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Mannose: A Promising Player in Clinical and Biomedical Applications. 甘露糖:在临床和生物医学应用中大有可为。
Pub Date : 2024-01-15 DOI: 10.2174/0115672018275954231220101637
Sijing Chen, Kana Wang, Qiao Wang

Mannose, an isomer of glucose, exhibits a distinct molecular structure with the same formula but a different atom arrangement, contributing to its specific biological functions. Widely distributed in body fluids and tissues, particularly in the nervous system, skin, testes, and retinas, mannose plays a crucial role as a direct precursor for glycoprotein synthesis. Glycoproteins, essential for immune regulation and glycosylation processes, underscore the significance of mannose in these physiological activities. The clinical and biomedical applications of mannose are diverse, encompassing its anti-inflammatory properties, potential to inhibit bacterial infections, role in metabolism regulation, and suggested involvement in alleviating diabetes and obesity. Additionally, mannose shows promise in antitumor effects, immune modulation, and the construction of drug carriers, indicating a broad spectrum of therapeutic potential. The article aims to present a comprehensive review of mannose, focusing on its molecular structure, metabolic pathways, and clinical and biomedical applications, and also to emphasize its status as a promising therapeutic agent.

甘露糖是葡萄糖的一种异构体,具有独特的分子结构,其分子式相同,但原子排列不同,因此具有特殊的生物功能。甘露糖广泛分布于体液和组织中,尤其是在神经系统、皮肤、睾丸和视网膜中,作为糖蛋白合成的直接前体,甘露糖发挥着至关重要的作用。糖蛋白是免疫调节和糖基化过程中必不可少的物质,这突出了甘露糖在这些生理活动中的重要作用。甘露糖的临床和生物医学应用多种多样,包括其抗炎特性、抑制细菌感染的潜力、在新陈代谢调节中的作用,以及参与缓解糖尿病和肥胖症的建议。此外,甘露糖在抗肿瘤作用、免疫调节和构建药物载体方面也大有可为,显示出广泛的治疗潜力。本文旨在对甘露糖进行全面综述,重点介绍其分子结构、代谢途径以及临床和生物医学应用,并强调其作为一种有前景的治疗剂的地位。
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引用次数: 0
Dextran-based Drug Delivery Approaches for Lung Diseases: A Review. 基于葡聚糖的肺部疾病给药方法:综述。
Pub Date : 2024-01-12 DOI: 10.2174/0115672018267737231116100812
Manisha Kumari, Sanyam Sharma, Navjot Kanwar, Subh Naman, Ashish Baldi

Respiratory disorders, such as tuberculosis, cystic fibrosis, chronic obstructive pulmonary disease, asthma, lung cancer, and pulmonary inflammation, are among the most prevalent ailments in today's world. Dextran, an exopolysaccharide formed by Leuconostoc mesenteroides (slimeproducing bacteria), and its derivatives are investigated for several therapeutic utilities. Dextranbased drug delivery system can become an innovative strategy in the treatment of several respiratory ailments as it offers numerous advantages, such as mucolytic action, airway hydration, antiinflammatory properties, and radioprotective effect as compared to other polysaccharides. Being biocompatible, flexible hydrophilic nature, biodegradable, tasteless, odourless, non-mutagenic, watersoluble and non-toxic edible polymer, dextran-based drug delivery systems have been explored for a wide range of therapeutic applications, especially in lungs and respiratory diseases. The present article comprehensively discusses various derivatives of dextran with their attributes to be considered for drug delivery and extensive therapeutic benefits, with a special emphasis on the armamentarium of dextran-based formulations for the treatment of respiratory disorders and associated pathological conditions. The information provided will act as a platform for formulation scientists as important considerations in designing therapeutic approaches for lung and respiratory diseases. With an emphasis on lung illnesses, this article will offer an in-depth understanding of dextran-based delivery systems in respiratory illnesses.

