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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。
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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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引用次数: 0
Characterization and In vivo Evaluation of Polymorphic Valnemulin Hydrogen Fumarate. 多态富马酸缬氨胆碱的特性和体内评估
Pub Date : 2024-06-05 DOI: 10.2174/0115672018289236240530095059
Zhu Xinle, Zhang Li, Li Jian, Zhao Hui, Gu Jinhua, Wang Hejia

Aims: In the present study, a valnemulin hydrogen fumarate prodrug was characterized, its stability was compared with valnemulin hydrochloride, and the efficacy was evaluated in Actinobacillus pleuropneumoniae-induced pneumonia in mice.

Method: Optical microscopy, X-ray powder diffraction, infrared spectroscopy, and hydrogen nuclear magnetic resonance spectroscopy were used to study the physical and chemical properties of the prodrug. The thermal stability was investigated in comparison with valnemulin hydrochloride to improve the preparation process of valnemulin hydrogen fumarate soluble powder and maximize its drug effect. Additionally, the efficacy of valnemulin hydrogen fumarate was evaluated in a challenge-treatment trial in mice using an in vitro antimicrobial susceptibility test.

Results: The valnemulin hydrogen fumarate had high crystallinity. After light irradiation for 20 days, valnemulin hydrogen fumarate did not degrade, whereas valnemulin hydrochloride did. These results showed that the valnemulin hydrogen fumarate was stable. At the same dose in drinking water, the valnemulin hydrogen fumarate was more effective than the reference drug (tiamulin fumarate) in an Actinobacillus pleuropneumoniae challenge-treatment trial.

Conclusion: Valnemulin hydrogen fumarate shows excellent potential for application as a veterinary drug.

目的:本研究对富马酸氢缬氨噻肟原药进行了表征,比较了其与盐酸缬氨噻肟的稳定性,并评估了其在胸膜肺炎放线杆菌诱导的小鼠肺炎中的疗效:方法:利用光学显微镜、X 射线粉末衍射、红外光谱和氢核磁共振光谱研究了原药的物理和化学特性。与盐酸缬奈莫林相比,研究了其热稳定性,以改进富马酸缬奈莫林可溶性粉末的制备工艺,最大限度地发挥其药效。此外,还利用体外抗菌药敏感性试验对富马酸缬奈莫林进行了小鼠挑战治疗试验,以评估其疗效:富马酸缬奈莫林的结晶度很高。在光照 20 天后,富马酸缬奈莫林没有降解,而盐酸缬奈莫林却降解了。这些结果表明富马酸氢缬氨醇是稳定的。在胸膜肺炎放线杆菌挑战治疗试验中,富马酸缬奈莫林在饮用水中的相同剂量下比参考药物(富马酸替莫林)更有效:结论:富马酸缬氨噻肟酯显示出作为兽药应用的巨大潜力。
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引用次数: 0
Mesothelin-Mediated Paclitaxel Phase-Shifted Nanodelivery System for Molecular Ultrasound Imaging and Targeted Therapy Potential in Ovarian Cancer. 间皮素介导的紫杉醇相移纳米给药系统用于卵巢癌的分子超声成像和靶向治疗。
Pub Date : 2024-06-05 DOI: 10.2174/0115672018300502240530064139
Yujie Wan, Li Luo, Xinzhi Xu, Qihuan Fu, Ying Li, Kaifeng Huang, Hang Zhou, Fang Li

Background: Ovarian cancer presents a substantial risk to women's health and lives, with early detection and treatment proving challenging. Targeted nanodelivery systems are viewed as a promising approach to enhance the effectiveness of ovarian cancer treatment and ultrasonic imaging outcomes.

Objective: A phase-shifted nanodelivery system (NPs) loaded with paclitaxel (PTX) and further conjugated with avidin (Ab) was studied, with the goal of investigating the effects of targeted nanodelivery strategies on the in vitro therapeutic efficacy and ultrasonic imaging of ovarian cancer. This study provides a foundation for future in vivo treatments utilizing this approach.

Methods: PTX-NPs were prepared using the single water-in-oil (O/W) emulsion solvent evaporation method, with avidin coupling achieved through biotin-avidin affinity. The encapsulation efficiency and release profile of PTX were analyzed using UV spectrophotometry. The phase-shift properties of the Ab-PTX-NPs delivery system were evaluated, and the targeting efficiency, cytotoxicity against SKOV3 cells, and in vivo biosafety of various nanodelivery systems were assessed.

