Current drug delivery最新文献

Enhanced Therapeutic Potential of Liposome-Coated Bushen Jianpi Recipe for Hepatocellular Carcinoma 增强脂质体包裹的釜陈陈皮配方对肝细胞癌的治疗潜力

IF 2.4 4区医学 Q2 PHARMACOLOGY & PHARMACY

Current drug delivery

Pub Date : 2024-09-18 DOI: 10.2174/0115672018318595240902095514

Siqi Feng, Yi Zhong, Yabin Li, Shiying Li, Yun Li, Zhangjie Zhou, Zhonghua Wu, Tingting Wu

Objective: Hepatocellular carcinoma (HCC) poses a major healthcare burden globally. Traditional Chinese medicine formula Bushen Jianpi (BSJP) recipe shows inhibitory effects on HCC but suffers from low bioavailability. This study aims to develop a BSJP-loaded liposome (BSJP@Lip) for targeted HCC treatment. Methods: BSJP@Lip was prepared using a microfluidic device. Particle characterization included size, morphology, drug loading, encapsulation efficiency, and release kinetics analysis. In vitro cytotoxicity, cellular uptake, apoptosis, and protein expression were evaluated in hepG2, Smmc-7721, and hepa 1-6 hepatic cancer cell lines treated with BSJP@Lip. Results: BSJP@Lip nanoparticles showed a uniform spherical shape with an average size of 50 nm and zeta potential at around -2.24 mV. They significantly inhibited cell viability and induced apoptosis in a dose-dependent manner compared with traditional decoction formulations. Enhanced cellular uptake of BSJP@Lip increased the expression of proinflammatory factors IL-18 and NLRP3. Conclusion: BSJP@Lip nanoparticles were found to be efficiently internalized by hepatic cancer cell lines, resulting in a dose-dependent inhibition of cell viability and induction of apoptosis. This effect was accompanied by the upregulation of IL-18 and NLRP3.

目的：肝细胞癌（HCC）是全球主要的医疗负担。传统中药配方布参建皮（BSJP）对 HCC 有抑制作用，但生物利用度较低。本研究旨在开发一种用于靶向治疗 HCC 的 BSJP 脂质体（BSJP@Lip）。研究方法使用微流控装置制备 BSJP@Lip。颗粒表征包括尺寸、形态、载药量、包封效率和释放动力学分析。在用 BSJP@Lip 处理的 hepG2、Smmc-7721 和 hepa 1-6 肝癌细胞系中，对体外细胞毒性、细胞摄取、细胞凋亡和蛋白表达进行了评估。结果显示BSJP@Lip 纳米粒子呈均匀球形，平均粒径为 50 nm，zeta 电位约为 -2.24 mV。与传统的煎煮制剂相比，BSJP@Lip 纳米颗粒能以剂量依赖性的方式明显抑制细胞活力并诱导细胞凋亡。增强细胞对 BSJP@Lip 的吸收会增加促炎因子 IL-18 和 NLRP3 的表达。结论研究发现，BSJP@Lip 纳米颗粒可被肝癌细胞株有效内化，从而导致剂量依赖性的细胞活力抑制和细胞凋亡诱导。这种效应伴随着 IL-18 和 NLRP3 的上调。

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引用次数: 0

Lignin Nanoparticles as pH-responsive Nanocarriers for Gastric-Irritant Oral Drug Aspirin 木质素纳米颗粒作为胃刺激性口服药物阿司匹林的 pH 值响应型纳米载体