肺结核、囊性纤维化、慢性阻塞性肺病、哮喘、肺癌和肺部炎症等呼吸系统疾病是当今世界最普遍的疾病之一。右旋糖酐是一种由肠道黏液产生菌(Leuconostoc mesenteroides)形成的外多糖,其衍生物被研究用于多种治疗用途。与其他多糖相比,葡聚糖具有多种优势,如粘液溶解作用、气道水合作用、抗炎特性和放射保护作用,因此,以葡聚糖为基础的给药系统可以成为治疗多种呼吸系统疾病的创新策略。葡聚糖是一种具有生物相容性、柔性亲水性、可生物降解、无味、无臭、无致突变性、水溶性和无毒的可食用聚合物,以葡聚糖为基础的给药系统已被广泛应用于治疗领域,尤其是肺部和呼吸系统疾病。本文全面论述了葡聚糖的各种衍生物,以及它们在给药方面的特性和广泛的治疗效果,特别强调了以葡聚糖为基础的配方在治疗呼吸系统疾病和相关病症方面的作用。所提供的信息将为制剂科学家提供一个平台,作为设计肺部和呼吸系统疾病治疗方法的重要考虑因素。本文将以肺部疾病为重点,深入介绍基于葡聚糖的给药系统在呼吸系统疾病中的应用。
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引用次数: 0
Synergistic Antibacterial Effect of ZnO Nanoparticles and Antibiotics against Multidrug-Resistant Biofilm Bacteria. 氧化锌纳米颗粒与抗生素对耐多药生物膜细菌的协同抗菌效果
Pub Date : 2024-01-12 DOI: 10.2174/0115672018279213240110045557
Majed M Masadeh, Noor M Bany-Ali, Mai S Khanfar, Karem H Alzoubi, Majd M Massadeh, Enaam M Almomani

Background: The misuse of antibiotics leads to a global increase in antibiotic resistance. Therefore, it is imperative to search for alternative compounds to conventional antibiotics. ZnO nanoparticles (Zn NP) are one of these alternatives because they are an effective option to overcome biofilm bacterial cells and a novel way to overcome multidrug resistance in bacteria. The current research study aims to characterize the efficacy of ZnO nanoparticles alone and in combination with other antibacterial drugs against bacterial biofilms.

Methods: ZnO NPs were prepared by co-precipitation method, and their anti-biofilm and antibacterial activities alone or combined with four types of broad-spectrum antibacterial (Norfloxacin, Colistin, Doxycycline, and Ampicillin) were evaluated against E. coli and S. aureus bacterial strains. Finally, the cytotoxicity and the hemolytic activity were evaluated.

Results: ZnO NPs were prepared, and results showed that their size was around 10 nm with a spherical shape and a zeta potential of -21.9. In addition, ZnO NPs were found to have a strong antibacterial effect against Gram-positive and Gram-negative microorganisms, with a minimum inhibitory concentration (MIC) of 62.5 and 125 μg/mL, respectively. Additionally, they could eradicate biofilmforming microorganisms at a concentration of 125 μg/m. ZnO NPs were found to be non-toxic to erythrocyte cells. Still, some toxicity was observed for Vero cells at effective concentration ranges needed to inhibit bacterial growth and eradicate biofilm-forming organisms. When combined with different antibacterial, ZnO NP demonstrated synergistic and additive effects with colistin, and the MIC and MBEC of the combination decreased significantly to 0.976 μg/mL against planktonic and biofilm strains of MDR Gram-positive bacteria, resulting in significantly reduced toxicity.

Conclusion: The findings of this study encourage the development of alternative therapies with high efficacy and low toxicity. ZnO nanoparticles have demonstrated promising results in overcoming multi-drug resistant bacteria and biofilms, and their combination with colistin has shown a significant reduction in toxicity. Further studies are needed to investigate the potential of ZnO nanoparticles as a viable alternative to conventional antibiotics.

背景:抗生素的滥用导致全球抗生素耐药性的增加。因此,寻找传统抗生素的替代化合物势在必行。氧化锌纳米粒子(Zn NP)是这些替代品之一,因为它们是克服生物膜细菌细胞的有效选择,也是克服细菌多重耐药性的一种新方法。目前的研究旨在确定氧化锌纳米粒子单独使用或与其他抗菌药物联合使用对细菌生物膜的疗效:方法:采用共沉淀法制备 ZnO NPs,并评估其单独或与四种广谱抗菌药物(诺氟沙星、可乐定、强力霉素和氨苄西林)联合使用对大肠杆菌和金黄色葡萄球菌的抗生物膜和抗菌活性。最后,还评估了细胞毒性和溶血活性:结果:制备出的 ZnO NPs 大小约为 10 nm,呈球形,Zeta 电位为 -21.9。此外,研究还发现 ZnO NPs 对革兰氏阳性和革兰氏阴性微生物具有很强的抗菌作用,其最低抑菌浓度(MIC)分别为 62.5 和 125 μg/mL。此外,在 125 μg/m 浓度下,它们还能消灭形成生物膜的微生物。研究发现,氧化锌纳米粒子对红细胞无毒。不过,在抑制细菌生长和根除生物膜形成微生物所需的有效浓度范围内,观察到氧化锌纳米粒子对 Vero 细胞有一定毒性。当氧化锌氮氧化物与不同的抗菌剂结合使用时,它与可乐定产生了协同和相加效应,对革兰氏阳性耐药菌的浮游菌株和生物膜菌株的 MIC 和 MBEC 显著下降至 0.976 μg/mL,从而大大降低了毒性:结论:本研究的发现有助于开发高效低毒的替代疗法。氧化锌纳米粒子在克服多重耐药细菌和生物膜方面取得了可喜的成果,其与可乐定的结合也显示出毒性的显著降低。需要进一步研究氧化锌纳米粒子作为传统抗生素可行替代品的潜力。
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引用次数: 0
Transdermal Drug Delivery System of Linagliptin Sustained-release Microparticle Gels: In vitro Characterization and In vivo Evaluation. 利拉利汀缓释微粒凝胶透皮给药系统:体外表征和体内评估。
Pub Date : 2024-01-11 DOI: 10.2174/0115672018279370240103062944
Jiayan Liu, Song Guo, Shuai Hong, Jingshu Piao, Mingguan Piao

