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Microneedles: An Efficient Technique to Increase Transdermal Drug Delivery System. 微针:增加透皮给药系统的有效技术。
Pub Date : 2024-07-18 DOI: 10.2174/0115672018301931240624072453
Sanjit Kr Roy, Kazi Asraf Ali, Mahua Biswas, Abhijit Dey, Amlan Bishal, Abhradeep Kuiry

Transdermal Drug Delivery Systems (TDDS) have gained attention as a viable substitute for traditional drug administration methods because of their controlled release capabilities and non-invasive design. Microneedles are a new and effective technology that has attracted a lot of attention recently to enhance the capabilities of TDDS further. The study on microneedles and their potential to improve transdermal medication delivery is thoroughly reviewed in this review article. The study initiates by clarifying the difficulties linked to traditional medication delivery techniques and the benefits provided by transdermal channels. The article then explores the development of microneedle technology, outlining the several kinds of microneedles-solid, hollow, and dissolving-as well as their uses. Because of their special capacity to penetrate the skin's protective layer painlessly and their ability to distribute drugs precisely and precisely, microneedles are a highly useful instrument in pharmaceutical research. The materials, geometry, and manufacturing processes that affect the design and creation of microneedles are critically analyzed and presented. The manuscript delves into the latest developments in microneedle technology, encompassing the utilization of biodegradable polymers, smart materials, and sensing components for in-the-- moment monitoring. This analysis concludes by highlighting the noteworthy advancements in the field of microneedles and their potential to transform transdermal drug delivery systems. This thorough knowledge seeks to further the current discussion in pharmaceutical research, encouraging creativity and opening the door for the creation of safer, more effective drug delivery systems.

透皮给药系统(TDDS)因其控释能力和非侵入性设计而备受关注,被视为传统给药方法的可行替代品。微针是一种新型而有效的技术,最近引起了广泛关注,以进一步提高透皮给药系统的能力。本综述文章全面回顾了微针研究及其改善透皮给药的潜力。研究首先阐明了与传统给药技术相关的困难以及透皮渠道带来的益处。文章随后探讨了微针技术的发展,概述了几种微针--实心、空心和溶解--及其用途。由于微针具有无痛穿透皮肤保护层的特殊能力,并能准确无误地分布药物,因此在药物研究中是一种非常有用的工具。书中对影响微针设计和制造的材料、几何形状和制造工艺进行了批判性分析和介绍。手稿深入探讨了微针技术的最新发展,包括利用可生物降解聚合物、智能材料和传感元件进行即时监测。分析报告最后强调了微针领域值得关注的进展及其改变透皮给药系统的潜力。这些全面的知识旨在推动当前的药物研究讨论,鼓励创新,为创造更安全、更有效的给药系统打开大门。
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引用次数: 0
Expanding Arsenal against Ocular Diseases through Nanoemulsion: Success So Far and the Road Ahead. 通过纳米乳剂扩大防治眼部疾病的武器库:迄今为止的成功与未来之路。
Pub Date : 2024-07-15 DOI: 10.2174/0115672018286288240705064730
Bala Vikash, Shashi, Narendra Kumar Pandey, Bimlesh Kumar, Sheetu Wadhwa, Ritu Gupta, Umesh Goutam, Amit Mittal, Dileep Singh Baghel, Sachin Kumar Singh, Saurabh Singh

The eye is a most delicate organ protected by several complex biological barriers that are static and dynamic. The presence of these ocular barriers retards drug absorption from topically applied dosage forms at the conjunctival sac. The efficient topical delivery of the drug into the globe is more difficult to achieve and there is a need to develop a topical formulation that may reduce the use of injections and increase patient compliance with decreased frequency of administration. In the advancements of research in nanotechnology, nanoemulsions can be used as biocompatible carriers to deliver the drug to the ocular cavity. The lipophilic globules can increase the solubility of hydrophobic cargos which provides increased permeation ability and ocular bioavailability which can sustain drug release and corneal retention. Because of their small size, these formulations do not cause blurring of vision. Nanoemulsions (NEs) over the past decade have been used to treat several ocular diseases in the anterior eye segment. This review summarizes the economic burden, pathology of ocular diseases, formulation considerations for ocular formulations, and recent advances of these NEs as effective carriers for ocular drug delivery highlighting their performance in pre-clinical studies.