IF 2.4 4区医学 Q2 PHARMACOLOGY & PHARMACY

Current drug delivery

Pub Date : 2024-09-18 DOI: 10.2174/0115672018318035240910050003

Tahmidul Islam Aquib, Sheikh Manjura Hoque, Mohammad Helal Uddin

Introduction: Although lignin is one of the most naturally abundant biopolymers, the overall status of its utilization has long been subpar. The ability of Lignin to readily self-assemble into nanoparticles, along with its good biocompatibility and minimal toxicity, makes it a perfect agent for nanocarriers and drug delivery. Method: Hence, in this study, we have attempted to examine lignin nanoparticles (LNPs) as an efficient pH-responsive nanocarrier for gastric-irritant oral NSAID, aspirin. Alkali lignin (AL) was extracted from rice straw via alkaline treatment, and the lignin nanoparticles were synthesized from lignin using the acid precipitation method. The average particle size was 201.37 ± 1.20 nm, and the synthesized LNPs exhibited a spherical shape and smooth outer surface along with high polydispersity (PDI= 0.284 ± 0.012). The LNPs showed moderate hemocompatibility during in vitro hemolysis studies. The nanoparticles presented nearly similar chemical structures to the AL from which they were developed, and the FT-IR absorption spectra confirmed the similarity of this chemical structure to the LNPs and AL. Aspirin was successfully loaded into the LNPs with a satisfactory drug loading value of 39.12 ± 1.50 and an excellent encapsulation efficiency value of 91.44 ± 0.59. Results: Finally, the LNPs were capable of protecting the loaded drug at the acidic pH of the stomach (1.2) with just 29.20% release of the loaded aspirin after 10 h of observation in vitro. Contrarily, the LNPs were capable of rapidly releasing the aspirin at the basic pH of the intestine (7.4) with nearly 90% release of the loaded drug after 10 h observation in vitro. The basic pH of the intestine might lead to gradual dissociation of the LNPs followed by swift release of the loaded cargo. Conclusion: These findings substantiate that the LNPs carry the potential to be an apt and safe nanocarrier for oral drugs like aspirin as well as parenteral drugs, and LNPs can be utilized as an efficient alternative to enteric coating.

简介：虽然木质素是天然含量最高的生物聚合物之一，但长期以来其整体利用状况一直不尽如人意。木质素能够很容易地自组装成纳米颗粒，而且具有良好的生物相容性和极低的毒性，因此是纳米载体和药物输送的理想剂型。研究方法因此，在本研究中，我们尝试将木质素纳米颗粒（LNPs）作为一种有效的 pH 响应型纳米载体，用于胃刺激性口服非甾体抗炎药阿司匹林。研究人员通过碱性处理从稻草中提取了碱木素（AL），并采用酸沉淀法从木质素中合成了木质素纳米颗粒。合成的木质素纳米粒子平均粒径为 201.37 ± 1.20 nm，呈球形，外表面光滑，具有较高的多分散性（PDI= 0.284 ± 0.012）。在体外溶血研究中，LNPs 表现出适度的血液相容性。这些纳米颗粒的化学结构与 AL 相似，傅立叶变换红外吸收光谱证实了 LNPs 和 AL 的化学结构相似。阿司匹林被成功装载到 LNPs 中，药物装载值为 39.12 ± 1.50，非常令人满意，封装效率值为 91.44 ± 0.59。结果最后，LNPs 能够在胃的酸性 pH 值（1.2）下保护所负载的药物，体外观察 10 小时后，所负载的阿司匹林仅释放了 29.20%。相反，在肠道的碱性 pH 值（7.4）下，LNPs 能够快速释放阿司匹林，体外观察 10 小时后，负载的药物释放了近 90%。肠道的碱性 pH 值可能会导致 LNPs 逐渐解离，然后迅速释放所负载的货物。结论这些研究结果证明，LNPs 有潜力成为阿司匹林等口服药物和肠外药物的一种合适而安全的纳米载体，LNPs 可作为肠道包衣的一种有效替代品。

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引用次数: 0

Exploring the Insights on Exosomes and their Utility in Treating Ophthalmic Disease: Delving into the Clinical Approval and Present Trials 探索外泌体及其在治疗眼科疾病中的作用：深入了解临床批准和当前试验