Background: Linagliptin (LNG) exhibits poor bioavailability and numerous side effects, significantly limiting its use. Transdermal drug delivery systems (TDDS) offer a potential solution to overcome the first-pass effect and gastrointestinal reactions associated with oral formulations.

Objective: The aim of this study was to develop LNG microparticle gels to enhance drug bioavailability and mitigate side effects.

Methods: Linagliptin hyaluronic acid (LNG-HA) microparticles were prepared by spray drying method and their formulation was optimized via a one-factor method. The solubility and release were investigated using the slurry method. LNG-HA microparticle gels were prepared and optimised using in vitro transdermal permeation assay. The hypoglycaemic effect of the LNG-HA microparticle gel was examined on diabetic mice.

Results: The results indicated that the LNG-HA microparticle encapsulation rate was 84.46%. Carbomer was selected as the gel matrix for the microparticle gels. Compared to the oral API, the microparticle gel formulation demonstrated a distinct biphasic release pattern. In the first 30 minutes, only 43.56% of the drug was released, followed by a gradual release. This indicates that the formulation achieved a slow-release effect from a dual reservoir system. Furthermore, pharmacodynamic studies revealed a sustained hypoglycemic effect lasting for 48 hours with the LNG microparticle gel formulation.

Conclusion: These findings signify that the LNG microparticle gel holds significant clinical value for providing sustained release and justifies its practical application.

背景:利拉利汀(LNG)生物利用度低,副作用多,严重限制了其使用。透皮给药系统(TDDS)为克服与口服制剂相关的首过效应和胃肠道反应提供了一种潜在的解决方案:本研究旨在开发 LNG 微颗粒凝胶,以提高药物的生物利用度并减轻副作用:方法:采用喷雾干燥法制备了利拉利汀透明质酸(LNG-HA)微颗粒,并通过单因素法对其配方进行了优化。采用浆液法研究了其溶解度和释放度。制备了 LNG-HA 微颗粒凝胶,并通过体外透皮试验对其进行了优化。在糖尿病小鼠身上检测了 LNG-HA 微颗粒凝胶的降血糖效果:结果:结果表明,LNG-HA 微颗粒的包封率为 84.46%。微颗粒凝胶选择了卡波姆作为凝胶基质。与口服原料药相比,微颗粒凝胶制剂表现出明显的双相释放模式。在最初的 30 分钟内,只有 43.56% 的药物被释放,随后药物逐渐释放。这表明该制剂实现了双储层系统的缓释效果。此外,药效学研究表明,液化天然气微粒凝胶配方的持续降糖效果可持续 48 小时:这些研究结果表明,液化天然气微颗粒凝胶在提供持续释放方面具有重要的临床价值,并证明了其实际应用的合理性。
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引用次数: 0
From Vision Correction to Drug Delivery: Unraveling the Potential of Therapeutic Contact Lens. 从视力矫正到药物输送:揭示治疗性隐形眼镜的潜力。
Pub Date : 2024-01-11 DOI: 10.2174/0115672018270396231213074746
Ankush Saini, Mohit Sharma, Indu Singh, Rajan Swami

Contact lenses (CLs) have become an essential tool in ocular drug delivery, providing effective treatment options for specific eye conditions. In recent advancements, Therapeutic CLs (TCLs) have emerged as a promising approach for maintaining therapeutic drug concentrations on the eye surface. TCLs offer unique attributes, including prolonged wear and a remarkable ability to enhance the bioavailability of loaded medications by more than 50%, thus gaining widespread usage. They have proven beneficial in pain management, medication administration, corneal healing, and protection. To achieve sustained drug delivery from TCLs, researchers are exploring diverse systems, such as polymeric nanoparticulate systems, lipidic systems, and the incorporation of agents like vitamin E or rate-limiting polymers. However, despite breakthrough successes, certain challenges persist, including ensuring drug stability during processing and manufacturing, controlling release kinetics, and biomaterial interaction, reducing protein adhesion, and addressing drug release during packaging and storage etc. While TCLs have shown overall success in treating corneal and ocular surface disorders, careful consideration of potential issues and contraindications is vital. This review offers an insightful perspective on the critical aspects that need to be addressed regarding TCLs, with a specific emphasis on their advantages and limitations.

