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Smart Ultrasound-responsive Polymers for Drug Delivery: An Overview on Advanced Stimuli-sensitive Materials and Techniques. 用于给药的智能超声响应聚合物:先进的刺激敏感材料和技术概览。
Pub Date : 2024-01-26 DOI: 10.2174/0115672018283792240115053302
Mostafa Yazdan, Seyed Morteza Naghib

In recent years, a notable advancement has occurred in the domain of drug delivery systems via the integration of intelligent polymers that respond to ultrasound. The implementation of this groundbreaking methodology has significantly revolutionised the controlled and precise delivery of therapeutic interventions. An in-depth investigation is conducted into the most recent developments in ultrasonic stimulus-responsive materials and techniques for the purpose of accomplishing precise medication administration. The investigation begins with an exhaustive synopsis of the foundational principles underlying drug delivery systems that react to ultrasonic stimuli, focusing specifically on the complex interplay between polymers and ultrasound waves. Significant attention is devoted to the development of polymers that demonstrate tailored responsiveness to ultrasound, thereby exemplifying their versatility in generating controlled drug release patterns. Numerous classifications of intelligent polymers are examined in the discussion, including those that react to variations in temperature, pH, and enzymes. When coupled with ultrasonic stimuli, these polymers offer a sophisticated framework for the precise manipulation of drug release in terms of both temporal and spatial dimensions. The present study aims to examine the synergistic effects of responsive polymers and ultrasound in overcoming biological barriers such as the blood-brain barrier and the gastrointestinal tract. By doing so, it seeks to shed light on the potential applications of these materials in intricate clinical scenarios. The issues and future prospects of intelligent ultrasound-responsive polymers in the context of drug delivery are critically analysed in this article. The objective of this study is to offer valuable perspectives on the challenges that must be overcome to enable the effective implementation of these technologies. The primary objective of this comprehensive review is to furnish researchers, clinicians, and pharmaceutical scientists with a wealth of information that will serve as a guide for forthcoming developments in the development and enhancement of intelligent drug delivery systems that employ ultrasound-responsive polymers to attain superior therapeutic outcomes.

近年来,通过整合能对超声波做出反应的智能聚合物,给药系统领域取得了显著进步。这一开创性方法的实施极大地改变了治疗干预的可控和精确输送。本研究深入探讨了超声波刺激响应材料和技术的最新发展,以实现精确给药的目的。研究首先详尽概述了对超声波刺激做出反应的给药系统的基本原理,特别侧重于聚合物与超声波之间复杂的相互作用。本研究重点关注聚合物的开发,这些聚合物对超声波具有量身定制的响应性,从而体现了它们在产生受控药物释放模式方面的多功能性。讨论中研究了智能聚合物的多种分类,包括对温度、pH 值和酶的变化有反应的聚合物。当与超声波刺激相结合时,这些聚合物可提供一个复杂的框架,从时间和空间两个维度精确控制药物释放。本研究旨在探讨响应性聚合物和超声波在克服血脑屏障和胃肠道等生物屏障方面的协同效应。通过这样做,研究试图揭示这些材料在错综复杂的临床场景中的潜在应用。本文对智能超声响应聚合物在药物输送方面的问题和未来前景进行了深入分析。本研究的目的是就有效实施这些技术必须克服的挑战提供有价值的观点。这篇综述的主要目的是为研究人员、临床医生和制药科学家提供丰富的信息,为今后开发和改进采用超声响应聚合物的智能给药系统提供指导,以实现卓越的治疗效果。
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引用次数: 0
Fiber Technology in Drug Delivery and Pharmaceuticals. 给药和制药中的纤维技术。
Pub Date : 2024-01-25 DOI: 10.2174/0115672018279628231221105210
Shivang Dhoundiyal, Aditya Sharma, Md Aftab Alam

