抗肿瘤药物靶向载体系统的研究与开发

综述肿瘤靶向给药的基础和抗肿瘤药物靶向载体系统的发展。分类介绍普通被动靶向载药系统（如微乳、传统脂质体、聚合物纳米粒、固体脂质纳米粒、纳米脂质载体、药-脂结合物纳米粒等）、表面修饰的被动靶向载药系统及主动靶向载药系统（如免疫脂质体、免疫聚合物纳米粒及受体-配体介导靶向纳米载体）的研究与开发。在传统药物制剂的基础上，发展抗肿瘤药物的新型靶向载体系统，改善药物在体内的代谢动力学特性，增加药物定向富集到肿瘤部位甚至肿瘤细胞内，提高疗效，降低毒副作用，是近年来备受关注的课题。     

脂质体的特性及临床治疗进展

近年来,靶向给药成为给药系统研究的热点,脂质体作为药物靶向载体引起了国内外广泛而深入的研究。这里对脂质体的作用机理、特点、分类、载药方式及应用进行总结和概括,并对热门的新型脂质体做出相关的介绍和分析,提出脂质体未来的发展趋势和前景。     

包合物脂质体靶向系统在给药中的应用

近年来,包合物和脂质体作为药物的载体被广泛用于药物制剂领域,各自发挥着自身的优势。将环糊精包合物应用于脂质体给药系统——这一新型的药物载体,能够更好地提高靶向给药效果。本文通过概述包合物及脂质体的优势,阐明包合物脂质体这一新型给药系统能提高药物的载药量,增加脂质体的稳定性,对提高药物的吸收和临床疗效等方面具有重要意义,对于靶向给药系统的进一步发展具有新的参考价值。     

抗癌中药靶向制剂概述

靶向给药系统亦称靶向制剂(targeted drug delivery sys- tem,TDDS),是指给药后能使药物主动地或被动地选择性浓集定位于病变组织、器官、细胞或细胞内结构的新型给药系统。按载体的不同可分为脂质体、微粒、纳米粒(毫微粒)、复合型乳剂等。靶向制剂可使药物到达靶区,提高疗效,降低毒副作用,是近年来国内外药品开发的热点。我国中药     

电磁波控制热敏磁性脂质体靶向给药

本文从新型靶向给药系统-热敏磁性脂质体靶向给药的几个关键之处出发，介绍了目前热敏磁性脂质体的脂质材料、磁性材料、磁定位和电磁波控释研究状况，分析讨论了电磁波在热敏磁性脂质体的磁靶向和药物控释方面的作用,并提出了测量热敏磁性脂质体的电磁参数和选择合适的电磁波频段用于药物控释的必要性。     

固体脂质纳米粒的研究新进展

固体脂质纳米粒是近年来很受重视的一种新型药物传递载体,具有靶向、控释、提高药物稳定性、毒性小、可大批量生产等优点,是一种极有发展前景的新型给药系统.现综述了近年来国内外固体脂质纳米粒的制备技术、作为药物载体的应用、存在问题以及发展前景.     

新型脂质体的研究概况

新型脂质体的研究概况吴传斌，石庭森（军事医学科学院毒物药物研究所北京１００８５０）脂质体具有使药物靶向性、延效、缓和毒性、提高疗效、避免耐药性，改变给药途径等优点，国内外对此进行了广泛的研究。特别是作为靶向给药系统的研究进展比较迅速［１，２］，如脂质...     

