性差的活性物质的输送仍然面临挑战,因此,这些物质在药理学上不安全,在经济上也不合格。目的:综述酪蛋白作为药物载体的应用及其临床应用潜力。方法:采用“酪蛋白”、“给药系统”、“药物载体”、“生物利用度”等关键词,从PubMed、Scopus、Google Scholar等正版在线科学数据库中检索酪蛋白相关文献。网上的文章和书籍都经过了全面的审查,关于酪蛋白作为药物载体的最相关的报告只包括在本研究中。结果:酪蛋白是一种牛奶蛋白,具有许多结构和物理化学性质,有助于其在输送系统中的功能。此外,它的两亲性使其成为疏水和亲水药物的最合适载体,而不会表现出任何毒性作用。与合成载体相比,天然载体具有易得、低成本、生物友好和无毒等特点,值得信赖。结论:酪蛋白在提高药物的生物利用度和药效方面具有独特的应用价值,是一种有效的天然药物载体。
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引用次数: 2
Wound Healing Properties of Pelargonium Graveolens L'Hér Extract Lipogel: In-Vivo Evaluation in an Animal Burn Model. 天竺葵提取物脂凝胶的伤口愈合性能:在动物烧伤模型中的体内评价。
IF 2.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.2174/1567201819666220509162659
Hossein Asgarirad, Bardia Berenji Tehrani, Mohammad Azadbakht, Pedram Ebrahimnejad, Ali Farmoudeh, Ali Davoodi, Anahita Rezaeiroshan, Seyyedeh Saba Hosseini

Background: Pelargonium graveolens L'Hér has traditionally been used to reduce skin inflammation, and recent studies have confirmed antioxidant compounds in the plant's extract. The present study aimed to prepare a lipogel formulation from P. graveolens hydroalcoholic extract and evaluate its efficacy on the wound healing process in an animal model.

Material and methods: The aerial part extract of P. graveolens was prepared through percolation. Additionally, plastibase was prepared by mixing 5% of low-molecular-weight polyethylene with hot mineral oil (130°C). The extract (5%) was levigated in the mineral oil (5-15%) and dispersed in the cooled plastibase. The physical properties of the lipogel, thermal stability, and microbial limits were tested. Further, the effect of the lipogel in the wound healing rate was examined among male Wistar rats, and skin tissue samples were assessed histologically.

Results and discussion: The results represented the best rheological and thermal stability characteristics in the formulation with 5% mineral oil (as the levigator). The lipogel-treated group had the least burn area compared to the silver sulfadiazine and negative control groups (p<0.05). The microscopic examination of tissue samples revealed increased collagen fiber production and maturation and significantly also faster epithelial repair among lipogel-treated rats than in the other two groups(p<0.05).

Conclusion: The results indicated the significant therapeutic effects of P. graveolens lipogelon burn healing. The suitable physicochemical properties and the low lipogel production cost facilitate further scale-up studies.

背景:天竺葵(Pelargonium graveolens L’h)传统上被用来减轻皮肤炎症,最近的研究证实了该植物提取物中含有抗氧化化合物。本研究旨在以石竹水醇提取物为原料制备脂凝胶制剂,并在动物模型上评价其对伤口愈合过程的影响。材料与方法:采用渗滤法制备黄连气部提取物。此外,通过将5%的低分子量聚乙烯与热矿物油(130°C)混合制备塑料基。提取液(5%)浸泡在矿物油(5-15%)中,分散在冷却的塑基中。测试了脂凝胶的物理性质、热稳定性和微生物限度。进一步,研究了脂凝胶对雄性Wistar大鼠伤口愈合率的影响,并对皮肤组织样本进行了组织学评估。结果与讨论:以5%矿物油为支撑剂的配方流变学和热稳定性最佳。与磺胺嘧啶银和阴性对照组相比,脂凝胶治疗组烧伤面积最小(p)。结论:脂凝胶治疗对烧伤愈合有显著的治疗作用。合适的理化性质和较低的生产成本有利于进一步的规模化研究。
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引用次数: 0
Enhanced Brain Delivery via Intranasal Administration of Carbamazepine Loaded Solid Lipid Nanoparticles: Optimization, Pharmacokinetic Analysis, In-vitro, and In-vivo Drug Release Study. 卡马西平固体脂质纳米颗粒经鼻内给药增强脑递送:优化、药代动力学分析、体外和体内药物释放研究。
IF 2.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.2174/1567201819666220519120837
Rajeshwar Kamal Kant Arya, Vijay Juyal, Dheeraj Bisht, Mohammad Rashid, Abdulmalik Saleh Alfawaz Altamimi, Obaid Afzal, Neeraj Kumar Sethiya