隐形眼镜(CL)已成为眼部给药的重要工具,为特定眼部疾病提供了有效的治疗方案。近年来,治疗型隐形眼镜(TCL)已成为一种在眼球表面保持治疗药物浓度的有效方法。TCL 具有独特的特性,包括佩戴时间长,能显著提高所含药物的生物利用度 50%以上,因此得到了广泛应用。事实证明,它们有利于疼痛控制、用药、角膜愈合和保护。为了实现 TCL 的持续给药,研究人员正在探索多种系统,如聚合物纳米颗粒系统、脂质系统,以及加入维生素 E 或限速聚合物等药剂。然而,尽管取得了突破性的成功,某些挑战依然存在,包括确保加工和制造过程中的药物稳定性、控制释放动力学和生物材料相互作用、减少蛋白质粘附以及解决包装和储存过程中的药物释放问题等。虽然 TCL 在治疗角膜和眼表疾病方面取得了全面成功,但仔细考虑潜在的问题和禁忌症至关重要。本综述就 TCL 需要解决的关键问题提供了深刻的见解,并特别强调了其优势和局限性。
{"title":"From Vision Correction to Drug Delivery: Unraveling the Potential of Therapeutic Contact Lens.","authors":"Ankush Saini, Mohit Sharma, Indu Singh, Rajan Swami","doi":"10.2174/0115672018270396231213074746","DOIUrl":"https://doi.org/10.2174/0115672018270396231213074746","url":null,"abstract":"<p><p>Contact lenses (CLs) have become an essential tool in ocular drug delivery, providing effective treatment options for specific eye conditions. In recent advancements, Therapeutic CLs (TCLs) have emerged as a promising approach for maintaining therapeutic drug concentrations on the eye surface. TCLs offer unique attributes, including prolonged wear and a remarkable ability to enhance the bioavailability of loaded medications by more than 50%, thus gaining widespread usage. They have proven beneficial in pain management, medication administration, corneal healing, and protection. To achieve sustained drug delivery from TCLs, researchers are exploring diverse systems, such as polymeric nanoparticulate systems, lipidic systems, and the incorporation of agents like vitamin E or rate-limiting polymers. However, despite breakthrough successes, certain challenges persist, including ensuring drug stability during processing and manufacturing, controlling release kinetics, and biomaterial interaction, reducing protein adhesion, and addressing drug release during packaging and storage etc. While TCLs have shown overall success in treating corneal and ocular surface disorders, careful consideration of potential issues and contraindications is vital. This review offers an insightful perspective on the critical aspects that need to be addressed regarding TCLs, with a specific emphasis on their advantages and limitations.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139428216","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Novel Products as Promising Therapeutic Agents for Angiogenesis Inhibition. 抑制血管生成的新型治疗药物。
Pub Date : 2024-01-09 DOI: 10.2174/0115672018277869231217165048
Shaheen Sultana, Shahnaz Sultana, Shehla Nasar Mir Najib Ullah, Ameeduzzafar Zafar

Objective: Angiogenesis is the process of forming new blood vessels from pre-existing vessels and occurs during development, wound healing, and tumor growth. In this review, we aimed to present a comprehensive view of various factors contributing to angiogenesis during carcinogenesis. Anti-angiogenesis agents prevent or slow down cancer growth by interrupting the nutrients and blood supply to the tumor cells, and thus can prove beneficial for treatment.

Method: The discovery of several novel angiogenic inhibitors has helped to reduce both morbidity and mortality from several life-threatening diseases, such as carcinomas. There is an urgent need for a new comprehensive treatment strategy combining novel anti-angiogenic agents for the control of cancer. The article contains details of various angiogenic inhibitors that have been adopted by scientists to formulate and optimize such systems in order to make them suitable for cancer.

Results: The results of several researches have been summarized in the article and all of the data support the claim that anti-angiogenic agent is beneficial for cancer treatment.

Conclusion: This review focuses on novel antiangiogenic agents that play a crucial role in controlling carcinogenesis.