眼睛是一个最脆弱的器官,受到多种复杂的静态和动态生物屏障的保护。这些眼屏障的存在阻碍了结膜囊对局部用药剂型的药物吸收。因此,需要开发一种局部用药配方,以减少注射次数,提高患者的依从性。随着纳米技术研究的发展,纳米乳剂可用作生物相容性载体,将药物输送到眼腔。亲脂性球状物可以增加疏水性载体的溶解度,从而提高渗透能力和眼部生物利用度,维持药物释放和角膜保留。由于体积小,这些制剂不会造成视力模糊。在过去十年中,纳米乳剂(NEs)已被用于治疗前眼部分的多种眼部疾病。本综述总结了经济负担、眼部疾病的病理、眼部制剂的配制注意事项,以及作为眼部给药有效载体的纳米乳剂的最新进展,并重点介绍了它们在临床前研究中的表现。
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引用次数: 0
Progress in Epigenetic Modification Regulating Drug Transporters in the Hypoxic Environment. 缺氧环境中调控药物转运体的表观遗传修饰研究进展。
Pub Date : 2024-06-27 DOI: 10.2174/0115672018295087240620061102
Ziqin Wei, Hongfang Mu, Xiaojing Zhang, Wenbin Li, Rong Wang

Drug transporters are critical factors influencing the pharmacokinetics of drugs under hypoxic conditions. Studies have shown significant changes in drug transporter levels in the hypoxic environment. In addition to being regulated by HIF-1, nuclear receptors, and inflammatory factors, hypoxia can also regulate transporters through epigenetic modifications, thereby affecting drug absorption, distribution, metabolism, and excretion. In recent years, increasing attention has been paid to the role of epigenetic modifications in regulating drug transporters under hypoxic conditions at high altitude. In this paper, we comprehensively review the effects of hypoxia on drug transporters and epigenetic modifications and explore the regulatory mechanism of epigenetic modifications on drug transporter expression under hypoxic conditions. The aim is to provide a reference for exploring the epigenetic regulation mechanism of drug transporter expression in the hypoxic environment at high altitude, and then guide the study of pharmacokinetics and promote effective and safe medication at high altitude.

药物转运体是影响缺氧条件下药物药代动力学的关键因素。研究表明,在缺氧环境下,药物转运体的水平会发生明显变化。除了受 HIF-1、核受体和炎症因子的调控外,缺氧还能通过表观遗传修饰调控转运体,从而影响药物的吸收、分布、代谢和排泄。近年来,人们越来越关注表观遗传修饰在高海拔缺氧条件下对药物转运体的调控作用。本文全面综述了缺氧对药物转运体及表观遗传修饰的影响,探讨了缺氧条件下表观遗传修饰对药物转运体表达的调控机制。旨在为探索高海拔缺氧环境下药物转运体表达的表观遗传调控机制提供参考,进而指导药代动力学研究,促进高海拔地区的有效安全用药。
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引用次数: 0
Machine Learning-Driven Advancements in Liposomal Formulations for Targeted Drug Delivery: A Narrative Literature Review. 机器学习驱动的靶向给药脂质体制剂的进步:叙述性文献综述。
Pub Date : 2024-06-27 DOI: 10.2174/0115672018302321240620072039
Benyamin Hoseini, Mahmoud Reza Jaafari, Amin Golabpour, Zahra Rahmatinejad, Maryam Karimi, Saeid Eslami