Background: Carbamazepine (Cbz) is the first-line drug for epileptic seizures but exhibits fluctuation at the plasma level and side effects after oral administration.To overcome these problems, Cbz should be targeted directly into the brain. Therefore, the current experimental design was aimed to formulate and optimize the Cbz containing solid lipid nanoparticles (SLNs) for brain delivery via intranasal administration to get rid of oral complications associated with Cbz.

Methods: A full factorial design was performed to evaluate the effect of variables (X1 lipid concentration, X2 surfactant concentration, and X3 sonication time) on the response variables (size of nanoparticles, entrapment efficiency, and drug release). A two-level, three-factor design was employed herewith, and eight formulations were developed. Further, the formation of Cbz containing SLNs was characterized by compatibility, particle size, entrapment efficiency, and drug release with the support of Fourier Transform Infra-Red (FTIR), Zeta sizer, Transmission Electron Microscopy (TEM), Ultra-violet (U.V.), and High-Performance Liquid Chromatography (HPLC).

Results: All eight formulations were characterized through particle size, entrapment efficiency, and invitro drug release performance. Out of eight characterized formulations, SN1 showed the most promising results, including particle size of 210 ± 2.14 nm, entrapment efficiency of 42.1 ± 1.09%, and drug release of 61.3 ± 2.02% and considered an optimized batch. Additionally, the optimized batch SN1was further evaluated for an in-vivo study on male Wistar Rats.

Conclusion: The study revealed that a high amount of drug was reached into the brain through intranasal administration compared to the intravenous route. Therefore, it can minimize the unwanted side effects of the Cbz associated with oral administration. The formulation SN1 possesses an excellent drug targeting efficiency of 3.014. Finally, the current experimental work concluded that there is a direct pathway from the intranasal route to the brain. This delivery system can be beneficial for directly delivering CNS-active drugs into the brain.

背景:卡马西平(Carbamazepine, Cbz)是治疗癫痫发作的一线药物,但口服后存在血浆水平波动和副作用。为了克服这些问题,Cbz应该直接针对大脑。因此,本实验设计旨在制备和优化含固体脂质纳米颗粒(SLNs)的脑内给药,以消除Cbz相关的口腔并发症。方法:采用全因子设计,评价不同因素(X1脂质浓度、X2表面活性剂浓度、X3超声时间)对纳米颗粒大小、包封效率和药物释放的影响。采用两水平、三因素设计,研制出八种配方。利用傅里叶变换红外(FTIR)、Zeta粒度仪、透射电子显微镜(TEM)、紫外(uv)和高效液相色谱(HPLC)等技术对含Cbz SLNs的相容性、粒径、包封效率和药物释放进行表征。结果:通过粒径、包封效率和体外释药性能对8种制剂进行了表征。结果表明,SN1的粒径为210±2.14 nm,包封效率为42.1±1.09%,释药率为61.3±2.02%,为最佳配方。此外,优化后的sn1批次在雄性Wistar大鼠体内进行了进一步的研究。结论:研究表明,与静脉给药相比,鼻内给药可使大量药物进入大脑。因此,它可以减少与口服给药有关的Cbz的不良副作用。制剂SN1具有优异的药物靶向效率,为3.014。最后,目前的实验工作得出结论,从鼻内途径到大脑有一个直接的途径。这种输送系统有利于将中枢神经系统活性药物直接输送到大脑。
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引用次数: 1
Artificial Intelligence Assisted Fabrication of 3D, 4D and 5D Printed Formulations or Devices for Drug Delivery. 人工智能辅助制造用于药物输送的3D, 4D和5D打印配方或设备。
IF 2.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.2174/1567201820666221207140956
Kiran Singh Sharma

