脂质聚合物杂化纳米粒的研究进展

目的：综述脂质聚合物杂化纳米粒的最新研究进展。方法：查阅近20年国内外有关脂质聚合物杂化纳米粒文献,对脂质聚合物杂化纳米粒的制备方法、主要影响因素及其应用现状进行总结。结果：核壳结构脂质聚合物杂化纳米粒兼具脂质体与聚合物纳米粒2种载体的优势,可一定程度改善脂质体和纳米粒存在的稳定性差、药物渗漏等不足。结论：脂质聚合物杂化纳米粒是一种性能优良,具有广阔发展前景的新型给药系统,但目前尚需对稳定性、在体药效及安全性等问题做深入研究。     

乳酸-羟基乙酸共聚物纳米粒的制备及其表面修饰

目的:促进生物可降解聚合物乳酸-羟基乙酸共聚物(PLGA)纳米粒作为蛋白、多肽类药物投递载体的应用。方法:综述近几年乳酸-羟基乙酸共聚物纳米粒的制备方法及其参数,并概述其纳米粒的表面修饰手段。结果:乳酸-羟基乙酸共聚物纳米粒的制备方法主要包括乳化-溶剂挥发法、相转变法、乳化-扩散法、沉淀法、盐析法以及高压乳匀法。制备纳米粒的一个关键性参数是表面活性剂/稳定剂。纳米粒表面修饰最常用聚乙二醇。结论:乳酸-羟基乙酸共聚物纳米粒作为一种新型的给药系统富有前景,可广泛应用于亲水性和疏水性药物,尤其是蛋白、疫苗、生物大分子的给药。     

9-硝基喜树碱半固体脂质纳米粒的制备及大鼠的药动学研究

采用高温乳化蒸发-低温固化法制备9-硝基喜树碱(1)半固体脂质纳米粒,并考察其形态、粒径、包封率、z电位及大鼠静脉给药后体内药物动力学行为。结果表明,1半固体脂质纳米粒为圆形,具有明显可见的亲水性聚乙二醇“外壳”,粒径为223.3～249.1nm,包封率为77.9%～83.5%,z电位为-28.4～-22.2mV。分别用1半固体脂质纳米粒和溶液对大鼠静脉给药,体内药物动力学参数分别为:t1/2 (14.9±0.3)h和(1.2±0.6)h,AUC0～t(486±37)mg·h·L-1和(117±64)mg·h·L-1,MRT (19.3±0.7)h和(1.7±1.0)h。表明1半固体脂质纳米粒可延长体循环时间,提高生物利用度。     

非洛地平-硬脂酸固体脂质纳米粒的制备及其体外透皮吸收研究

目的:以固体脂质纳米粒为栽体,通过透皮给药达到提高非洛地平透皮吸收及缓释长效的目的.方法:采用溶剂挥发-超声法制备非洛地平固体脂质纳米粒水分散体,以大鼠皮肤为渗透屏障对非洛地平固体脂质纳米粒的经皮渗透进行研究.结果:非洛地平-硬脂酸固体脂质纳米粒为类球形实体粒子,平均粒径范围在50～150 nm,包封率大于85%,栽药量大于7%,药物体外释放符合一级动力学过程.体外经皮渗透速率显著高于空白对照组.结论:非洛地平固体脂质纳米粒处方设计合理,制备工艺可靠,以纳米粒作为透皮给药载体具有广阔的发展前景.     

醋酸地塞米松固体类脂纳米粒在小鼠体内的靶向性研究

目的 探讨醋酸地塞米松固体脂质纳米粒在小鼠体内的靶向性。方法 用HPLC测定生物样品中醋酸地塞米松的含量,比较醋酸地塞米松纳米粒和原药给药后在不同时间各脏器的药物含量、各脏器中药物的量占给药量的百分数及药动学参数,以评价醋酸地塞米松固体脂质纳米粒的靶向性。结果 在肺部,醋酸地塞米松纳米粒给药组的地塞米松含量、地塞米松量占给药量的百分数远高于原药给药组,两者的AUC值相差约16倍。结论 醋酸地塞米松固体脂质纳米粒在小鼠体内具有肺靶向性。     