IF 2.4 4区医学 Q2 PHARMACOLOGY & PHARMACY

Current drug delivery

Pub Date : 2024-09-18 DOI: 10.2174/0115672018324046240905134931

Ashish Ranjan Dwivedi, Yogesh Murti, Pramod Rawat, Shriya Mahajan, Harsimrat Kandhari, Gaurav Joshi, Bhupinder Kumar

: Ophthalmic diseases include a wide array of conditions, each requiring individualized treatment approaches. In ophthalmic research and as therapeutics against potential pharmacological indications, several subtypes of exosomes (EVs) have been reconnoitered, mainly for their regenerative, neuroprotective, and anti-inflammatory characteristics. EVs are recently gaining wider attention as promising vehicles for therapies because of their natural participation in communication between cells and targeted delivery. These small vesicles, derived from cells, transport numerous molecules between cells, thus contributing advantages like low immunogenicity, stability, and the ability to target cells specifically. These inherent advantages of carrying the therapeutic cargo and enabling intercellular signaling make them a captivating avenue for progressing ophthalmic disease treatment options. While research is ongoing, and clinical applications are still emerging, several EV subtypes have shown promise for possible applications in addressing several ophthalmic diseases, such as glaucoma, age-related macular degenerative disorders, retinal degenerative disorders, and ocular inflammatory conditions.

:眼科疾病种类繁多，每种疾病都需要个性化的治疗方法。在眼科研究和针对潜在药理适应症的治疗中，已经发现了几种亚型的外泌体（EVs），主要用于再生、神经保护和抗炎。由于外泌体可自然参与细胞间的交流和靶向递送，因此作为有前景的治疗载体，外泌体最近正受到越来越广泛的关注。这些源自细胞的小囊泡可在细胞间运输多种分子，因此具有免疫原性低、稳定性强、可特异性靶向细胞等优点。这些固有的携带治疗货物和实现细胞间信号传递的优势，使它们成为眼科疾病治疗方案取得进展的迷人途径。虽然研究仍在进行，临床应用也在不断涌现，但有几种 EV 亚型已显示出有望应用于治疗几种眼科疾病，如青光眼、老年性黄斑变性疾病、视网膜变性疾病和眼部炎症。

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引用次数: 0

Lipid Nanoparticles as a Platform for miRNA and siRNA Delivery in Hepatocellular Carcinoma 将脂质纳米颗粒作为肝细胞癌中 miRNA 和 siRNA 的递送平台

IF 2.4 4区医学 Q2 Pharmacology, Toxicology and Pharmaceutics

Current drug delivery

Pub Date : 2024-05-03 DOI: 10.2174/0115672018292331240404070236

Gaidaa Dogheim, Sampath Chinnam, Mohamed T. Amralla

: Liver cancer is the sixth most common cancer and the fourth leading cause of death worldwide. Hepatocellular carcinoma (HCC) comprises 75-80% of liver cancer cases. Therapeutic strategies for HCC are available and have been shown to prolong survival but not treat HCC. Gene expression and regulation are responsible for the pathogenesis and progression of HCC. Altering these genetic networks can impact cellular behaviors and in turn cure HCC. Single-stranded and double-stranded non-coding ribonucleic acid known as microRNA and small interfering RNA, respectively have been investigated as possible therapeutic options. Currently, efficient delivery systems that ensure cell-specific targeting and efficient transfection into tumor cells are still under investigation. Viral vectors have been studied extensively, but immunogenicity hinders their use as delivery systems. Non-viral vectors which include inorganic, lipid, or polymeric nanoparticles are promising delivery systems. However, there are a lot of challenges during the formulation of such systems to ensure efficient and specific delivery. In vitro and in vivo studies have investigated different LNPs to deliver miRNA or siRNA. In this review, we highlight the role of LNPs as a delivery system for miRNA and siRNA in HCC in addition to the latest results achieved using this approach.