脂质体在给药系统的应用与研究

脂质体是将药物包封于类脂双分子层形成的薄膜中间所制成的超微型球状载体制剂。是一种具有多功能的定向药物载体，能够降低药物毒副作用，提高生物利用度，并具有长效缓释作用。由于其组成和结构的特点，脂质体用作药物的载体使药剂学的研究领域进入靶向给药的新天地，同时也更新了给药途径。本文就脂质体在给药系统的研究进展进行综述。     

PEG化隐形纳米脂质体的研究进展

PEG化隐形纳米脂质体作为一种新型药物载体,由于其特殊的体内作用特点,和普通脂质体相比具有长效、靶向、高效、低毒等优点,已在靶向制剂、控释制剂等领域中得到广泛应用。本文重点围绕PEG化隐形纳米脂质体的药动学、组织分布、提高肿瘤靶向性、降低药物毒性等方面对其近年来在药物转运系统中的研究与应用做一综述。     

纳米粒淋巴靶向的研究进展

目的从淋巴靶向方面综述脂质体、纳米活性炭以及纳米碳管纳米粒的研究进展。方法参考近年来32篇相关的中外文献,在淋巴系统的生理基础上,探讨上述纳米粒的淋巴靶向性及其在淋巴靶向方面的应用。结果脂质体具有天然的淋巴靶向性。纳米活性炭有较好的淋巴趋向性,并能在淋巴结处缓缓释放出药物。纳米碳管可通过表面修饰来提高其淋巴靶向性。上述纳米粒均可以作为显影剂与药物载体以提高其淋巴靶向性。结论纳米粒有较好的淋巴靶向性,可以作为显影剂和药物靶向淋巴的理想载体。     

PEG–lipid micelles as drug carriers: physiochemical attributes,formulation principles and biological implication

PEG–lipid micelles, primarily conjugates of polyethylene glycol (PEG) and distearyl phosphatidylethanolamine (DSPE) or PEG–DSPE, have emerged as promising drug-delivery carriers to address the shortcomings associated with new molecular entities with suboptimal biopharmaceutical attributes. The flexibility in PEG–DSPE design coupled with the simplicity of physical drug entrapment have distinguished PEG–lipid micelles as versatile and effective drug carriers for cancer therapy. They were shown to overcome several limitations of poorly soluble drugs such as non-specific biodistribution and targeting, lack of water solubility and poor oral bioavailability. Therefore, considerable efforts have been made to exploit the full potential of these delivery systems; to entrap poorly soluble drugs and target pathological sites both passively through the enhanced permeability and retention (EPR) effect and actively by linking the terminal PEG groups with targeting ligands, which were shown to increase delivery efficiency and tissue specificity. This article reviews the current state of PEG–lipid micelles as delivery carriers for poorly soluble drugs, their biological implications and recent developments in exploring their active targeting potential. In addition, this review sheds light on the physical properties of PEG–lipid micelles and their relevance to the inherent advantages and applications of PEG–lipid micelles for drug delivery.     

Nanostructured materials in drug and gene delivery: a review of the state of the art

A wide variety of drug delivery systems have been developed, each with its own advantages and limitations, but the important goals of all of the systems are to enhance bioavailability, reduce drug toxicity, target to a particular organ, and increase the stability of the drug. The development of nanostructured drug carriers have grasped increased attention from scientific and commercial organizations due to their unique ability to deliver drugs and challenging molecules such as proteins and nucleic acids. These carriers present many technological advantages such as high carrier capacity, high chemical and biological stability, feasibility of incorporating both hydrophilic and hydrophobic substances, and their ability to be administered by a variety of routes (including oral, inhalational, and parenteral) to provide controlled/sustained drug release. Moreover, applications of nanoparticulate formulations in enhancing drug solubility, dissolution, bioavailability, safety, and stability have already been proven. In the view of their multifaceted applications, the present review aims to discuss and summarize some of the interesting findings and applications, methods of preparation, and characterization of various nanostructured carriers useful in drug delivery. Included in this discussion are polymeric nanoparticles, solid lipid nanoparticles, nanostructured lipid carriers, dendrimers, cyclodextrins, fullerenes, gold and silica nanoparticles, and quantum dots. Because there are likely to be new applications for nanoparticles in drug delivery, they are expected to solve many problems associated with the delivery of drugs and biomolecules through different delivery routes.     