Nanoliposomal formulations, utilizing lipid bilayers to encapsulate therapeutic agents, hold promise for targeted drug delivery. Recent studies have explored the application of machine learning (ML) techniques in this field. This study aims to elucidate the motivations behind integrating ML into liposomal formulations, providing a nuanced understanding of its applications and highlighting potential advantages. The review begins with an overview of liposomal formulations and their role in targeted drug delivery. It then systematically progresses through current research on ML in this area, discussing the principles guiding ML adaptation for liposomal preparation and characterization. Additionally, the review proposes a conceptual model for effective ML incorporation. The review explores popular ML techniques, including ensemble learning, decision trees, instance- based learning, and neural networks. It discusses feature extraction and selection, emphasizing the influence of dataset nature and ML method choice on technique relevance. The review underscores the importance of supervised learning models for structured liposomal formulations, where labeled data is essential. It acknowledges the merits of K-fold cross-validation but notes the prevalent use of single train/test splits in liposomal formulation studies. This practice facilitates the visualization of results through 3D plots for practical interpretation. While highlighting the mean absolute error as a crucial metric, the review emphasizes consistency between predicted and actual values. It clearly demonstrates ML techniques' effectiveness in optimizing critical formulation parameters such as encapsulation efficiency, particle size, drug loading efficiency, polydispersity index, and liposomal flux. In conclusion, the review navigates the nuances of various ML algorithms, illustrating ML's role as a decision support system for liposomal formulation development. It proposes a structured framework involving experimentation, physicochemical analysis, and iterative ML model refinement through human-centered evaluation, guiding future studies. Emphasizing meticulous experimentation, interdisciplinary collaboration, and continuous validation, the review advocates seamless ML integration into liposomal drug delivery research for robust advancements. Future endeavors are encouraged to uphold these principles.

利用脂质双层膜包裹治疗药物的纳米脂质体制剂有望实现靶向给药。最近的研究探索了机器学习(ML)技术在这一领域的应用。本研究旨在阐明将 ML 集成到脂质体制剂中的动机,提供对其应用的细致理解,并强调其潜在优势。综述首先概述了脂质体制剂及其在靶向给药中的作用。然后,系统地介绍了该领域目前对 ML 的研究,讨论了指导 ML 适应脂质体制备和表征的原则。此外,该综述还提出了有效结合 ML 的概念模型。综述探讨了流行的 ML 技术,包括集合学习、决策树、基于实例的学习和神经网络。它讨论了特征提取和选择,强调了数据集性质和 ML 方法选择对技术相关性的影响。综述强调了监督学习模型对于结构化脂质体配方的重要性,在这种配方中,标记数据至关重要。它承认 K 倍交叉验证的优点,但指出在脂质体制剂研究中普遍使用单一的训练/测试分割。这种做法有利于通过三维图对结果进行可视化的实际解释。在强调平均绝对误差这一关键指标的同时,综述还强调了预测值与实际值之间的一致性。综述清楚地展示了 ML 技术在优化封装效率、粒度、药物负载效率、多分散指数和脂质体通量等关键制剂参数方面的有效性。总之,综述介绍了各种 ML 算法的细微差别,说明了 ML 作为脂质体制剂开发决策支持系统的作用。它提出了一个结构化框架,包括实验、理化分析以及通过以人为本的评估迭代完善 ML 模型,为未来的研究提供指导。该综述强调细致的实验、跨学科合作和持续验证,主张将 ML 无缝集成到脂质体给药研究中,以实现强劲的进步。我们鼓励未来的努力坚持这些原则。
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引用次数: 0
Nanocarriers: Exploring the Potential of Oligonucleotide Delivery. 纳米载体:探索寡核苷酸传递的潜力。
Pub Date : 2024-06-24 DOI: 10.2174/0115672018306882240618093152
Omar Awad Alsaidan

Nanoparticle-based delivery systems have emerged as promising tools in oligonucleotide therapeutics, facilitating precise and targeted delivery to address several disease conditions. The multifaceted landscape of nanoparticle-based oligonucleotide delivery encompasses the fundamental aspects of nanotechnology in delivery systems, various classes of oligonucleotides, and the growing field of ON-based therapeutics. These ON-based therapeutics are utilized to target specific genetic sequences within cells, offering promising avenues for treating various diseases by regulating gene expression or interfering with specific cellular processes. The integration of nanotechnology in delivery systems offers several advantages, given their intricate systems. Being a diverse class of agents, oligonucleotides provide a wide range of potential owed to each class of agents that support therapeutic interventions. Oligonucleotide-based platforms have demonstrated their versatility in molecular targeting and intervention strategies. Moreover, the complexities and delivery challenges in oligonucleotide therapeutics are expected to be overcome by the application of nanotechnology-based platforms.Because nanoparticles can overcome biological barriers and improve bioavailability, stability, and specificity, their role in developing oligonucleotide delivery systems is greatly valued. The innovative solutions facilitated by nanoparticles are efficient strategies to address the arduous barriers. These strategies beat obstacles like enzymatic degradation, cellular uptake, and immune response, which in turn paves the way for enhanced therapeutic efficacy. This review paper intends to explore the various applications of nanoparticle-mediated oligonucleotide delivery in a variety of diseases. It outlines the promising growth of therapies enabled by these systems, extending from cancer to genetic disorders, neurodegenerative diseases, etc. We have underscored the pivotal role of nanoparticle-based delivery systems in uncovering the full potential of oligonucleotide therapeutics, thereby fostering advancements in precision medicine and targeted therapies.