The field of fiber technology is a dynamic and innovative domain that offers novel solutions for controlled and targeted therapeutic interventions. This abstract provides an overview of key aspects within this field, encompassing a range of techniques, applications, commercial developments, intellectual property, and regulatory considerations. The foundational introduction establishes the significance of fiber-based drug delivery systems. Electrospinning, a pivotal technique, has been explored in this paper, along with its various methods and applications. Monoaxial, coaxial, triaxial, and side-by-side electrospinning techniques each offer distinct advantages and applications. Centrifugal spinning, solution and melt blowing spinning, and pressurized gyration further contribute to the field's diversity. The review also delves into commercial advancements, highlighting marketed products that have successfully harnessed fiber technology. The role of intellectual property is acknowledged, with patents reflecting the innovative strides in fiber-based drug delivery. The regulatory perspective, essential for ensuring safety and efficacy, is discussed in the context of global regulatory agencies' evaluations. This review encapsulates the multidimensional nature of fiber technology in drug delivery and pharmaceuticals, showcasing its potential to revolutionize medical treatments and underscores the importance of continued collaboration between researchers, industry, and regulators for its advancement.

纤维技术领域是一个充满活力和创新的领域,它为可控和靶向治疗干预提供了新颖的解决方案。本摘要概述了这一领域的主要方面,包括一系列技术、应用、商业发展、知识产权和监管考虑因素。基础性介绍确立了纤维给药系统的重要性。本文探讨了电纺丝这一关键技术及其各种方法和应用。单轴、同轴、三轴和并排电纺丝技术各有其独特的优势和应用。离心纺丝、溶液纺丝和熔体吹塑纺丝以及加压回旋进一步丰富了这一领域。综述还深入探讨了商业进展,重点介绍了成功利用纤维技术的市场产品。知识产权的作用得到了认可,专利反映了纤维给药技术的创新进步。本综述从监管角度出发,结合全球监管机构的评估,讨论了对确保安全性和有效性至关重要的问题。这篇综述概括了纤维给药和制药技术的多面性,展示了其彻底改变医疗方法的潜力,并强调了研究人员、行业和监管机构之间持续合作对其发展的重要性。
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引用次数: 0
Recent Developments in Tyrosine Kinase Inhibitor-based Nanotherapeutics for EGFR-resistant Non-small Cell Lung Cancer. 基于酪氨酸激酶抑制剂的纳米疗法治疗表皮生长因子受体耐药的非小细胞肺癌的最新进展。
Pub Date : 2024-01-24 DOI: 10.2174/0115672018278617231207051907
Eknath Kole, Krishna Jadhav, Raghuraj Singh, Shilpa Mandpe, Ashwin Abhang, Rahul K Verma, Jitendra Naik

The advent of drug resistance in response to epidermal growth factor receptor (EGFR)- tyrosine kinase inhibitor (TKI) targeted therapy represents a serious challenge in the management of non-small cell lung cancer (NSCLC). These acquired resistance mutations, attributed to several advanced EGFR mutations and, necessitated the development of new-generation TKIs. Nanomedicine approaches provide a plausible way to address these problems by providing targeted delivery and sustained release, which have demonstrated success in preclinical trials. This review article provides a summary of nano-formulations designed for EGFR-TKI-resistant NSCLC, highlighting their efficacy in both in vitro and in vivo models. These findings reveal insights into the design of nanoparticles and multifunctional nanosystems, offering a potential avenue for efficacious treatment of EGFR-TKIresistant NSCLC.

表皮生长因子受体(EGFR)-酪氨酸激酶抑制剂(TKI)靶向治疗出现的耐药性是非小细胞肺癌(NSCLC)治疗面临的严峻挑战。这些获得性耐药突变归因于几种晚期表皮生长因子受体突变,因此有必要开发新一代 TKIs。纳米医学方法通过提供靶向给药和持续释放为解决这些问题提供了一种可行的途径,这些方法已在临床前试验中取得了成功。这篇综述文章总结了为表皮生长因子受体-TKI耐药NSCLC设计的纳米制剂,强调了它们在体外和体内模型中的疗效。这些发现揭示了纳米颗粒和多功能纳米系统的设计思路,为有效治疗耐 EGFR-TKI NSCLC 提供了潜在的途径。
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引用次数: 0
A Comprehensive Review on Polyphenols Based Nanovesicular System for Topical Delivery. 基于多酚的局部给药纳米囊泡系统综述。
Pub Date : 2024-01-24 DOI: 10.2174/0115672018265118231213094410
Anshu Singh, Zeeshan Fatima, Dipti Srivastava