5D & 4D printings are an advanced version of 3D printing class and are one of the most revolutionary and powerful fabrication methods used for preparing innovative structures and solid substances using precise additive manufacturing technology. It captures the imagination of one with its potential to produce flexible designing and fabrication of innovative products with high complexity and speed. This technology with the assistance of AI (Artificial Intelligence) facilitates real-time sensing, adapting to change, and predicting the state of printing. 3D printing works by employing advanced materials utilizing a computer aided design with tomography scan under AI control which deposits printing material in accordance with the nature of a file usually in STL format, but it requires time for printing. This shortcoming can be overcome by 4D printing where smart materials are incorporated with time as 4th dimension. This technique has self-repair and self-assembly properties that will save around 80% of time. Some printed materials are made sensitive to temperature, humidity, light, and other parameters so that they can respond to stimulus, but it's one limitation of not being able to print complex shapes having curved surfaces can be overcome by utilising 5D printing where additive manufacturing is done by rotation of extruder head and rotation of print bed to print in 5 different axes. This review evaluates the prospective of these techniques with AI interference in medicine and pharmacy, with its effective and efficient production for the required design precision.

5D和4D打印是3D打印类的高级版本,是最具革命性和强大的制造方法之一,用于使用精确的增材制造技术制备创新结构和固体物质。它抓住了一个人的想象力,它具有生产灵活设计和制造创新产品的潜力,具有高复杂性和速度。这项技术在人工智能(AI)的帮助下,有助于实时感知,适应变化,并预测打印状态。3D打印的工作原理是采用先进的材料,利用计算机辅助设计,在人工智能控制下进行断层扫描,根据文件的性质沉积打印材料,通常为STL格式,但打印需要时间。这一缺点可以通过4D打印来克服,其中智能材料与时间结合为第四维。这种技术具有自我修复和自组装的特性,可以节省大约80%的时间。一些打印材料对温度、湿度、光线和其他参数很敏感,因此它们可以对刺激做出反应,但是不能打印具有曲面的复杂形状的一个限制可以通过利用5D打印来克服,其中增材制造是通过旋转挤出机头和旋转打印床来在5个不同的轴上打印的。本文综述了这些人工智能干扰技术在医学和药学领域的前景,以及其有效和高效的生产所要求的设计精度。
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引用次数: 3
Current Novel Drug Deliveries for Oral Cancer: A Chronotherapeutic Approach. 目前口腔癌的新药物递送:一种时间治疗方法。
IF 2.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.2174/1567201819666220408094520
Kishori P Sutar, Nisha S Shirkoli, Prasanna S Sutar, Bhaskar K Kurangi, Panchaxari M Dandagi, Rajashree Masareddy

Oral squamous cell carcinoma is a malignant disease that is causing considerable mortality worldwide. Conventional treatment approaches, like surgery, cause destructive alterations in facial appearance and oral function impairments associated with psychological and social functioning. Chemotherapy exhibits low bioaccessibility of the anticancer drugs, multiple drug resistance, higher dose necessities, which elevate toxicities to the normal cells, low therapeutic index, and non-specific targeting. Radiation therapies significantly affect the well-being of the patient and impair the quality of life. Therefore, chemotherapeutics are developed that can either actively or passively target the carcinomas, reduce the adverse side effect, and improve therapeutic efficacy. Innovations in novel drug delivery systems deliver the drugs to the desired site of action with better treatment approaches with reduced toxicities to the normal cells and improve the health and survival rate of the patient. Cancer chronotherapy enhances the treatment proficiency by administration of the drugs at the best time, considering biological timings to improve the treatment profiles. Chronotherapy provides benefits to the current anticancer therapies, with minimum adverse effects to the healthy cells. This review discusses the risk factors for oral carcinomas, targeted therapy by nanocarriers, nanotechnology approaches, the role of circadian rhythm in the management of oral cancer, and advances in controlled drug delivery.