基于纳米粒子的递送系统已成为寡核苷酸疗法中前景广阔的工具,可促进精确和靶向递送,以治疗多种疾病。基于纳米粒子的寡核苷酸递送技术涉及多个方面,包括递送系统中纳米技术的基本方面、各类寡核苷酸以及不断发展的基于 ON 的疗法。这些基于 ON 的疗法可用于靶向细胞内的特定基因序列,通过调节基因表达或干扰特定细胞过程来治疗各种疾病,前景广阔。由于纳米技术系统错综复杂,因此将纳米技术融入给药系统具有多种优势。寡核苷酸是一类多种多样的制剂,为支持治疗干预的每一类制剂提供了广泛的潜在用途。基于寡核苷酸的平台已经证明了其在分子靶向和干预策略方面的多功能性。此外,寡核苷酸疗法的复杂性和递送难题有望通过应用纳米技术平台来克服。由于纳米颗粒可以克服生物障碍,提高生物利用度、稳定性和特异性,因此它们在开发寡核苷酸递送系统中的作用备受重视。纳米颗粒所提供的创新解决方案是解决棘手障碍的有效策略。这些策略克服了酶降解、细胞吸收和免疫反应等障碍,从而为提高疗效铺平了道路。本综述旨在探讨纳米粒子介导的寡核苷酸递送在各种疾病中的各种应用。它概述了这些系统带来的治疗方法的发展前景,包括癌症、遗传性疾病、神经退行性疾病等。我们强调了基于纳米粒子的递送系统在发掘寡核苷酸疗法的全部潜力方面所起的关键作用,从而促进了精准医学和靶向疗法的发展。
{"title":"Nanocarriers: Exploring the Potential of Oligonucleotide Delivery.","authors":"Omar Awad Alsaidan","doi":"10.2174/0115672018306882240618093152","DOIUrl":"https://doi.org/10.2174/0115672018306882240618093152","url":null,"abstract":"<p><p>Nanoparticle-based delivery systems have emerged as promising tools in oligonucleotide therapeutics, facilitating precise and targeted delivery to address several disease conditions. The multifaceted landscape of nanoparticle-based oligonucleotide delivery encompasses the fundamental aspects of nanotechnology in delivery systems, various classes of oligonucleotides, and the growing field of ON-based therapeutics. These ON-based therapeutics are utilized to target specific genetic sequences within cells, offering promising avenues for treating various diseases by regulating gene expression or interfering with specific cellular processes. The integration of nanotechnology in delivery systems offers several advantages, given their intricate systems. Being a diverse class of agents, oligonucleotides provide a wide range of potential owed to each class of agents that support therapeutic interventions. Oligonucleotide-based platforms have demonstrated their versatility in molecular targeting and intervention strategies. Moreover, the complexities and delivery challenges in oligonucleotide therapeutics are expected to be overcome by the application of nanotechnology-based platforms.Because nanoparticles can overcome biological barriers and improve bioavailability, stability, and specificity, their role in developing oligonucleotide delivery systems is greatly valued. The innovative solutions facilitated by nanoparticles are efficient strategies to address the arduous barriers. These strategies beat obstacles like enzymatic degradation, cellular uptake, and immune response, which in turn paves the way for enhanced therapeutic efficacy. This review paper intends to explore the various applications of nanoparticle-mediated oligonucleotide delivery in a variety of diseases. It outlines the promising growth of therapies enabled by these systems, extending from cancer to genetic disorders, neurodegenerative diseases, etc. We have underscored the pivotal role of nanoparticle-based delivery systems in uncovering the full potential of oligonucleotide therapeutics, thereby fostering advancements in precision medicine and targeted therapies.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-06-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"141452568","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
The Dilemma of Insulin Delivery into the Brain: A Comprehensive Review. 胰岛素进入大脑的困境:全面回顾。
Pub Date : 2024-06-20 DOI: 10.2174/0115672018305677240611080910
Hooman Hatami, Vahid Reza Askari, Vafa Baradaran Rahimi, Md Saquib Hasnain, Amit Kumar Nayak