Background: Polyphenols are naturally occurring compounds having more than one hydroxy functional group. They are ubiquitous secondary plant metabolites possessing a wide range of pharmacological activity. Brightly colored fruits and vegetables are the natural source of polyphenols. Majorly, they possess antioxidant, anti-inflammatory and antimicrobial properties which make them suitable candidates to target skin related disorders.

Objective: This study is focused to explore the potential of polyphenols loaded nanovesicles for skin related disorders. The aim of the study is to review the applicability and efficacy of different vesicular systems encapsulated with various classes of polyphenols for skin related disorders, thus opening the opportunity for future studies based on these drug delivery systems.

Method: Web of Science, PubMed, Scopus database, and the search engine Google Scholar were accessed for the literature search. The results were then filtered based on the titles, abstracts, and accessibility of the complete texts.

Results: The expository evaluation of the literature revealed that various nanovesicles like liposomes, niosomes, ethosomes and transferosomes incorporating polyphenol have been formulated to address issues pertaining to delivery across the skin. These developed nano vesicular systems have shown improvement in the physicochemical properties and pharmacological action.

Conclusion: Polyphenol based nano-vesicular formulations have proved to be an effective system for topical delivery and henceforth, they might curtail the use of other skin therapies having limited applicability.

背景:多酚是具有一个以上羟基官能团的天然化合物。它们是无处不在的植物次生代谢物,具有广泛的药理活性。颜色鲜艳的水果和蔬菜是多酚的天然来源。它们主要具有抗氧化、抗炎和抗菌特性,因此适合用于治疗皮肤相关疾病:本研究的重点是探索多酚负载纳米颗粒治疗皮肤相关疾病的潜力。本研究的目的是回顾包裹了各种多酚的不同囊泡系统对皮肤相关疾病的适用性和疗效,从而为今后基于这些给药系统的研究提供机会:方法:使用 Web of Science、PubMed、Scopus 数据库和搜索引擎 Google Scholar 进行文献检索。方法:通过 Web Science、PubMus、Scopus 数据库和搜索引擎 Google Scholar 进行文献检索,然后根据标题、摘要和全文的可读性对结果进行筛选:对文献进行的阐述性评估显示,为了解决跨皮肤给药的相关问题,人们配制了各种纳米囊泡,如含有多酚的脂质体、niosomes、ethosomes 和 transferosomes。这些开发的纳米囊泡系统在理化性质和药理作用方面都有所改进:结论:以多酚为基础的纳米囊泡配方已被证明是一种有效的局部给药系统,因此可能会减少其他适用性有限的皮肤疗法的使用。
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引用次数: 0
Current Trends in Nanotechnology-based Drug Delivery Systems for the Diagnosis and Treatment of Malaria: A Review. 基于纳米技术的疟疾诊断和治疗给药系统的当前趋势:综述》(Nanotechnology-based Drug Delivery Systems for the Diagnosis and Treatment of Malaria: A Review)。
Pub Date : 2024-01-23 DOI: 10.2174/0115672018291253240115012327
Rohitas Deshmukh, Bhuvaneshwari Dewangan, Ranjit K Harwansh, Rutvi Agrawal, Akash Garg, Himansu Chopra