口腔鳞状细胞癌是一种恶性疾病,在世界范围内造成相当大的死亡率。传统的治疗方法,如手术,会导致面部外观的破坏性改变和与心理和社会功能相关的口腔功能损伤。化疗具有抗癌药物生物可及性低、多重耐药、剂量要求高、对正常细胞毒性升高、治疗指数低、非特异性靶向等特点。放射治疗显著影响病人的健康,损害生活质量。因此,开发主动或被动靶向肿瘤的化疗药物,减少不良副作用,提高治疗效果。新型药物输送系统的创新将药物输送到所需的作用部位,采用更好的治疗方法,减少对正常细胞的毒性,提高患者的健康和存活率。癌症时间疗法通过在最佳时间给药来提高治疗能力,同时考虑生物时间来改善治疗概况。时间疗法为目前的抗癌疗法提供了好处,对健康细胞的不良影响最小。本文综述了口腔癌的危险因素、纳米载体靶向治疗、纳米技术方法、昼夜节律在口腔癌治疗中的作用以及控制给药方面的进展。
{"title":"Current Novel Drug Deliveries for Oral Cancer: A Chronotherapeutic Approach.","authors":"Kishori P Sutar,&nbsp;Nisha S Shirkoli,&nbsp;Prasanna S Sutar,&nbsp;Bhaskar K Kurangi,&nbsp;Panchaxari M Dandagi,&nbsp;Rajashree Masareddy","doi":"10.2174/1567201819666220408094520","DOIUrl":"https://doi.org/10.2174/1567201819666220408094520","url":null,"abstract":"<p><p>Oral squamous cell carcinoma is a malignant disease that is causing considerable mortality worldwide. Conventional treatment approaches, like surgery, cause destructive alterations in facial appearance and oral function impairments associated with psychological and social functioning. Chemotherapy exhibits low bioaccessibility of the anticancer drugs, multiple drug resistance, higher dose necessities, which elevate toxicities to the normal cells, low therapeutic index, and non-specific targeting. Radiation therapies significantly affect the well-being of the patient and impair the quality of life. Therefore, chemotherapeutics are developed that can either actively or passively target the carcinomas, reduce the adverse side effect, and improve therapeutic efficacy. Innovations in novel drug delivery systems deliver the drugs to the desired site of action with better treatment approaches with reduced toxicities to the normal cells and improve the health and survival rate of the patient. Cancer chronotherapy enhances the treatment proficiency by administration of the drugs at the best time, considering biological timings to improve the treatment profiles. Chronotherapy provides benefits to the current anticancer therapies, with minimum adverse effects to the healthy cells. This review discusses the risk factors for oral carcinomas, targeted therapy by nanocarriers, nanotechnology approaches, the role of circadian rhythm in the management of oral cancer, and advances in controlled drug delivery.</p>","PeriodicalId":10842,"journal":{"name":"Current drug delivery","volume":"20 3","pages":"237-249"},"PeriodicalIF":2.4,"publicationDate":"2023-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"9233263","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 1
A Review of the Use of Metallic Nanoparticles as a Novel Approach for Overcoming the Stability Challenges of Blood Products: A Narrative Review from 2011-2021. 金属纳米颗粒作为克服血液制品稳定性挑战的新方法的回顾:2011-2021年的叙述性回顾。
IF 2.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.2174/1567201819666220513092020
Tahereh Zadeh Mehrizi, Mehdi Shafiee Ardestani, Sedigheh Amini Kafiabad

Purpose: To obtain safe and qualified blood products (e.g., platelets, plasma, and red blood cells), various limitations such as limited shelf life (especially for platelets) and stability must be addressed. In this review study, the most commonly used metal nanomaterials (e.g., gold, silver, iron, and magnetic) reported in the literature from 2011 to 2021 were discussed owing to their unique properties, which provide exciting approaches to overcome these limitations and improve the stability, safety, and quality of blood products. Novelty: This study reviews for the first time the results of studies (from 2011 to 2021) that consider the effects of various metallic nanoparticles on the different blood products.