Results: The prepared nanodelivery system showed a stable and uniform structure with a good particle size distribution and exhibited favorable release characteristics under ultrasound exposure. In vitro experiments revealed that the nanodelivery system displayed excellent targeting and cytotoxic effects against SKOV3 cells, indicating the potential of the Ab-PTX-NPs delivery system for targeted ovarian cancer therapy. In vivo safety studies demonstrated the high biosafety of the prepared nanodelivery system.

Conclusion: A novel nanodelivery system was developed, and the experimental results obtained provide a solid experimental basis for further research on in vivo ultrasound molecular imaging technology, offering new insights into targeted ultrasound molecular imaging and the treatment of ovarian cancer.

背景:卵巢癌对妇女的健康和生命构成巨大风险,早期检测和治疗具有挑战性。靶向纳米给药系统被认为是提高卵巢癌治疗效果和超声波成像结果的一种有前途的方法:研究了一种负载紫杉醇(PTX)并进一步与阿维丁(Ab)共轭的相移纳米给药系统(NPs),旨在探讨靶向纳米给药策略对卵巢癌体外疗效和超声成像的影响。这项研究为未来利用这种方法进行体内治疗奠定了基础:方法:采用单一油包水(O/W)乳液溶剂蒸发法制备 PTX-NPs,并通过生物素-阿维蛋白亲和力实现阿维蛋白偶联。采用紫外分光光度法分析了 PTX 的包封效率和释放曲线。评价了 Ab-PTX-NPs 给药系统的相移特性,并评估了各种纳米给药系统的靶向效率、对 SKOV3 细胞的细胞毒性和体内生物安全性:结果:制备的纳米给药系统结构稳定均匀,粒度分布良好,在超声暴露下表现出良好的释放特性。体外实验显示,该纳米给药系统对SKOV3细胞具有良好的靶向性和细胞毒性作用,表明Ab-PTX-NPs给药系统具有卵巢癌靶向治疗的潜力。体内安全性研究表明所制备的纳米给药系统具有很高的生物安全性:结论:该研究开发了一种新型纳米给药系统,其实验结果为进一步研究体内超声分子成像技术提供了坚实的实验基础,为靶向超声分子成像和卵巢癌治疗提供了新的思路。
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引用次数: 0
Niosome-Based Hydrogel of Quince Extract: A Promising Strategy for Expedited Full-thickness Wound Healing in Rat. 基于榅桲提取物的水凝胶:加速大鼠全厚伤口愈合的有效策略
Pub Date : 2024-06-04 DOI: 10.2174/0115672018282735240528072715
Pedram Ebrahimnejad, Paria Fadaee Heydarabadi, Fereshteh Talebpour Amiri, Fatemeh Mirzaee, Melika Ahmadi, Somayeh Shahani

Background: The regeneration of tissue damage involves a series of molecular and cellular events that can be mediated by various natural compounds. Recent studies have highlighted the anti-inflammatory, anti-ulcer, and skin-protecting properties of Cydonia oblonga (Quince), which are mainly attributed to phenolic compounds. These compounds may have some drawbacks when targeting wound applications, including low bioavailability at the wound site. Moreover, to overcome these limitations, surfactant-based nanovesicular systems have been developed as carriers of such compounds for wound healing.

Objective: This study aimed to highlight the possible therapeutic potential of niosome-based hydrogel from Quince extract to stabilize and deliver the related bioactive compounds to full-thickness wounds in rats.

Methods: The niosomal hydrogel was prepared using a thin-film hydration method with the fruit extract (70% methanol). The formulation was optimized by evaluating size, zeta potential, dispersion index, and drug encapsulation efficiency. Full-thickness wounds were created on the dorsal cervical area of Wistar rats, and histopathological analysis of biopsy specimens was conducted on the 12th day of treatment.

Results: Under the study conditions, niosomal hydrogel displayed good physicochemical stability. Histopathological findings demonstrated that niosomal gel promoted angiogenesis, fibroblast maturation, collagen deposition, keratinization, and epidermal layer formation more effectively than control and hydrogel base. Furthermore, niosomal gel treatment markedly reduced inflammation. The total phenol concentration was determined to be 13.34 ± 0.90 mg gallic acid equivalents per gram of dried extract.