SLN, NLC, LDC: state of the art in drug and active delivery

Drug delivery system focuses on the regulation of the in vivo dynamics, in order to improve the effectiveness and safety of the incorporated drugs by use of novel drug formulation technologies. Lipids such as fatty acids, triglycerides, vegetable oils and their derivatives, used for developing multiparticulate dosage forms, may be available in solid, semi-solid or liquid state. Solid lipid nanoparticles (SLNs), nanostructured lipid carriers (NLCs) and lipid drug conjugate (LDCs) nanoparticles are novel lipid drug delivery systems. They were devised to address some of the challenges of conventional drug delivery systems ranging from low drug encapsulation efficiency to low bioavailability of Biopharmaceutical Classification Systems (BCS) class II and class IV drugs. SLNs are based on melt-emulsified lipids, which are solid at room temperature and consist of physiologically well tolerated ingredients often generally recognised as safe. NLCs are colloidal carriers characterized by a solid lipid core consisting of a mixture of solid and liquid lipids, and having a mean particle size in the nanometer range. LDC are nanoparticles contain drugs linked to lipid particles. This minireview highlights these three different but related technologies in lipid drug delivery. The objectives of their introduction, current applications, major challenges and some patented formulations are highlighted.     

Nanoparticles as drug delivery systems

Controlled drug delivery systems (DDS) have several advantages compared to the traditional forms of drugs. A drug is transported to the place of action, hence, its influence on vital tissues and undesirable side effects can be minimized. Accumulation of therapeutic compounds in the target site increases and, consequently, the required doses of drugs are lower. This modern form of therapy is especially important when there is a discrepancy between the dose or the concentration of a drug and its therapeutic results or toxic effects. Cell-specific targeting can be accomplished by attaching drugs to specially designed carriers. Various nanostructures, including liposomes, polymers, dendrimers, silicon or carbon materials, and magnetic nanoparticles, have been tested as carriers in drug delivery systems. In this review, the aforementioned nanocarriers and their connections with drugs are analyzed. Special attention is paid to the functionalization of magnetic nanoparticles as carriers in DDS. Then, the advantages and disadvantages of using magnetic nanoparticles as DDS are discussed.     

固体脂质纳米粒和纳米结构脂质载体在经皮给药系统中的研究进展

目的介绍固体脂质纳米粒和纳米结构脂质载体在经皮给药系统中的应用与优势,为其开发利用提供参考。方法查阅国内外相关文献共30余篇,从固体脂质纳米粒和纳米结构脂质载体用于经皮给药系统的优势、药物在固体脂质纳米粒和纳米结构脂质载体中的分布形式及固体脂质纳米粒和纳米结构脂质载体在经皮给药领域中的应用等方面进行综述。结果固体脂质纳米粒和纳米结构脂质载体可以增强药物稳定性,能在皮肤表面产生包封效应,增加皮肤水合作用,具有药物靶向性。结论固体脂质纳米粒和纳米结构脂质载体是极有发展前景的新型经皮给药系统。     

Perspectives on cutting-edge nanoparticulate drug delivery technologies based on lipids and their applications

Numerous nanotech arenas in therapeutic biology have recently provided a scientific platform to manufacture a considerable swath of unique chemical entities focusing on drugs. Recently, nanoparticulate drug delivery systems have emerged to deliver a specific drug to a specified site. Among all other carriers, lipids possess features exclusive to nanostructured dosage forms. The bioavailability of orally administered drugs is typically negatively affected by their poor water solubility, resulting from the unique chemical moieties introduced. Because of their unique advantages, lipid nanoparticles must become increasingly predictable as a robust delivery mechanism. The enhanced biopharmaceutical properties and significance of lipid-based targeting technologies such as liposomes, niosomes, solid lipid nanoparticles and micelles are highlighted in this review. Pharmaceutical implications of lipid nanocarriers for the transport and distribution of various therapeutic agents, such as biotechnological products and small pharmaceutical molecules, is a booming topic. Lipid nanoparticles as drug delivery systems have many appealing properties, including high biocompatibility, ease of preparation, tissue specificity, avoidance of reticuloendothelial systems, delayed drug release, scale-up feasibility, nontoxicity and targeted delivery. The use of lipid nanoparticles to enhance the transport of biopharmaceuticals is currently considered state-of-the-art. Similarly, we critically examine the upcoming guidelines that therapeutic scientists should handle.     