:肝癌是全球第六大常见癌症和第四大死亡原因。肝细胞癌（HCC）占肝癌病例的 75-80%。目前已有针对 HCC 的治疗策略，这些策略已被证明可延长 HCC 的生存期，但无法治疗 HCC。基因表达和调控是导致 HCC 发病和进展的原因。改变这些基因网络可影响细胞行为，进而治愈 HCC。单链和双链非编码核糖核酸（分别称为 microRNA 和小干扰 RNA）已被研究为可能的治疗方案。目前，确保细胞特异性靶向和高效转染肿瘤细胞的高效递送系统仍在研究之中。病毒载体已被广泛研究，但其免疫原性阻碍了其作为递送系统的使用。包括无机、脂质或聚合物纳米颗粒在内的非病毒载体是很有前景的递送系统。然而，在配制此类系统以确保高效和特异性递送的过程中存在许多挑战。体外和体内研究调查了不同的 LNPs 来递送 miRNA 或 siRNA。在这篇综述中，我们将重点介绍 LNPs 作为 miRNA 和 siRNA 的递送系统在 HCC 中的作用，以及使用这种方法所取得的最新成果。

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引用次数: 0

Applications of Inorganic Nanomaterials against Tuberculosis: A Comprehensive Review 无机纳米材料在结核病防治中的应用：全面综述

IF 2.4 4区医学 Q2 Pharmacology, Toxicology and Pharmaceutics

Current drug delivery

Pub Date : 2024-05-02 DOI: 10.2174/0115672018295247240426055330

Debabrata Ghosh Dastidar, Arnab Roy, Gourav Ghosh, Supratim Mandal

: Tuberculosis (TB) continues to pose a significant global health threat, with millions of new infections recorded annually. Current treatment strategies, such as Directly Observed Treatment (DOT), face challenges, including patient non-compliance and the emergence of drug-resistant TB strains. In response to these obstacles, innovative approaches utilizing inorganic/metallic nanomaterials have been developed to enhance drug delivery to target alveolar macrophages, where Mycobacterium tuberculosis resides. These nanomaterials have shown effectiveness against various strains of TB, offering benefits such as improved drug efficacy, minimized side effects, and sustained drug release at the infection site. This comprehensive review explores the applications of different metal nanoparticles, metal oxide nanoparticles, and metal-metal oxide hybrid nanoparticles in the management of TB, including multidrug-resistant (MDR) and extensively drug-resistant (XDR) strains. The synergistic effects of combining inorganic nanoparticles with conventional anti-TB drugs have demonstrated promising results in combating TB infections. Further research and development in this field hold great promise for overcoming the challenges faced in current TB therapy and improving patient outcomes.

:结核病（TB）继续对全球健康构成重大威胁，每年新增感染人数达数百万。目前的治疗策略，如直接观察治疗（DOT），面临着患者不依从和耐药结核菌株出现等挑战。为了应对这些障碍，人们开发了利用无机/金属纳米材料的创新方法，以加强针对肺泡巨噬细胞的药物输送，而肺泡巨噬细胞正是结核分枝杆菌的栖息地。这些纳米材料已显示出对各种结核菌株的有效性，具有提高药效、减少副作用和在感染部位持续释放药物等优点。本综述探讨了不同金属纳米粒子、金属氧化物纳米粒子和金属-金属氧化物混合纳米粒子在结核病治疗中的应用，包括耐多药（MDR）和广泛耐药（XDR）菌株。无机纳米粒子与传统抗结核药物的协同作用在抗结核感染方面取得了可喜的成果。该领域的进一步研究和开发为克服当前结核病治疗所面临的挑战和改善患者预后带来了巨大希望。

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引用次数: 0

Evaluation of Moringa Oleifera Leaf Extract for its In vitro Antibacterial Properties, Mechanism of Action, and In vivo Corneal Ulcer Healing Effects in Rabbits’ Eyes 评估辣木叶提取物的体外抗菌特性、作用机制和在兔子体内的角膜溃疡愈合效果