Insulin is a peptide hormone that is essential for regulating body homeostasis. Furthermore, it is involved in various neurological functions such as memory, behaviors, and cognition. The ubiquitous distribution of insulin receptors on various brain cells, such as neurons, microglia, astrocytes, and oligodendrocytes, and their differential localization across various brain regions, including the hippocampus, hypothalamus, and olfactory bulb, collectively underscore the crucial involvement of insulin in the modulation of cerebral functions. Along with ageing, in some pathological conditions such as diabetes and brain insulin resistance, the need for exogenous insulin is felt to compensate for insulin deficiency. In these cases, the biggest obstacle to the delivery of insulin to the brain is the blood-brain barrier (a physical barrier consisting of endothelial cells with tight junctions), which prevents the direct entry of most substances possessing high molecular weight, like insulin, into the brain. Therefore, different delivery methods have been proposed by researchers for insulin delivery that directly or indirectly cause the transfer of insulin to the brain. Some of these methods lack high efficiency and cause many side effects for the patient. In this regard, many new technologies have come to the aid of researchers and have introduced more effective delivery strategies, including the use of nanocarriers. Despite the promising outcomes demonstrated in the experimental models, the utilization of these techniques in human studies remains at a nascent stage and necessitates further comprehensive investigation. This review article aims to examine the diverse methods of insulin administration to the brain by gathering extensive information on insulin and its obstacles to brain delivery.

胰岛素是一种肽类激素,对调节体内平衡至关重要。此外,它还参与各种神经功能,如记忆、行为和认知。胰岛素受体在神经元、小胶质细胞、星形胶质细胞和少突胶质细胞等各种脑细胞上的分布无处不在,它们在海马、下丘脑和嗅球等不同脑区的定位也各不相同,这些都凸显了胰岛素在调节大脑功能方面的重要作用。随着年龄的增长,在某些病理情况下,如糖尿病和脑胰岛素抵抗,需要外源性胰岛素来弥补胰岛素的不足。在这些情况下,将胰岛素输送到大脑的最大障碍是血脑屏障(由具有紧密连接的内皮细胞组成的物理屏障),它阻止了大多数具有高分子量的物质(如胰岛素)直接进入大脑。因此,研究人员提出了不同的胰岛素输送方法,直接或间接地将胰岛素输送到大脑。其中一些方法效率不高,而且会对病人产生许多副作用。在这方面,许多新技术为研究人员提供了帮助,推出了更有效的给药策略,包括使用纳米载体。尽管在实验模型中显示出了良好的效果,但在人体研究中使用这些技术仍处于初级阶段,有必要进行进一步的全面调查。这篇综述文章旨在通过收集有关胰岛素及其脑部给药障碍的广泛信息,研究脑部给药胰岛素的各种方法。
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引用次数: 0
24 Factorial Design Formulation Optimization and In vitro Characterization of Desloratadine Nanosuspension Prepared Using Antisolvent Precipitation. 24 采用抗溶剂沉淀法制备的地氯雷他定纳米悬浮液的因子设计配方优化和体外表征
Pub Date : 2024-06-11 DOI: 10.2174/0115672018312715240604054857
Mohamed T El-Sebaiy, Mohammad H Alyami, Hamad S Alyami, Mohammad Amjad Kamal, Noura Eissa, Gehan Balata, Hanan El-Nahas

Introduction: Desloratadine, a second-generation antihistaminic drug, is poorly watersoluble and requires amelioration of the dissolution rate to improve its pharmacokinetics properties.