醋酸地塞米松固体类脂纳米粒在小鼠体内的靶向性研究

目的 探讨醋酸地塞米松固体脂质纳米粒在小鼠体内的靶向性。方法 用HPLC测定生物样品中醋酸地塞米松的含量,比较醋酸地塞米松纳米粒和原药给药后在不同时间各脏器的药物含量、各脏器中药物的量占给药量的百分数及药动学参数,以评价醋酸地塞米松固体脂质纳米粒的靶向性。结果 在肺部,醋酸地塞米松纳米粒给药组的地塞米松含量、地塞米松量占给药量的百分数远高于原药给药组,两者的AUC值相差约16倍。结论 醋酸地塞米松固体脂质纳米粒在小鼠体内具有肺靶向性。     

脂质聚合物杂交纳米粒的研究进展

脂质聚合物杂交纳米粒（Lipid polymerhybrid nanoparticles,LPHNPs）是一种新型载药系统,该纳米粒由修饰亲水性聚合物的脂质外壳包裹疏水性聚合物内核组成,LPHNPs具有较高的结构完整性、良好的生物相容性和载药量及制备材料多样化等优点,使得其在药物递送、诊断成像、基因治疗领域被广泛研究。现主要对LPHNPs的基本特点、结构、制备方法及应用进行综述,以期为后续研究提供参考。     

5-氟尿嘧啶聚乙二醇-聚十六烷基氰丙烯酸酯纳米粒的制备

目的:以聚乙二醇-聚十六烷基氰丙烯酸酯(PEG-PHDCA)聚合物制备5-氟尿嘧啶(5-Fu)纳米粒,并对其进行体外释药研究.方法:采用溶剂扩散法制备5-Fu PEG-PHDCA纳米粒,在单因素基础上采用正交设计法优化得到最佳处方,并对5-Fu聚合物纳米粒的粒径、Zeta电位、载药量、包封率和体外释放进行了研究.结果:制得的5-Fu聚合物纳米粒的平均粒径为132 nm,Zeta电位为-(12±2)V,载药量为12.3%,包封率为48.8%.体外释放研究发现,5-Fu PEG-PHDCA纳米粒释药近似符合Higuchi释药模型:Q=0.564 4+8.386t1/2(r=0.996 0).结论:采用溶剂扩散法制备5-Fu聚合物纳米粒方法简单,重现性好,其体外释放显示出明显缓释作用.     

联苯双酯固体脂质纳米粒注射给药在大鼠体内的药动学

目的:研究联苯双酯固体脂质纳米粒在大鼠体内的药动学。方法:制备联苯双酯固体脂质纳米粒,大鼠尾静脉注射给药,高效液相色谱法测定不同时间血浆中联苯双酯的浓度,通过3P97程序计算药动学参数。结果:药动学研究表明联苯双酯固体脂质纳米粒消除较慢,生物利用度较高,无论是药物溶液还是纳米混悬液,在大鼠体内的药动学过程均符合二室模型。结论:与药物溶液相比,联苯双酯固体脂质纳米粒具有明显的缓释效果,同时还能提高药物的生物利用度。     

新型纳米结构脂质载体给药系统的研究进展

纳米结构脂质载体是在第1代脂质纳米粒-固体脂质纳米粒的基础上发展起来的一种新型药物给药系统,相比于传统脂质纳米粒,具有载药量高、安全性好、稳定性高等优势,故引起了国内外医药工作者的广泛关注。该文对纳米结构脂质载体的作用特点、脂质材料及稳定性、结构特征、包封率及载药量、制备方法及其应用情况进行了概述,为其在医药领域中的深度开发提供参考。     