IF 2.4 4区医学 Q2 Pharmacology, Toxicology and Pharmaceutics

Current drug delivery

Pub Date : 2024-04-19 DOI: 10.2174/0115672018275561240228065755

Ayesha Bibi, Meenakshi dhanawat, Shahbaz Aman, Samrat Chauhan, Rishabh Chalotra, Somdutt Mujwar, Narinder Kaur, ChamasseHomary Maivagna, Sumeet Gupta

: M. oleifera is the most adapted tree species in different medicinal eco-systems and has resilience against climate changes. This multiple-use tree provides healthy foods, snacks, honey, and fuel. Besides this, it has immense promising applicationsby offering antimicrobial and antibacterial activities for targeted uses. This validates the court of Hippocrates that let food be the medicine and medicine be the food for which moringa qualifies. In view of this, the antioxidant and in vitro antibacterial potency of the hydro-ethanolic extract of M. oleifera was evaluated on clinically isolated multidrug-resistant strains of Staphylococcus aureus. Furthermore, in vivo, the healing response of M. oleifera extract was analysed on corneal ulcers induced in rabbit eyes infected with methicillin-resistant Staphylococcus aureus. TheM. oleifera extract exhibited exponential antioxidant activity. In-vitro antibacterial activity was evaluated by agar well diffusion assay showing zone of inhibition ranging from 11.05±0.36 to 20±0.40 mm at concentrations of 20, 40, 80, and 160 mg/ml, whereas, in our finding, no zone of inhibition was observed below 20 mg/ml concentration, which indicated that there is threshold limit below which the antibacterial activity of M. oleifera extract is not observed. Furthermore, continuous application of 3% and 5% M. oleifera extract (eye drop) four times a day for 14 consecutive days showed a significant healing response of the eyes of rabbits with corneal ulcers. These results suggest that M. oleifera extract could be a viable alternative to existing antibacterial therapies for corneal ulcers. Additionally, there is a possibility of commercial formulation of M. oleifera extract in the form of deliverable pharmaceutical products; therefore, it should be explored further.

:油橄榄是最适应不同药用生态系统的树种，具有抵御气候变化的能力。这种多用途树种可提供健康食品、零食、蜂蜜和燃料。此外，它还具有抗菌和抑菌活性，应用前景广阔。这印证了希波克拉底的观点，即让食物成为药物，让药物成为食物，而莫林葛就符合这一观点。有鉴于此，我们对油橄榄果实水乙醇提取物的抗氧化和体外抗菌效力进行了评估，该提取物适用于临床分离的金黄色葡萄球菌耐多药菌株。此外，还分析了 M. oleifera 提取物对兔眼感染耐甲氧西林金黄色葡萄球菌诱发的角膜溃疡的体内愈合反应。油橄榄提取物表现出指数级的抗氧化活性。通过琼脂井扩散试验评估了体外抗菌活性，结果表明，在 20、40、80 和 160 毫克/毫升浓度下，抑菌区范围为 11.05±0.36 至 20±0.40 毫米，而我们的研究结果表明，在 20 毫克/毫升浓度以下未观察到抑菌区，这表明油橄榄叶提取物的抗菌活性存在阈值。此外，连续 14 天每天四次滴用 3% 和 5%的油橄榄叶提取物（滴眼液），结果表明患有角膜溃疡的兔子的眼睛有明显的愈合反应。这些结果表明，油橄榄叶提取物可以替代现有的角膜溃疡抗菌疗法。此外，M. oleifera 提取物还有可能以可递送药品的形式进行商业化配制；因此，应该对其进行进一步的探索。

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引用次数: 0

Gold Nanoparticle-Based Drug Delivery System for the Diagnosis and Treatment of Bacterial Meningitis 用于诊断和治疗细菌性脑膜炎的基于金纳米粒子的给药系统