Method: This study investigated the impact of polymer, surfactant types, and concentration on the particle size, zeta potential, and dissolution efficiency of nanosuspensions formulated through the solvent antisolvent precipitation method. To optimize the delivery of Desloratadine nanosuspension, we used Minitab software and a 4-factor, 2-level full factorial design. Physicochemical properties and drug release studies were conducted to evaluate the suggested nanosuspension formulations. The optimization goals included minimizing particle size and zeta potential while maximizing dissolution efficiencies.

Result: The selected optimal nanosuspension demonstrated favourable values, including a particle size of 478.63 ± 15.67 nm, a zeta potential of -36.24 ± 3.21 mV, and dissolution efficiencies in double distilled water and buffer of 90.29 ± 3.75 % and 93.70 ± 3.67 %, respectively. The optimized formulation was subjected to additional analysis using X-ray powder diffraction (XPRD), scanning and transmission electron microscopy (SEM and TEM), and Fourier-transform infrared spectroscopy (FTIR).

Conclusion: The optimized nanosuspension formulation also underwent further studies under optimal lyophilization conditions, revealing the effectiveness of mannitol as a cryoprotectant at a concentration of 8%.

简介地氯雷他定是一种第二代抗组胺药物,水溶性较差,需要改善溶出率以提高其药代动力学特性:本研究探讨了聚合物、表面活性剂类型和浓度对通过溶剂反沉淀法配制的纳米悬浮剂的粒度、ZETA电位和溶解效率的影响。为了优化地氯雷他定纳米悬浮剂的给药,我们使用了 Minitab 软件和 4 因子 2 级全因子设计。对建议的纳米悬浮剂配方进行了理化性质和药物释放研究。优化目标包括最小化粒度和 zeta 电位,同时最大化溶出效率:结果:选定的最佳纳米悬浮液表现出良好的数值,包括粒径为 478.63 ± 15.67 nm,zeta 电位为 -36.24 ± 3.21 mV,在双蒸馏水和缓冲液中的溶出效率分别为 90.29 ± 3.75 % 和 93.70 ± 3.67 %。对优化后的配方还进行了 X 射线粉末衍射(XPRD)、扫描和透射电子显微镜(SEM 和 TEM)以及傅立叶变换红外光谱(FTIR)分析:结论:优化后的纳米悬浮剂配方还在最佳冻干条件下进行了进一步研究,结果表明甘露醇浓度为 8%时可有效用作低温保护剂。
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引用次数: 0
Frontiers of Plant-derived Exosomes from Research Methods to Pharmaceutical Applications in Plant-based Therapeutics 从研究方法到植物治疗药物应用的植物外泌体前沿。
Pub Date : 2024-06-11 DOI: 10.2174/0115672018305953240606063911
Wenshang Fu, Pingli Zhang, Wei Wang, Mengdie Du, Rui Ni, Yongshun Sun

Exosomes have emerged as critical mediators of intercellular communication and various physiological processes between cells and their environment. These nano-sized vesicles have been extensively investigated and confirmed to exhibit multifunctionality in animal systems. In particular, they participate in intercellular signaling, influence disease progression, and exhibit biological activity. However, Plant-Derived Exosomes (PDEs), especially therapeutic PDEs, have received relatively limited attention in the past few decades. Recent studies have demonstrated that PDEs are involved in signaling molecule transport in addition to intercellular communication, as they serve as functional molecules in the cellular microenvironment. This characteristic highlights the immense potential of PDEs for a wide array of applications, including antioxidation, anti-inflammation, tumour cell elimination, immune modulation, and tissue regeneration. In addition, PDEs hold substantial promise as efficient drug carriers, enhancing the stability and bioavailability of therapeutic agents and consequently enabling targeted delivery to specific cells or tissues. Therefore, PDEs may serve as effective tools for drug delivery and the treatment of various diseases. This comprehensive review provides an overview of recent studies on therapeutic PDEs, focusing on their extraction, isolation, characterization methods, biological activities, and application prospects. It summarises the research progress of exosome-like nanovesicles derived from medicinal plants, with a specific emphasis on traditional Chinese medicine, and highlights their importance in disease treatment and nanoparticle delivery. The main objective is to accelerate the clinical translation of these nanovesicles while providing novel approaches and methodologies for the research and development of innovative drugs.