目的:血管生成是由原有血管形成新血管的过程,发生在发育、伤口愈合和肿瘤生长过程中。在这篇综述中,我们旨在全面介绍癌变过程中导致血管生成的各种因素。抗血管生成药物通过阻断肿瘤细胞的营养和血液供应,防止或减缓癌症的生长,从而有利于治疗:方法:几种新型血管生成抑制剂的发现有助于降低几种危及生命的疾病(如癌症)的发病率和死亡率。目前迫切需要一种新的综合治疗策略,将新型抗血管生成药物结合起来,以控制癌症。本文详细介绍了科学家们采用的各种血管生成抑制剂,以配制和优化此类系统,使其适用于癌症:结果:文章总结了多项研究成果,所有数据都支持抗血管生成剂有利于癌症治疗的说法:本综述重点介绍了在控制癌变方面发挥关键作用的新型抗血管生成剂。
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引用次数: 0
TPGS-mediated Transethosomes Enhance Transdermal Administration of Curcumin via Effects on Deformability and Stability. TPGS 介导的转吸附体通过对变形性和稳定性的影响增强姜黄素的透皮给药。
Pub Date : 2024-01-09 DOI: 10.2174/0115672018279577231208055415
Teng Guo, Chenming Zhang, Yuling Chen, Yihan Wu, Zhenda Liu, Yongtai Zhang, Nianping Feng

Background: Adding a suitable surfactant can enhance the transdermal permeability of transethosomes while also leveraging its functionality as a functional material. In this study, transethosomes were prepared using D-α-tocopherol acid polyethylene glycol succinate (TPGS) as edge activators for transdermal delivery of curcumin (Cur).

Methods: The TPGS-mediated curcumin-loaded transethosomes (Cur@TES) were prepared and formulated optimally, and the optimized formulations were characterized for their morphology, particle size, entrapment efficiency (EE) and drug loading (DL). The stability and deformability of Cur@TES were investigated, while the transdermal delivery of Cur@TES was investigated through in vitro transdermal assays and fluorescence imaging. A mouse ear swelling model was performed to determine the anti-inflammatory effect of Cur@TES.

Results: Cur@TES appeared round or elliptical in shape. The particle size, EE and DL for the optimized formulation were observed as 131.2 ± 7.2 nm, 97.68 ± 2.26%, and 6.58 ± 0.62%, respectively. X-ray diffraction analysis confirmed the formation of disordered structures in the inner core of the vesicles. Moreover, Cur@TES system demonstrated better stability and deformability compared to the curcumin-loaded ethosomes (Cur@ES). In-vitro transdermal experiments demonstrated that Cur@TES significantly increased the amount of drug retained in the skin (P<0.05). Fluorescence imaging confirmed that the skin distribution were distinctly enhanced with the delivery by TPGS mediated transethosomes. In addition, Cur@TES showed a significant inhibitory effect on Inflammatory swelling in the mouse ear-swelling model.

Conclusion: TPGS-mediated transethosomes exhibit significant transdermal advantages and enhanced anti-inflammatory effects, providing a new perspective for the transdermal delivery of curcumin.

背景:添加适当的表面活性剂可以提高透硫体的透皮渗透性,同时还能利用其作为功能材料的特性。本研究以 D-α-生育酚酸聚乙二醇琥珀酸酯(TPGS)为边缘活化剂,制备了用于姜黄素(Cur)透皮递送的透硫体:方法:制备并优化了TPGS介导的姜黄素负载透硫体(Cur@TES),并对优化后的制剂进行了形态、粒度、包埋效率(EE)和载药量(DL)的表征。研究了 Cur@TES 的稳定性和变形性,并通过体外透皮试验和荧光成像研究了 Cur@TES 的透皮给药效果。为了确定 Cur@TES.Results 的抗炎效果,对小鼠耳朵肿胀模型进行了研究:Cur@TES呈圆形或椭圆形。优化配方的粒度、EE 和 DL 分别为 131.2 ± 7.2 nm、97.68 ± 2.26% 和 6.58 ± 0.62%。X 射线衍射分析证实,囊泡内核形成了无序结构。此外,与载姜黄素的乙硫体(Cur@ES)相比,Cur@TES 系统表现出更好的稳定性和可变形性。体外透皮实验表明,Cur@TES 能显著增加皮肤中的药物保留量(P<0.05)。荧光成像证实,TPGS 介导的透硫体在皮肤中的分布明显增强。此外,在小鼠耳肿胀模型中,Cur@TES 对炎性肿胀有明显的抑制作用:结论:TPGS 介导的反式硫体具有明显的透皮优势和更强的抗炎效果,为姜黄素的透皮给药提供了新的视角。
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引用次数: 0
TPGS-modified Chitosan Nanoparticles of EGFR Inhibitor: Physicochemical and In vitro Evaluation against HepG2 Cell Lines. 表皮生长因子受体抑制剂的 TPGS 改性壳聚糖纳米颗粒:针对 HepG2 细胞系的理化和体外评估
Pub Date : 2024-01-08 DOI: 10.2174/0115672018268315231206045504
Mahendra Singh, Alka, Prashant Shukla, Zhi-Hong Wen, Chou-Yuan Ko, Ramachandran Vinayagam