IF 2.4 4区医学 Q2 Pharmacology, Toxicology and Pharmaceutics

Current drug delivery

Pub Date : 2024-04-17 DOI: 10.2174/0115672018278607240405060054

Darsh Gautam, Vinay Pandit, Sanjay Kumar, Poonam Talwan, Tarun Sharma

: Managing bacterial pathogens in the central nervous system is an immense issue for researchers all around the globe. The problem of these infections remains throughout the population, regardless of the discovery of several possible medicines. The major obstacle to drug delivery is the BBB, but only a few medicines that fulfill demanding requirements can penetrate it. Considering inadequate antibiotic alternatives and the increasing development of resistance, it is more important than ever to find new approaches to address this worldwide problem. Medical nanotechnology has evolved as a cutting-edge and effective means of treating many of the most difficult CNS illnesses, including bacterial meningitis. Various metallic nanoparticles, such as gold, silver, and titanium oxide, have shown bactericidal potential. Gold nanoparticles have gotten a great deal of interest due to their excellent biocompatibility, simplicity of surface modification, and optical qualities. The current study described AuNP-based detection and therapy options against meningitis-- causing bacteria, including bacterial pathogens' mechanisms for crossing BBB and AuNPs' mode of Action against those bacteria. The current study looked into green synthesized bactericidal gold nanoparticles-based therapy techniques for diagnosing and intervening in bacterial meningitis. Nevertheless, more research is needed before these laboratory findings can be translated into therapeutic trials. Nonetheless, we can confidently assert that the knowledge acquired and addressed in this study will benefit neuro-nanotechnology researchers.

:管理中枢神经系统中的细菌病原体是全球研究人员面临的一个巨大问题。尽管已经发现了多种可能的药物，但这些感染问题在整个人群中依然存在。药物输送的主要障碍是生物BB，但只有少数符合要求的药物能够穿透生物BB。考虑到抗生素替代品的不足和抗药性的日益发展，寻找新的方法来解决这一世界性难题比以往任何时候都更加重要。医学纳米技术已发展成为治疗细菌性脑膜炎等许多最棘手的中枢神经系统疾病的尖端有效手段。金、银和氧化钛等各种金属纳米粒子已显示出杀菌潜力。金纳米粒子因其良好的生物相容性、简单的表面改性和光学特性而备受关注。本研究介绍了基于金纳米粒子的检测和治疗脑膜炎致病菌的方法，包括细菌病原体穿过 BBB 的机制和金纳米粒子对这些细菌的作用模式。本研究探讨了基于绿色合成的杀菌金纳米粒子的治疗技术，用于诊断和干预细菌性脑膜炎。不过，在将这些实验室研究成果转化为治疗试验之前，还需要进行更多的研究。尽管如此，我们可以自信地断言，这项研究中获得和解决的知识将使神经纳米技术研究人员受益匪浅。

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引用次数: 0

An Epic Advancement in Targeting Macrophages for Cancer Therapy Approach 针对巨噬细胞的癌症治疗方法取得重大进展