Results: The results of this review study showed that some metallic nanoparticles are effective in improving the stability of plasma proteins. For this purpose, modified Fe3O4 magnetic nanoparticles and citrate-AuNPs protect albumin products against stressful situations. Also, SiO2 microspheres and silicacoated magnetite nanoparticles are highly capable of improving IgG stability. ZnO nanoparticles also reduced thrombin production, and protein-coated GMNP nanoparticles prevented unwanted leakage of factor VIII through blood vessels. Furthermore, the stability and longevity of erythrocytes can be improved by AuNP nanoparticles and Zr-based organic nanoparticles. In addition, platelet storage time can be improved using PEGylated Au and functionalized iron oxide nanoparticles.

Suggestion: According to the results of this study, it is suggested that further research should be conducted on metal nanoparticles as the most promising candidates to prepare metal nanoparticles with improved properties to increase the stability of various blood products.

目的:为了获得安全和合格的血液制品(如血小板、血浆和红细胞),必须解决各种限制,如有限的保质期(特别是血小板)和稳定性。在本综述研究中,由于其独特的性质,讨论了2011年至2021年文献中最常用的金属纳米材料(如金、银、铁和磁性),这些材料为克服这些限制并提高血液制品的稳定性、安全性和质量提供了令人兴奋的方法。新颖性:本研究首次回顾了考虑各种金属纳米颗粒对不同血液制品影响的研究结果(从2011年到2021年)。结果:本文的研究结果表明,一些金属纳米颗粒对提高血浆蛋白的稳定性有一定的作用。为此,修饰的Fe3O4磁性纳米颗粒和柠檬酸盐- aunps保护白蛋白产物免受应激情况的影响。此外,二氧化硅微球和硅包覆磁铁矿纳米颗粒也能显著提高IgG的稳定性。氧化锌纳米颗粒还可以减少凝血酶的产生,蛋白质包被的GMNP纳米颗粒可以防止VIII因子通过血管泄漏。此外,AuNP纳米粒子和zr基有机纳米粒子可以提高红细胞的稳定性和寿命。此外,聚乙二醇化的金和功能化的氧化铁纳米颗粒可以提高血小板的储存时间。建议:根据本研究结果,建议进一步研究金属纳米颗粒作为最有希望的候选材料,以制备性能更好的金属纳米颗粒,以提高各种血液制品的稳定性。
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引用次数: 0
Nanoformulations of Plant-Derived Compounds as Emerging Therapeutic Approach for Colorectal Cancer. 植物源化合物纳米制剂作为治疗结直肠癌的新途径。
IF 2.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.2174/1567201819666220823155526
Hossein Biganeh, Sahand Mirzaei Dizaji, Yasamin Davatgaran Taghipour, Ghulam Murtaza, Roja Rahimi

Background: Colorectal cancer (CRC) represents one of the most daunting health problems accompanied by progressive undesirable socio-economic effects. Phytochemicals, bioactive ingredients majorly found in plants, have gained momentum for their potential against CRC occurrence and regression. However, these phytoconstituents are not exempt from biopharmaceutical drawbacks; therefore, novel strategies, especially nanotechnology, are exploited to surmount the aforementioned bottlenecks. The current paper aims to comprehensively review the phytochemical-based nanoformulations and their mechanisms in the setting of CRC.