Malaria is still a major endemic disease transmitted in humans via Plasmodium-infected mosquitoes. The eradication of malarial parasites and the control measures have been rigorously and extensively deployed by local and international health organizations. Malaria's recurrence is a result of the failure to entirely eradicate it. The drawbacks related to malarial chemotherapy, non-specific targeting, multiple drug resistance, requirement of high doses, intolerable toxicity, indefinable complexity of Plasmodium's life cycle, and advent of drug-resistant strains of P. falciparum are the causes of the ineffective eradication measures. With the emergence of nanotechnology and its application in various industrial domains, the rising interest in the medical field, especially in epidemiology, has skyrocketed. The applications of nanosized carriers have sparked special attention, aiming towards minimizing the overall side effects caused due to drug therapy and avoiding bioavailability. The applications of concepts of nanobiotechnology to both vector control and patient therapy can also be one of the approaches. The current study focuses on the use of hybrid drugs as next-generation antimalarial drugs because they involve fewer drug adverse effects. The paper encompasses the numerous nanosized delivery-based systems that have been found to be effective among higher animal models, especially in treating malarial prophylaxis. This paper delivers a detailed review of diagnostic techniques, various nanotechnology approaches, the application of nanocarriers, and the underlying mechanisms for the management of malaria, thereby providing insights and the direction in which the current trends are imparted from the innovative and technological perspective.

疟疾仍然是通过受疟原虫感染的蚊子传播给人类的一种主要地方病。疟疾寄生虫的根除和控制措施已由当地和国际卫生组织进行了严格和广泛的部署。疟疾的复发是未能完全根除的结果。疟原虫化疗的弊端、非特异性靶向性、多重抗药性、高剂量要求、难以忍受的毒性、疟原虫生命周期难以确定的复杂性,以及恶性疟原虫抗药性菌株的出现,都是根除措施效果不佳的原因。随着纳米技术的出现及其在各个工业领域的应用,人们对医学领域,尤其是流行病学领域的兴趣急剧上升。纳米级载体的应用引发了人们的特别关注,其目的是最大限度地减少药物治疗引起的整体副作用,避免生物利用度。将纳米生物技术的概念应用于病媒控制和患者治疗也是方法之一。目前的研究重点是使用混合药物作为下一代抗疟药物,因为它们涉及较少的药物不良反应。本文介绍了许多基于纳米尺寸的给药系统,这些系统在高等动物模型中被发现是有效的,尤其是在治疗疟疾预防方面。本文详细综述了诊断技术、各种纳米技术方法、纳米载体的应用以及疟疾治疗的基本机制,从而从创新和技术的角度提供了当前趋势的见解和方向。
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引用次数: 0
Controlled Release of Aspirin in the Body using Pectin-coated ZIF-8 Nanoparticles. 使用果胶包裹的 ZIF-8 纳米粒子控制阿司匹林在体内的释放。
Pub Date : 2024-01-17 DOI: 10.2174/0115672018288328240109064308
Fatemeh Shahidi, M Reza Naimi-Jamal, Azizollah Habibi, Mohammad G Dekamin

Introduction: Zeolitic imidazolate frameworks (ZIFs) play a crucial role among metalorganic frameworks due to their highly desirable properties, including high surface area, appropriate pore size, and excellent thermal and chemical stability.

Method: In this study, ZIF-8 loaded with aspirin and coated using pectin (ZIF-8/Asp@Pectin) was utilized as a suitable and effective platform for the drug delivery system. The preparation of this coated MOF followed environmentally friendly methods, and aspirin was successfully loaded.

Result: Characterization of the obtained ZIF-8/Asp@Pectin was performed using X-ray diffraction (XRD), scanning electron microscopy (SEM), thermal gravimetric analysis (TGA), Fourier Transform Infrared (FT-IR) spectroscopy, and BET analysis.

Conclusion: The release of aspirin from ZIF-8/Asp@Pectin was studied using UV-Vis spectroscopy at 258 nm under in vitro conditions in HCl and PBS buffer solutions.