IF 2.4 4区医学 Q2 Pharmacology, Toxicology and Pharmaceutics

Current drug delivery

Pub Date : 2024-04-09 DOI: 10.2174/0115672018299798240403062508

Lu Xiaohong, Fu Qiuxia, Li Ruie, Wang Daijie, Tobias Achu Muluh, Yan Zhang

: Macrophages are immune cells with high heterogeneity and plasticity, crucial for recognizing and eliminating foreign substances, including cancer cells. However, cancer cells can evade the immune system by producing signals that cause macrophages to switch to a pro-tumor phenotype, promoting tumor growth and progression. Tumor-associated macrophages, which infiltrate into tumor tissue, are important immune cells in the tumor microenvironment and can regulate cancer's growth, invasion, and metastasis by inhibiting tumor immunity. This review article highlights the characteristics of tumor-associated macrophages and their role in the occurrence and development of cancer. It outlines how reprogramming macrophages towards an anti-tumor phenotype can improve the response to cancer therapy. Explore the intricate process of engineered nanoparticles serving as carriers for immunostimulatory molecules, activating macrophages to instigate an anti-tumor response. Finally, it summarizes several studies demonstrating targeting macrophages is a potential in preclinical cancer models. Several challenges must be addressed in developing effective macrophage-targeted therapies, such as the heterogeneity of macrophage subtypes and their plasticity. Further research is needed to understand the mechanisms underlying macrophage function in the tumor microenvironment and identify novel targets for macrophage-directed therapies. Targeting macrophages is a promising and innovative approach to improving cancer therapy and patient outcomes.

:巨噬细胞是一种具有高度异质性和可塑性的免疫细胞，对于识别和清除包括癌细胞在内的外来物质至关重要。然而，癌细胞可以通过产生信号，使巨噬细胞转为有利于肿瘤的表型，促进肿瘤的生长和进展，从而逃避免疫系统的攻击。渗入肿瘤组织的肿瘤相关巨噬细胞是肿瘤微环境中重要的免疫细胞，可通过抑制肿瘤免疫来调节癌症的生长、侵袭和转移。这篇综述文章重点介绍了肿瘤相关巨噬细胞的特点及其在癌症发生和发展中的作用。文章概述了如何将巨噬细胞重编程为抗肿瘤表型，从而改善对癌症治疗的反应。探索工程纳米粒子作为免疫刺激分子载体的复杂过程，激活巨噬细胞以激发抗肿瘤反应。最后，报告总结了几项研究，这些研究表明，在临床前癌症模型中，以巨噬细胞为靶点是一种潜在的方法。开发有效的巨噬细胞靶向疗法必须应对一些挑战，如巨噬细胞亚型的异质性及其可塑性。要了解巨噬细胞在肿瘤微环境中的功能机制并确定巨噬细胞靶向疗法的新靶点，还需要进一步的研究。以巨噬细胞为靶点是改善癌症治疗和患者预后的一种前景广阔的创新方法。

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引用次数: 0

Evaluation of Doxorubicin-loaded Echogenic Macroemulsion for Targeted Drug Delivery. 用于靶向给药的负载型多柔比星回声大乳剂的评估

IF 2.4 4区医学 Q2 Pharmacology, Toxicology and Pharmaceutics

Current drug delivery

Pub Date : 2024-01-01 DOI: 10.2174/1567201820666230403111118

Jong-Ryul Park, Gayoung Kim, Jongho Won, Chul-Woo Kim, Donghee Park

Background: The latest technology trend in targeted drug delivery highlights stimuliresponsive particles that can release an anticancer drug in a solid tumor by responding to external stimuli.

Objective: This study aims to design, fabricate, and evaluate an ultrasound-responsive drug delivery vehicle for an ultrasound-mediated drug delivery system.

Methods: The drug-containing echogenic macroemulsion (eME) was fabricated by an emulsification method using the three phases (aqueous lipid solution as a shell, doxorubicin (DOX) contained oil, and perfluorohexane (PFH) as an ultrasound-responsive agent). The morphological structure of eMEs was investigated using fluorescence microscopy, and the size distribution was analyzed by using DLS. The echogenicity of eME was measured using a contrast-enhanced ultrasound device. The cytotoxicity was evaluated using a breast cancer cell (MDA-MB-231) via an in vitro cell experiment.

Results: The obtained eME showed an ideal morphological structure that contained both DOX and PFH in a single particle and indicated a suitable size for enhancing ultrasound response and avoiding complications in the blood vessel. The echogenicity of eME was demonstrated via an in vitro experiment, with results showcasing the potential for targeted drug delivery. Compared to free DOX, enhanced cytotoxicity and improved drug delivery efficiency in a cancer cell were proven by using DOX-loaded eMEs and ultrasound.