Methods: Electronic databases including Scopus, PubMed, and Web of Science were searched with the keywords "colon cancer" or "colorectal cancer", and "plant", "phytochemical", "extract", or "herb", and "nano", "nanoformulation", "Nanoencapsulation", "nanoparticle", "nanostructure", or "nanoliposome", until January 2021.

Results: Of the 1230 research hits, only 69 articles were consequently analyzed. The results indicated nanoformulations of several secondary plant metabolites such as berberine, camptothecin, colchicine, apigenin, chrysin, fisetin, quercetin, curcumin, gallic acid, resveratrol, and ursolic acid have profound effects in a broad range of preclinical models of CRC. A wide variety of nanoformulations have been utilized to deliver these phytochemicals, such as nanocomposite, nanocolloids, and mesoporous silica nanoparticles, which have consequently decreased tumor angiogenesis and mitochondrial membrane potential, increased radical scavenging activity, induced cell cycle arrest at different phases of the cancer cell cycle, and induction of apoptosis process via decreased anti-apoptotic proteins (BRAF, CD44, and Bcl-2) and increased in pro-apoptotic ones (Bax, Fas, caspase 3,8, and 9), as well as modulated biopharmaceutical properties. Chitosan and PEG and their derivatives are among the polymers exploited in the phytochemicals' nanoformulations.

Conclusion and perspective: To conclude, nanoformulated forms of natural ingredients depicted outstanding anti-CRC activity that could hold promise for help in treating CRC. However, well-designed clinical trials are needed to build up a whole picture of the health profits of nanoformulation of natural products in CRC management.

背景:结直肠癌(CRC)是最令人生畏的健康问题之一,并伴有不良的社会经济影响。植物化学物质(Phytochemicals)是一种主要存在于植物中的生物活性成分,因其在防治结直肠癌发生和消退方面的潜力而受到广泛关注。然而,这些植物成分也不能免于生物制药的缺点;因此,新的策略,特别是纳米技术,被用来克服上述瓶颈。本文旨在全面综述植物化学纳米制剂及其在结直肠癌中的作用机制。方法:以关键词“结肠癌”或“结直肠癌”、“植物”、“植物化学”、“提取物”或“草药”、“纳米”、“纳米配方”、“纳米胶囊”、“纳米颗粒”、“纳米结构”或“纳米脂质体”等检索Scopus、PubMed、Web of Science等电子数据库,检索截止日期为2021年1月。结果:在1230篇研究点击中,只有69篇文章被分析。结果表明,几种次生植物代谢物的纳米制剂,如小檗碱、喜树碱、秋水仙碱、芹菜素、大黄素、非塞酮、槲皮素、姜黄素、没食子酸、白藜芦醇和熊果酸,在广泛的CRC临床前模型中具有深远的影响。各种各样的纳米制剂已被用于传递这些植物化学物质,如纳米复合材料、纳米胶体和介孔二氧化硅纳米颗粒,它们因此降低了肿瘤血管生成和线粒体膜电位,增加了自由基清除活性,在癌细胞周期的不同阶段诱导细胞周期阻滞,并通过降低抗凋亡蛋白(BRAF、CD44、和Bcl-2),促凋亡因子(Bax、Fas、caspase 3、8和9)的表达增加,以及生物制药特性的调节。壳聚糖和聚乙二醇及其衍生物是植物化学物质纳米配方中开发的聚合物。结论与展望:综上所述,纳米形式的天然成分具有出色的抗结直肠癌活性,有望帮助治疗结直肠癌。然而,需要精心设计的临床试验来全面了解天然产品纳米配方在结直肠癌管理中的健康效益。
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引用次数: 2
Desonide Nanoemulsion Gel for Transdermal Absorption Drug Delivery: Pharmacodynamic and Safety Evaluation. 地奈德纳米乳凝胶经皮吸收给药:药效学和安全性评价。
IF 2.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.2174/1567201819666220819110128
Jiaqi Zhang, Yu Yao, Hanbing Liu, Qiuyan Ma, Lanyi Huang, Yuan Chen, Huaqing Lin

Background: When administered transdermally, desonide is ineffective due to its poor solubility. As a new transdermal delivery system, nanoemulsion gel has demonstrated significant advantages for drug delivery over conventional formulations. We have established desonide nanoemulsion gel (DES NE gel) for better transdermal absorption, but its efficacy and safety still need to be evaluated. This study aims to provide additional evidence demonstrating the improved pharmacodynamics and safety of transdermal delivery of Desonide via nanoemulsion gel.