Background: Gefitinib (GFN) is an Epithelial Growth Factor Receptor (EGFR) inhibitor, and Food and Drug Administration (FDA) has approved medication to treat lung cancer. However, this investigation aimed to produce and characterize Gefitinib (GFN)-loaded chitosan and soy lecithin nanoparticles (NPs) modified with D-α-tocopheryl polyethylene glycol 1000 succinate mono ester (TPGS) and assess their therapeutic potential against HepG2 liver cell lines.

Methods: Chitosan, a cationic polymer with biocompatible and biodegradable properties, was combined with soy lecithin to develop the NPs loaded with GFN using a self-organizing ionic interaction methodology.

Results: The entrapment efficiency and drug loading were found to be 59.04±4.63 to 87.37±3.82% and 33.46±3.76 to 49.50±4.35%, respectively, and results indicated the encapsulation of GEN in NPs. The pH of the formulations was observed between 4.48-4.62. Additionally, all the prepared NPs showed the size and PDI range of 89.2±15.9 nm to 799.2±35.8 nm and 0.179±0.065 to 0.455±0.097, respectively. The FTIR bands in optimized formulation (GFN-NP1) indicated that the drug might be contained within the NP's core. The SEM photograph revealed the spherical shape of NPs. The kinetic release model demonstrated the combination of diffusion and erosion mechanisms. The IC50 value of GFN and GFN-NP1 formulation against the HepG2 cell lines were determined and found to be 63.22±3.36 μg/ml and 45.80±2.53 μg/ml, respectively. DAPI and PI staining agents were used to detect nuclear morphology.

Conclusion: It was observed that the optimized GFN-NP1 formulation successfully internalized and inhibited the growth of HepG2 cells. Hence, it can be concluded that the prepared NPs can be a new therapeutic option for treating liver cancer.

背景:吉非替尼(Gefitinib,GFN)是一种上皮生长因子受体(EGFR)抑制剂,美国食品和药物管理局(FDA)已批准该药用于治疗肺癌。然而,本研究旨在制备和表征用 D-α-生育酚聚乙二醇 1000 丁二酸单酯(TPGS)修饰的吉非替尼(GFN)负载壳聚糖和大豆卵磷脂纳米颗粒(NPs),并评估其对 HepG2 肝细胞系的治疗潜力:方法:壳聚糖是一种具有生物相容性和生物可降解性的阳离子聚合物,它与大豆卵磷脂相结合,利用自组织离子相互作用方法开发出了负载 GFN 的 NPs:结果表明,GEN 在 NPs 中的包封效率和载药量分别为 59.04±4.63% 至 87.37±3.82%,33.46±3.76% 至 49.50±4.35%。制剂的 pH 值在 4.48-4.62 之间。此外,所有制备的 NPs 的尺寸和 PDI 范围分别为 89.2±15.9 nm 至 799.2±35.8 nm 和 0.179±0.065 至 0.455±0.097。优化配方(GFN-NP1)中的傅立叶变换红外光谱带表明药物可能包含在 NP 核心中。扫描电镜照片显示 NPs 呈球形。动力学释放模型显示了扩散和侵蚀机制的结合。经测定,GFN 和 GFN-NP1 制剂对 HepG2 细胞株的 IC50 值分别为 63.22±3.36 μg/ml 和 45.80±2.53 μg/ml。DAPI和PI染色剂用于检测核形态:结论:经过优化的 GFN-NP1 制剂成功内化并抑制了 HepG2 细胞的生长。因此,可以认为制备的 NPs 是治疗肝癌的一种新疗法。
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引用次数: 0
Overcoming Skin Barrier with Transfersomes: Opportunities, Challenges, and Applications. 转运体克服皮肤屏障:机遇、挑战和应用。
Pub Date : 2024-01-04 DOI: 10.2174/0115672018272012231213100535
Bhupendra Dixena, Rashmi Madhariya, Anupama Panday, Alpana Ram, Akhlesh K Jain