Conclusion: The niosomal hydrogel containing C. oblonga extract shows potential as a novel approach for wound healing, warranting further investigation in this field.

背景:组织损伤的再生涉及一系列分子和细胞事件,这些事件可由各种天然化合物介导。最近的研究强调了榅桲(Cydonia oblonga)的抗炎、抗溃疡和皮肤保护特性,这些特性主要归因于酚类化合物。这些化合物在针对伤口应用时可能存在一些缺点,包括在伤口部位的生物利用率较低。此外,为了克服这些局限性,人们开发了基于表面活性剂的纳米囊泡系统,作为此类化合物的载体,用于伤口愈合:本研究旨在强调从榅桲提取物中提取的基于niosome的水凝胶可能具有的治疗潜力,以稳定相关生物活性化合物并将其输送到大鼠的全厚伤口中:方法:采用薄膜水合法,用榅桲提取物(70%甲醇)制备榅桲水凝胶。通过评估尺寸、ZETA电位、分散指数和药物封装效率,对配方进行了优化。在 Wistar 大鼠的颈背部位造成全厚伤口,并在治疗的第 12 天对活检标本进行组织病理学分析:结果:在研究条件下,水凝胶具有良好的理化稳定性。组织病理学研究结果表明,与对照组和水凝胶基质相比,尼泊金凝胶能更有效地促进血管生成、成纤维细胞成熟、胶原沉积、角质化和表皮层形成。此外,尼索米尔凝胶还能明显减轻炎症反应。经测定,每克干燥提取物的总酚浓度为 13.34 ± 0.90 毫克没食子酸当量:含有 C. oblonga 提取物的透明质水凝胶显示出作为伤口愈合新方法的潜力,值得在该领域开展进一步研究。
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引用次数: 0
Recent Advancement of Nanotheranostics in Cancer Applications. 纳米otheranostics 在癌症应用中的最新进展。
Pub Date : 2024-05-29 DOI: 10.2174/0115672018307617240514092110
Suphiya Parveen, R Abira, Safal Paikray, Liza Sahoo, Nigam Sekahr Tripathy, Fahima Dilnawaz

The field of nanomedicine shows promising implications in the concurrent delivery of therapeutic and diagnostic (theranostics) compounds in a single platform. Nanotheranostics is incredibly promising since it offers simultaneous non-invasive disease detection and treatment together with the exciting ability to track drug release and distribution in real-time, thereby forecasting and evaluating the efficacy of the therapy. The cancer theranostic approach improves the cancer prognosis safely and effectively. Common classes of nanoscale biomaterials, including magnetic nanoparticles, quantum dots, upconversion nanoparticles, mesoporous silica nanoparticles, carbon- based nanoparticles, and organic dye-based nanoparticles, have demonstrated enormous potential for theranostic activity. The need for improved disease detection and enhanced chemotherapeutic treatments, together with realistic considerations for clinically translatable nanomaterials will be key driving factors for theranostic agent research shortly. The developments of precision theranostic nanomaterials are employed in imaging systems like, MRI, PET, and SPECT with multifunctional ability. In this review, different nanoparticles/nanomaterials that are used/developed for theranostic activity are discussed.

纳米医学领域显示出在单一平台上同时提供治疗和诊断(治疗)化合物的广阔前景。纳米治疗学具有令人难以置信的前景,因为它能同时进行非侵入性疾病检测和治疗,并能实时跟踪药物的释放和分布,从而预测和评估疗效。癌症治疗方法能安全有效地改善癌症预后。磁性纳米粒子、量子点、上转换纳米粒子、介孔二氧化硅纳米粒子、碳基纳米粒子和有机染料基纳米粒子等常见的纳米级生物材料已显示出巨大的治疗活性潜力。改善疾病检测和提高化疗效果的需求,以及对可临床转化的纳米材料的现实考虑,将成为近期治疗剂研究的关键驱动因素。精确治疗纳米材料的开发应用于成像系统,如具有多功能能力的 MRI、PET 和 SPECT。本综述讨论了用于/开发治疗活性的不同纳米颗粒/纳米材料。
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引用次数: 0
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Current drug delivery
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