Methods: Pharmacodynamics and safety of Desonide nanoemulsion gel were evaluated using Desonate ® as the reference formulation. To assess the difference in curative effect between DES NE gel and Desonate® and to ensure safety, atopic dermatitis (AD) models in KM mice were developed using 2,4-dinitrofluorobenzene (DNFB). The degree of ear swelling, ear mass difference, thymus, spleen index, and HE conventional pathology of mice were used as pharmacodynamic evaluation indexes, and the irritation was predicted by the New Zealand rabbit epidermal stimulation assay.

Results: Nanoemulsion gels may facilitate transdermal penetration of drugs by influencing the skin condition. Medium and high doses of DES NE gel significantly ameliorated the inflammation and swelling of the ear caused by dermatitis/eczema in mice. In addition, compared with DES gel, skin irritation extent did not increase.

Conclusion: Nanoemulsion gel can be applied to improve the efficacy of drugs with low potency or poor solubility. DES NE gel provides a higher transdermal potential than other delivery systems. In this study, it was found that nanoemulsion gel is a promising percutaneous carrier of DES. DES NE-GEL has a significant curative effect on dermatitis/eczema in a mouse model and is expected to provide a new, efficient, and low toxic preparation for clinical treatment of dermatitis/eczema through the percutaneous system.

背景:经皮给药时,地奈德由于溶解度差而无效。纳米乳凝胶作为一种新型的透皮给药系统,在给药方面具有传统给药方式无法比拟的优势。我们已经建立了地奈德纳米乳凝胶(DES NE凝胶),具有更好的透皮吸收效果,但其有效性和安全性仍有待评价。本研究旨在提供额外的证据,证明通过纳米乳凝胶经皮给药地奈德的药效学和安全性得到改善。方法:以地奈德®为参比制剂,评价地奈德纳米乳凝胶的药效学和安全性。为了评估DES - NE凝胶与地索酸钠(Desonate®)的疗效差异,并确保安全性,采用2,4-二硝基氟苯(DNFB)建立KM小鼠特应性皮炎(AD)模型。以小鼠耳肿胀程度、耳肿块差、胸腺、脾脏指数、HE常规病理作为药效学评价指标,采用新西兰兔表皮刺激法预测刺激效果。结果:纳米乳凝胶可通过影响皮肤状况促进药物的透皮渗透。中、高剂量DES NE凝胶可显著改善小鼠皮炎/湿疹引起的耳部炎症和肿胀。此外,与DES凝胶相比,皮肤刺激程度没有增加。结论:纳米乳凝胶可用于提高低效或溶解度差的药物的疗效。DES - NE凝胶提供了比其他输送系统更高的透皮潜能。本研究发现纳米乳凝胶是一种很有前景的经皮DES载体,DES NE-GEL在小鼠皮炎/湿疹模型中具有显著的疗效,有望为临床经皮治疗皮炎/湿疹提供一种新型、高效、低毒的制剂。
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引用次数: 1
Emerging Strategies to Improve the Stability and Bioavailability of Insulin: An Update on Formulations and Delivery Approaches. 提高胰岛素稳定性和生物利用度的新策略:配方和给药方法的最新进展。
IF 2.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.2174/1567201820666221102094433
Pak Kheong Tan, Umah Rani Kuppusamy, Kek Heng Chua, Bavani Arumugam

One of the primary goals of diabetes management is to maintain blood glucose levels within a normal range, and insulin plays a vital role in achieving this. All Type 1 DM patients and advanced Type 2 DM patients require insulin. Insulin is administered subcutaneously, which may cause patient discomfort from the use of needles. Therefore, developing alternative routes of insulin administration has always been a major focus of diabetes research. This review aims to provide an update on the insulin formulations and delivery routes as well as strategies used to improve its stability and bioavailability for the treatment of diabetes.