外泌体已成为细胞间通信以及细胞与其环境之间各种生理过程的关键媒介。这些纳米大小的囊泡已被广泛研究,并被证实在动物系统中表现出多功能性。特别是,它们参与细胞间信号传递、影响疾病进展并表现出生物活性。然而,在过去几十年中,植物衍生外泌体(PDEs),尤其是治疗性PDEs受到的关注相对有限。最近的研究表明,除细胞间通信外,PDEs 还参与信号分子的转运,因为它们是细胞微环境中的功能分子。这一特性凸显了多羟基二苯醚在抗氧化、抗炎、消除肿瘤细胞、免疫调节和组织再生等广泛应用中的巨大潜力。此外,多溴联苯醚有望成为高效的药物载体,提高治疗药物的稳定性和生物利用度,从而实现向特定细胞或组织的靶向给药。因此,PDEs 可作为药物输送和治疗各种疾病的有效工具。本综述概述了近期有关治疗用多肽酶的研究,重点介绍了多肽酶的提取、分离、表征方法、生物活性和应用前景。它总结了从药用植物中提取的外泌体纳米颗粒的研究进展,特别强调了传统中药,并强调了它们在疾病治疗和纳米颗粒递送方面的重要性。主要目的是加速这些纳米颗粒的临床转化,同时为创新药物的研发提供新的途径和方法。
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引用次数: 0
Nanovesicles as Potential Carriers for Delivery of Antiviral Drugs: A Comprehensive Review. 纳米颗粒作为抗病毒药物的潜在载体:全面综述。
Pub Date : 2024-06-06 DOI: 10.2174/0115672018313783240603114509
Sabitri Bindhani, Amit Kumar Nayak

Different nanocarriers-based strategies are now extensively being used as an important strategy for improving drug efficacy and responsiveness, reducing toxicity issues related to drugs and harmful side effects, and overcoming the numerous significant difficulties related to absorption and bioavailability. Amongst different nanocarriers, nanovesicles are excellent and versatile systems for effectively delivering biomolecules, drugs, and targeted ligand distribution and location. Nanovesicles are nanosized self-assembling spherical capsules with an aqueous core and one/more lipid(s) layers. Several synthetic nanovesicles have been developed and investigated for their prospective uses in delivering drugs, proteins, peptides, nutrients, etc. Important procedures for nanovesicle manufacturing are thin-film hydration, unshaken method, ethanol injection, ether injection, proliposomes, freeze-drying, hot method, cold method, reverse-phase evaporation, and ultrasonication. Liposomes, liposomes, ethosomes, exosomes, and transferosomes (elastic vesicles) are the nonvesicular candidates extensively investigated to deliver antiviral drugs. This review article comprehensively reviews different nanovesicles, their compositions, manufacturing, and applications as potential carriers for effectively delivering different antiviral drugs to treat viral diseases.

目前,各种基于纳米载体的策略正被广泛用作提高药物疗效和反应性、减少药物毒性问题和有害副作用,以及克服与吸收和生物利用度有关的诸多重大难题的重要策略。在各种纳米载体中,纳米微粒是有效传递生物大分子、药物、靶向配体分布和定位的优秀多功能系统。纳米囊泡是一种纳米级的自组装球形胶囊,具有水性核心和一层或多层脂质。目前已开发出多种合成纳米微粒,并对其在输送药物、蛋白质、肽、营养物质等方面的应用前景进行了研究。制造纳米微粒的重要方法有薄膜水合法、未摇动法、乙醇注射法、乙醚注射法、脂质体、冷冻干燥法、热法、冷法、反相蒸发法和超声波法。脂质体、脂质体、乙体、外泌体和转运体(弹性囊泡)是被广泛研究用于递送抗病毒药物的非囊泡候选物质。这篇综述文章全面评述了不同的纳米微粒、其组成、制造和应用,它们是有效递送不同抗病毒药物以治疗病毒性疾病的潜在载体。
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引用次数: 0
Formulation and Characterization of Triamcinolone Acetonide Acetate-Loaded Microspheres Prepared by a Static Mixing Technique. 采用静态混合技术制备的醋酸曲安奈德微球的配方与表征
Pub Date : 2024-06-05 DOI: 10.2174/0115672018302129240603052316
Huan-Huan Du, Li-Rong Wang, Xin-Hong Wu, Xue-Ai Liu, Ming-Wei Huo, Xiang-Xiang Huang, Ling-Zhi Shi, Yawen Liu, Min Tang, Li-Li Shi, Qing-Ri Cao