Conclusion: This study established a platform technology to fabricate the ultrasound-responsive vehicle. The designed drug-loaded eME could be a promising platform with ultrasound technology for targeted drug delivery.

背景：靶向给药的最新技术趋势强调刺激性共振颗粒，这种颗粒可以通过对外界刺激的反应在实体瘤中释放抗癌药物：本研究旨在设计、制造和评估一种超声响应给药载体，用于超声介导的给药系统：方法：采用乳化方法，利用三相（脂质水溶液作为外壳、含油的多柔比星（DOX）和全氟己烷（PFH）作为超声响应剂）制成含药回声大乳剂（eME）。利用荧光显微镜研究了 eMEs 的形态结构，并利用 DLS 分析了其粒度分布。使用对比增强超声装置测量了 eME 的回声性。通过体外细胞实验，使用乳腺癌细胞（MDA-MB-231）评估了细胞毒性：结果：获得的 eME 具有理想的形态结构，在单个颗粒中同时含有 DOX 和 PFH，其大小适合增强超声响应和避免血管并发症。体外实验证明了 eME 的回声性，其结果显示了靶向给药的潜力。与游离 DOX 相比，通过使用负载 DOX 的 eMEs 和超声波，证明了在癌细胞中增强了细胞毒性并提高了给药效率：本研究建立了一种制造超声响应载体的平台技术。结论：本研究建立了制造超声响应载体的平台技术，所设计的药物负载 eME 可与超声技术相结合，成为一种前景广阔的靶向给药平台。

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引用次数: 0

Nanocarrier Mediated Intranasal Drug Delivery Systems for the Management of Parkinsonism: A Review. 纳米载体介导的鼻内给药系统用于治疗帕金森病：综述。

IF 2.4 4区医学 Q2 Pharmacology, Toxicology and Pharmaceutics

Current drug delivery

Pub Date : 2024-01-01 DOI: 10.2174/1567201820666230523114259

Archita Kapoor, Abdul Hafeez, Poonam Kushwaha

The transport of drugs to the brain becomes a key concern when treating disorders of the central nervous system. Parkinsonism is one of the major concerns across the world populations, which causes difficulty in coordination and balance. However, the blood-brain barrier is a significant barrier to achieving optimal brain concentration through oral, transdermal, and intravenous routes of administration. The intranasal route with nanocarrier-based formulations has shown potential for managing Parkinsonism disorder (PD). Direct delivery to the brain through the intranasal route is possible via the olfactory and trigeminal pathways using drug-loaded nanotechnology-based drug delivery systems. The critical analysis of reported works demonstrates dose reduction, brain targeting, safety, effectiveness, and stability for drug-loaded nanocarriers. The important aspects of intranasal drug delivery, PD details, and nanocarrier-based intranasal formulations in PD management with a discussion of physicochemical characteristics, cell line studies, and animal studies are the major topics in this review. Patent reports and clinical investigations are summarized in the last sections.

在治疗中枢神经系统疾病时，如何将药物输送到大脑是一个关键问题。帕金森氏症是全球人口关注的主要问题之一，它会导致协调和平衡困难。然而，血脑屏障是通过口服、透皮和静脉给药途径达到最佳脑部浓度的重要障碍。使用纳米载体制剂的鼻内给药途径已显示出治疗帕金森氏症（PD）的潜力。使用基于纳米技术的载药系统，可通过鼻内途径经由嗅觉和三叉神经通路直接向大脑给药。对所报道作品的批判性分析表明了药物纳米载体的剂量减少、脑靶向性、安全性、有效性和稳定性。本综述的主要内容包括鼻内给药、PD 详情以及基于纳米载体的鼻内制剂在 PD 治疗中的重要作用，并讨论了理化特性、细胞系研究和动物研究。最后几节总结了专利报告和临床研究。

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引用次数: 0