囊泡及微粒经皮给药系统的研究进展

近年来,各种方法被用于促进药物的经皮渗透,其中囊泡及微粒系统是一种简单便捷的方法.本文综述了促进药物经皮渗透的各种囊泡(变形脂质体、醇质体、类脂囊泡)及微粒系统(微乳、固体脂质纳米粒及纳米脂质载体)用于经皮给药系统的作用机制以及相关研究工作的进展.     

Lipid nanoparticles as novel delivery systems for cosmetics and dermal pharmaceuticals

INTRODUCTION: Lipid nanoparticles are innovative carrier systems developed as an alternative to traditional vehicles such as emulsions, liposomes and polymeric nanoparticles. Solid lipid nanoparticles (SLN) and the newest nanostructured lipid carriers (NLC) show important advantages for dermal application of cosmetics and pharmaceuticals. AREA COVERED: This article focuses on the main features of lipid nanoparticles, in terms of their preparation and recent advancements. A detailed review of the literature is presented, introducing the importance of these systems in the topical delivery of drugs and active substances. EXPERT OPINION: Lipid nanoparticles are able to enhance drug penetration into the skin, allowing increased targeting to the epidermis and consequently increasing treatment efficiency and reducing the systemic absorption of drugs and cosmetic actives. The complete biodegradation of lipid nanoparticles and their biocompatible chemical nature have secured them the title of 'nanosafe carriers.' SLN and NLC represent a new technological era, which has been taken over by the cosmetic and pharmaceutical industry, which will open new channels for effective topical delivery of substances.     

Current strategies for targeted delivery of bio-active drug molecules in the treatment of brain tumor

Brain tumor is one of the most challenging diseases to treat. The major obstacle in the specific drug delivery to brain is blood–brain barrier (BBB). Mostly available anti-cancer drugs are large hydrophobic molecules which have limited permeability via BBB. Therefore, it is clear that the protective barriers confining the passage of the foreign particles into the brain are the main impediment for the brain drug delivery. Hence, the major challenge in drug development and delivery for the neurological diseases is to design non-invasive nanocarrier systems that can assist controlled and targeted drug delivery to the specific regions of the brain. In this review article, our major focus to treat brain tumor by study numerous strategies includes intracerebral implants, BBB disruption, intraventricular infusion, convection-enhanced delivery, intra-arterial drug delivery, intrathecal drug delivery, injection, catheters, pumps, microdialysis, RNA interference, antisense therapy, gene therapy, monoclonal/cationic antibodies conjugate, endogenous transporters, lipophilic analogues, prodrugs, efflux transporters, direct conjugation of antitumor drugs, direct targeting of liposomes, nanoparticles, solid–lipid nanoparticles, polymeric micelles, dendrimers and albumin-based drug carriers.     

纳米结构脂质载体肺部给药研究进展

传统吸入疗法不能使药物靶向到肺的特定部位,而纳米载体药物的肺部给药系统可克服传统吸入药物的不足。其中纳米结构脂质载体是固体和液体脂质的混合物经表面活性剂乳化后形成的纳米粒,具有更好的胶体稳定性和持续的药物释放行为。其组成成分具有无毒、生理惰性和生物相容性的特点,还具有良好的雾化特性,特别适用于肺部应用,并且生产过程简单（高压均质）,适合大规模生产。本文介绍了常见肺部给药纳米载体,概述了纳米结构脂质载体应用于肺部的优势,为其在肺部给药领域中的深度开发提供参考。