简介:沸石咪唑酸盐框架(ZIFs)具有高比表面积、适当的孔径以及优异的热稳定性和化学稳定性等理想特性,因此在金属有机框架中发挥着重要作用:本研究利用负载阿司匹林并使用果胶包覆的 ZIF-8(ZIF-8/Asp@Pectin)作为药物输送系统的合适而有效的平台。该包覆 MOF 的制备采用了环境友好型方法,并成功负载了阿司匹林:结果:采用 X 射线衍射 (XRD)、扫描电子显微镜 (SEM)、热重分析 (TGA)、傅立叶变换红外光谱 (FT-IR) 和 BET 分析对获得的 ZIF-8/Asp@Pectin 进行了表征:结论:在盐酸和 PBS 缓冲溶液的体外条件下,使用 258 纳米波长的紫外可见光谱研究了阿司匹林从 ZIF-8/Asp@Pectin 中的释放情况。
{"title":"Controlled Release of Aspirin in the Body using Pectin-coated ZIF-8 Nanoparticles.","authors":"Fatemeh Shahidi, M Reza Naimi-Jamal, Azizollah Habibi, Mohammad G Dekamin","doi":"10.2174/0115672018288328240109064308","DOIUrl":"https://doi.org/10.2174/0115672018288328240109064308","url":null,"abstract":"<p><strong>Introduction: </strong>Zeolitic imidazolate frameworks (ZIFs) play a crucial role among metalorganic frameworks due to their highly desirable properties, including high surface area, appropriate pore size, and excellent thermal and chemical stability.</p><p><strong>Method: </strong>In this study, ZIF-8 loaded with aspirin and coated using pectin (ZIF-8/Asp@Pectin) was utilized as a suitable and effective platform for the drug delivery system. The preparation of this coated MOF followed environmentally friendly methods, and aspirin was successfully loaded.</p><p><strong>Result: </strong>Characterization of the obtained ZIF-8/Asp@Pectin was performed using X-ray diffraction (XRD), scanning electron microscopy (SEM), thermal gravimetric analysis (TGA), Fourier Transform Infrared (FT-IR) spectroscopy, and BET analysis.</p><p><strong>Conclusion: </strong>The release of aspirin from ZIF-8/Asp@Pectin was studied using UV-Vis spectroscopy at 258 nm under in vitro conditions in HCl and PBS buffer solutions.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-17","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139514470","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
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":" ","pages":""},"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。
{"title":"TPGS-mediated Transethosomes Enhance Transdermal Administration of Curcumin via Effects on Deformability and Stability.","authors":"Teng Guo, Chenming Zhang, Yuling Chen, Yihan Wu, Zhenda Liu, Yongtai Zhang, Nianping Feng","doi":"10.2174/0115672018279577231208055415","DOIUrl":"https://doi.org/10.2174/0115672018279577231208055415","url":null,"abstract":"<p><strong>Background: </strong>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).</p><p><strong>Methods: </strong>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.</p><p><strong>Results: </strong>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.</p><p><strong>Conclusion: </strong>TPGS-mediated transethosomes exhibit significant transdermal advantages and enhanced anti-inflammatory effects, providing a new perspective for the transdermal delivery of curcumin.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139418909","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
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。
{"title":"TPGS-modified Chitosan Nanoparticles of EGFR Inhibitor: Physicochemical and In vitro Evaluation against HepG2 Cell Lines.","authors":"Mahendra Singh, Alka, Prashant Shukla, Zhi-Hong Wen, Chou-Yuan Ko, Ramachandran Vinayagam","doi":"10.2174/0115672018268315231206045504","DOIUrl":"https://doi.org/10.2174/0115672018268315231206045504","url":null,"abstract":"<p><strong>Background: </strong>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.</p><p><strong>Methods: </strong>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.</p><p><strong>Results: </strong>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.</p><p><strong>Conclusion: </strong>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.</p>","PeriodicalId":94287,"journal":{"name":"Current drug delivery","volume":" ","pages":""},"PeriodicalIF":0.0,"publicationDate":"2024-01-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139418910","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
期刊
Current drug delivery
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