Background: Transdermal drug delivery systems (TDDS) offer several advantages over traditional methods like injections and oral administration, including preventing first-pass metabolism, providing consistent and sustained activity, reducing side effects, enabling the use of short halflife drugs, improving physiological response, and enhancing patient convenience. However, the permeability of skin poses a challenge for TDDS, as it is impermeable to large molecules and hydrophilic drugs but permeable to small molecules and lipophilic medications. To overcome this barrier, researchers have investigated vesicular systems, such as transfersomes, liposomes, niosomes, and ethosomes. Among these vesicular systems, transfersomes are particularly promising for non-invasive drug administration due to their deformability and flexible membrane. They have been extensively studied for delivering anticancer drugs, insulin, corticosteroids, herbal medicines, and NSAIDs through the skin. Transfersomes have demonstrated efficacy in treating skin cancer, improving insulin delivery, enhancing site-specific corticosteroid delivery, and increasing the permeation and therapeutic effects of herbal medicines. They have also been effective in delivering pain relief with minimal side effects using NSAIDs and opioids. Transfersomes have been used for transdermal immunization and targeted drug delivery, offering site-specific release and minimizing adverse effects. Overall, transfersomes are a promising approach for transdermal drug delivery in various therapeutic applications.

Objectives: The aim of the present review is to discuss the various advantages and limitations of transfersomes and their mechanism to penetration across the skin, as well as their application for the delivery of various drugs like anticancer, antidiabetic, NSAIDs, herbal drugs, and transdermal immunization.

Methods: Data we searched from PubMed, Google Scholar, and ScienceDirect.

Results: In this review, we have explored the various methods of preparation of transferosomes and their application for the delivery of various drugs like anticancer, antidiabetic, NSAIDs, herbal drugs, and transdermal immunization.

Conclusion: In comparison to other vesicular systems, transfersomes are more flexible, have greater skin penetration capability, can transport systemic medicines, and are more stable. Transfersomes are capable of delivering both hydrophilic and hydrophobic drugs, making them suitable for transdermal drug delivery. The developed transfersomal gel could be used to improve medicine delivery through the skin.

背景:与注射和口服等传统方法相比,透皮给药系统(TDDS)具有多种优势,包括防止首过代谢、提供一致和持续的活性、减少副作用、允许使用半衰期短的药物、改善生理反应以及为患者提供更多便利。然而,皮肤的渗透性给 TDDS 带来了挑战,因为皮肤对大分子和亲水性药物不具渗透性,但对小分子和亲油性药物具有渗透性。为了克服这一障碍,研究人员研究了囊泡系统,如转移体、脂质体、niosomes 和 ethosomes。在这些囊泡系统中,转运体因其可变形性和柔性膜而特别有望用于非侵入性给药。在通过皮肤给药抗癌药物、胰岛素、皮质类固醇、草药和非甾体抗炎药方面,人们对它们进行了广泛的研究。转移体在治疗皮肤癌、改善胰岛素给药、增强皮质类固醇的特定部位给药以及提高中草药的渗透性和治疗效果等方面都有显著疗效。在使用非甾体抗炎药和阿片类药物止痛时,它们也能将副作用降到最低。转移体已被用于透皮免疫和靶向给药,提供特定部位的释放,并将不良反应降至最低。总之,转移体是一种很有前景的透皮给药方法,可用于多种治疗应用:本综述旨在讨论转移体的各种优势和局限性、它们在皮肤上的渗透机制,以及它们在抗癌、抗糖尿病、非甾体抗炎药、草药和透皮免疫等各种药物递送中的应用:方法:我们从 PubMed、Google Scholar 和 ScienceDirect 上搜索数据:在这篇综述中,我们探讨了转移体的各种制备方法及其在抗癌、抗糖尿病、非甾体抗炎药、草药和透皮免疫等各种药物递送中的应用:结论:与其他囊泡系统相比,转运体更灵活,皮肤穿透能力更强,可转运全身性药物,而且更稳定。转移体既能输送亲水性药物,也能输送疏水性药物,因此适用于透皮给药。所开发的转移体凝胶可用于改善经皮肤给药。
{"title":"Overcoming Skin Barrier with Transfersomes: Opportunities, Challenges, and Applications.","authors":"Bhupendra Dixena, Rashmi Madhariya, Anupama Panday, Alpana Ram, Akhlesh K Jain","doi":"10.2174/0115672018272012231213100535","DOIUrl":"https://doi.org/10.2174/0115672018272012231213100535","url":null,"abstract":"<p><strong>Background: </strong>Transdermal drug delivery systems (TDDS) offer several advantages over traditional methods like injections and oral administration, including preventing first-pass metabolism, providing consistent and sustained activity, reducing side effects, enabling the use of short halflife drugs, improving physiological response, and enhancing patient convenience. However, the permeability of skin poses a challenge for TDDS, as it is impermeable to large molecules and hydrophilic drugs but permeable to small molecules and lipophilic medications. To overcome this barrier, researchers have investigated vesicular systems, such as transfersomes, liposomes, niosomes, and ethosomes. Among these vesicular systems, transfersomes are particularly promising for non-invasive drug administration due to their deformability and flexible membrane. They have been extensively studied for delivering anticancer drugs, insulin, corticosteroids, herbal medicines, and NSAIDs through the skin. Transfersomes have demonstrated efficacy in treating skin cancer, improving insulin delivery, enhancing site-specific corticosteroid delivery, and increasing the permeation and therapeutic effects of herbal medicines. They have also been effective in delivering pain relief with minimal side effects using NSAIDs and opioids. Transfersomes have been used for transdermal immunization and targeted drug delivery, offering site-specific release and minimizing adverse effects. Overall, transfersomes are a promising approach for transdermal drug delivery in various therapeutic applications.</p><p><strong>Objectives: </strong>The aim of the present review is to discuss the various advantages and limitations of transfersomes and their mechanism to penetration across the skin, as well as their application for the delivery of various drugs like anticancer, antidiabetic, NSAIDs, herbal drugs, and transdermal immunization.</p><p><strong>Methods: </strong>Data we searched from PubMed, Google Scholar, and ScienceDirect.</p><p><strong>Results: </strong>In this review, we have explored the various methods of preparation of transferosomes and their application for the delivery of various drugs like anticancer, antidiabetic, NSAIDs, herbal drugs, and transdermal immunization.</p><p><strong>Conclusion: </strong>In comparison to other vesicular systems, transfersomes are more flexible, have greater skin penetration capability, can transport systemic medicines, and are more stable. Transfersomes are capable of delivering both hydrophilic and hydrophobic drugs, making them suitable for transdermal drug delivery. The developed transfersomal gel could be used to improve medicine delivery through the skin.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2024-01-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139099457","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Recent Advancements in Bioelectronic Medicine: A Review. 生物电子医学的最新进展:回顾。
Pub Date : 2024-01-03 DOI: 10.2174/0115672018286832231218112557
Sudipta Das, Baishali Ghosh, Rudra Narayan Sahoo, Amit Kumar Nayak