糖尿病管理的主要目标之一是将血糖水平维持在正常范围内,胰岛素在实现这一目标方面起着至关重要的作用。所有1型糖尿病患者和晚期2型糖尿病患者都需要胰岛素。胰岛素是皮下注射,这可能会引起患者使用针头的不适。因此,开发胰岛素的替代给药途径一直是糖尿病研究的重点。这篇综述旨在提供最新的胰岛素配方和给药途径,以及用于提高其稳定性和生物利用度治疗糖尿病的策略。
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引用次数: 6
Oral Candidiasis and Novel Therapeutic Strategies: Antifungals, Phytotherapy, Probiotics, and Photodynamic Therapy. 口腔念珠菌病和新的治疗策略:抗真菌、植物疗法、益生菌和光动力疗法。
IF 2.4 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pub Date : 2023-01-01 DOI: 10.2174/1567201819666220418104042
Maria Contaldo, Dario Di Stasio, Antonio Romano, Fausto Fiori, Fedora Della Vella, Cosimo Rupe, Carlo Lajolo, Massimo Petruzzi, Rosario Serpico, Alberta Lucchese

Oral candidiasis is an opportunistic infection of the oral mucosa sustained by fungi of the genus Candida. Various Candida species, with a predominance of C. albicans, normally a saprophyte of the oral cavity, may become virulent and infect the oral mucosa with variegated clinical presentation, in case of imbalance of the oral microbiota, the presence of local predisposing factors and systemic conditions that weaken the immune system. Conventionally, oral candidiasis eradication is done with the help of antifungal drugs. However, the growing phenomena of drug resistance and the increase in infections sustained by non-albicans species being less responsive to common antifungals have orientied researches towards the experimentation of alternative therapies. The present review considered the most promising alternative therapeutic proposals. The use of plant derivatives with phytotherapy is a promising option, such as probiotics, to rebalance the oral microbiota in case of dysbiosis. Finally, antimicrobial photodynamic therapy (aPDT), with highly selective fungicidal activity and free of side effects, is also being studied as a powerful alternative to drug administration. All these therapies are alternatives or supportive to the conventional treatment of recurrent and non-drug-responsive forms of oral candidiasis. However, further studies are needed to define the most active compounds, the efficacy of the therapies compared with the conventional ones, and the planning of regulated and standardized protocols.

口腔念珠菌病是由念珠菌属真菌引起的口腔黏膜机会性感染。不同种类的念珠菌,以白色念珠菌为优势,通常是口腔的腐生菌,在口腔微生物群失衡、局部易感因素和全身条件削弱免疫系统的情况下,可能变得有毒并感染口腔黏膜,临床表现各异。传统上,口腔念珠菌病的根除是在抗真菌药物的帮助下完成的。然而,越来越多的耐药性现象和非白色念珠菌对普通抗真菌药反应较差的感染的增加,使研究转向了替代疗法的实验。本综述考虑了最有希望的替代治疗建议。在植物疗法中使用植物衍生物是一个很有前途的选择,如益生菌,在生态失调的情况下重新平衡口腔微生物群。最后,抗菌光动力疗法(aPDT)具有高度选择性的杀真菌活性和无副作用,也正在研究作为药物管理的有力替代方案。所有这些疗法都是复发性和非药物反应性口腔念珠菌病常规治疗的替代或支持。然而,需要进一步的研究来确定最有效的化合物,与传统疗法相比的疗效,以及制定规范和标准化的方案。
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引用次数: 14
期刊
Current drug delivery
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