Purpose: Reproducibility and scale-up production of microspheres through spray drying present significant challenges. In this study, biodegradable microspheres of Triamcinolone Acetonide Acetate (TAA) were prepared using a novel static mixing method by employing poly( lactic-co-glycolic acid) (PLGA) as the sustained-release carrier.

Methods: TAA-loaded microspheres (TAA-MSs) were prepared using a static mixing technique. The PLGA concentration, polyvinyl alcohol concentration (PVA), phase ratio of oil/water, and phase ratio of water/solidification were optimized in terms of the particle size, drug loading (DL), and encapsulation efficiency (EE) of TAA-MSs. The morphology of TAA-MSs was examined using Scanning Electron Microscopy (SEM), while the physicochemical properties were evaluated through X-ray diffraction (XRD), Differential Scanning Calorimetry (DSC), and Fourier Transform Infrared Spectroscopy (FT-IR). The in vitro release of TAA-MSs was compared to that of the pure drug (TAA) using a water-bath vibration method in the medium of pH 7.4 at 37°C.

Results: The formulation composition and preparation condition for the preparation of TAA-MSs were optimized as follows: the PLGA concentration was 1%, the phase ratio of oil(dichloromethane) /water (PVA solution) was 1:3, the phase ratio of water (PVA solution)/solidification was 1:2. The optimized TAA-MSs displayed spherical particles with a size range of 30-70 μm, and DL and EE values of 27.09% and 98.67%, respectively. Moreover, the drug-loaded microspheres exhibited a significant, sustained release, with 20% of the drug released over a period of 28 days. The XRD result indicated that the crystalline form of TAA in microspheres had been partly converted into the amorphous form. DSC and FT-IR results revealed that some interactions between TAA and PLGA occurred, indicating that the drug was effectively encapsulated into PLGA microspheres.

Conclusion: TAA-loaded PLGA microspheres have been successfully prepared via the static mixing technique with enhanced EE and sustained-release manner.

目的:通过喷雾干燥法生产微球的可重复性和规模化生产面临重大挑战。本研究采用新型静态混合法制备了醋酸曲安奈德(TAA)生物可降解微球,并以聚乳酸-聚乙二醇酸(PLGA)作为缓释载体:方法:采用静态混合技术制备了负载TAA的微球(TAA-MSs)。从TAA-MSs的粒径、载药量(DL)和包封效率(EE)的角度优化了PLGA浓度、聚乙烯醇浓度(PVA)、油/水相比例和水/固相比例。使用扫描电子显微镜(SEM)检查了 TAA-MSs 的形态,并通过 X 射线衍射(XRD)、差示扫描量热仪(DSC)和傅立叶变换红外光谱(FT-IR)评估了其理化性质。在 pH 值为 7.4、温度为 37°C 的介质中,采用水浴振荡法比较了 TAA-MSs 与纯药物(TAA)的体外释放情况:制备TAA-MSs的配方组成和制备条件优化如下:PLGA浓度为1%,油(二氯甲烷)/水(PVA溶液)相比为1:3,水(PVA溶液)/固化相比为1:2。优化后的 TAA-MS 呈球形颗粒,粒径范围为 30-70 μm,DL 值和 EE 值分别为 27.09% 和 98.67%。此外,载药微球表现出显著的持续释放性,在 28 天内释放了 20% 的药物。XRD 结果表明,微球中的 TAA 晶体已部分转化为无定形形式。DSC 和傅立叶变换红外光谱结果表明,TAA 与 PLGA 之间发生了一些相互作用,这表明药物被有效地包裹在 PLGA 微球中:结论:通过静态混合技术成功制备了负载 TAA 的 PLGA 微球,其 EE 和缓释效果均有所提高。
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Current drug delivery
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