Bioelectronic medicine is a multidisciplinary field that combines molecular medicine, neurology, engineering, and computer science to design devices for diagnosing and treating diseases. The advancements in bioelectronic medicine can improve the precision and personalization of illness treatment. Bioelectronic medicine can produce, suppress, and measure electrical activity in excitable tissue. Bioelectronic devices modify specific neural circuits using electrons rather than pharmaceuticals and use bioelectronic processes to regulate the biological processes underlining various diseases. This promotes the potential to address the underlying causes of illnesses, reduce adverse effects, and lower costs compared to conventional medication. The current review presents different important aspects of bioelectronic medicines with recent advancements. The area of bioelectronic medicine has a lot of potential for treating diseases, enabling non-invasive therapeutic intervention by regulating brain impulses. Bioelectronic medicine uses electricity to control biological processes, treat illnesses, or regain lost capability. These new classes of medicines are designed by the technological developments in the detection and regulation of electrical signaling methods in the nervous system. Peripheral nervous system regulates a wide range of processes in chronic diseases; it involves implanting small devices onto specific peripheral nerves, which read and regulate the brain signaling patterns to achieve therapeutic effects specific to the signal capacity of a particular organ. The potential for bioelectronic medicine field is vast, as it investigates for treatment of various diseases, including rheumatoid arthritis, diabetes, hypertension, paralysis, chronic illnesses, blindness, etc.

生物电子医学是一个多学科领域,它将分子医学、神经学、工程学和计算机科学结合起来,设计用于诊断和治疗疾病的设备。生物电子医学的进步可以提高疾病治疗的精确性和个性化。生物电子医学可以产生、抑制和测量可兴奋组织中的电活动。生物电子设备利用电子而不是药物来改变特定的神经回路,并利用生物电子过程来调节各种疾病的生物过程。与传统药物治疗相比,生物电子设备具有解决疾病根本原因、减少不良反应和降低成本的潜力。本综述介绍了生物电子药物的不同重要方面以及最新进展。生物电子医学领域在治疗疾病方面具有很大的潜力,可通过调节脑脉冲实现非侵入性治疗干预。生物电子医学利用电能控制生物过程、治疗疾病或恢复丧失的能力。这些新型药物是通过检测和调节神经系统电信号方法的技术发展设计出来的。外周神经系统调节慢性疾病的各种过程;它涉及在特定外周神经上植入小型装置,读取并调节大脑信号模式,以达到针对特定器官信号能力的治疗效果。生物电子医学领域潜力巨大,它研究如何治疗各种疾病,包括类风湿性关节炎、糖尿病、高血压、瘫痪、慢性病、失明等。
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引用次数: 0
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Current drug delivery
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