Core–shell-type lipid–polymer hybrid nanoparticles as a drug delivery platform

The focus of nanoparticle design over the years has evolved toward more complex nanoscopic core–shell architecture using a single delivery system to combine multiple functionalities within nanoparticles. Core–shell-type lipid–polymer hybrid nanoparticles (CSLPHNs), which combine the mechanical advantages of biodegradable polymeric nanoparticles and biomimetic advantages of liposomes, have emerged as a robust and promising delivery platform. In CSLPHNs, a biodegradable polymeric core is surrounded by a shell composed of layer(s) of phospholipids. The hybrid architecture can provide advantages such as controllable particle size, surface functionality, high drug loading, entrapment of multiple therapeutic agents, tunable drug release profile, and good serum stability. This review focuses on current research trends on CSLPHNs including classification, advantages, methods of preparation, physicochemical characteristics, surface modifications, and immunocompatibility. Additionally, the review deals with applications for cancer chemotherapy, vaccines, and gene therapeutics.From the Clinical EditorThis comprehensive review covers the current applications of core–shell-type lipid–polymer hybrid nanoparticles, which combine the mechanical advantages of biodegradable polymeric nanoparticles and biomimetic advantages of liposomes to enable an efficient drug delivery system.     

聚乙二醇1000维生素E琥珀酸酯在纳米制剂中的应用进展

目的综述聚乙二醇1000维生素E琥珀酸酯(D-α-tocopherol polyethylene glycol 1000 succi-nate,TPGS)在各种纳米制剂中的最新进展。方法查阅国内外相关文献共48篇,对这些文献进行分析、概括和总结。结果 TPGS能够提高药物包封率和细胞吸收,改善药物释放,提高药物生物利用度,并能协同起抗癌疗效。广泛应用于聚合物纳米粒、聚合物胶束、纳米脂质体、纳米药物等纳米给药系统中。结论 TPGS在纳米制剂中有着良好应用前景。     

Polymeric nanoparticles for drug delivery to the central nervous system

The central nervous system (CNS) poses a unique challenge for drug delivery. The blood-brain barrier significantly hinders the passage of systemically delivered therapeutics and the brain extracellular matrix limits the distribution and longevity of locally delivered agents. Polymeric nanoparticles represent a promising solution to these problems. Over the past 40years, substantial research efforts have demonstrated that polymeric nanoparticles can be engineered for effective systemic and local delivery of therapeutics to the CNS. Moreover, many of the polymers used in nanoparticle fabrication are both biodegradable and biocompatible, thereby increasing the clinical utility of this strategy. Here, we review the major advances in the development of polymeric nanoparticles for drug delivery to the CNS.     

Formation, characterization, and fate of inhaled drug nanoparticles

Nanoparticles bring many benefits to pulmonary drug delivery applications, especially for systemic delivery and drugs with poor solubility. They have recently been explored in pressurized metered dose inhaler, nebulizer, and dry powder inhaler applications, mostly in polymeric forms. This article presents a review of processes that have been used to generate pure (non polymeric) drug nanoparticles, methods for characterizing the particles/formulations, their in-vitro and in-vivo performances, and the fate of inhaled nanoparticles.     

PCL/PEG copolymeric nanoparticles: potential nanoplatforms for anticancer agent delivery

Nanotechnology provides researchers with new tools for cancer treatment. Biodegradable polymeric nanoparticles, as an advanced drug delivery system, have promising applications in cancer treatment. Poly(ε-caprolactone)/poly(ethylene glycol) (PCL/PEG) copolymers are biodegradable and amphiphilic, and show potential application in drug delivery. In recent years, PCL/PEG copolymeric nanoparticles, as a potential nanoplatform for anticancer agent delivery, received increasing attention. This paper reviews PCL/PEG copolymer nanoparticles for anticancer agent delivery, including overcoming water insolubility of hydrophobic drug, targeting chemotherapeutic drug to tumor, and delivering genes, vaccines, and diagnostic agents.     

Microencapsulation of lipid nanoparticles containing lipophilic drug

A polymeric emulsion bead, which consists of core and capsule, was prepared. The core is composed of lipid nanoparticles containing lipophilic drug and semi-interpenetrating networks (semi-IPNs) are prepared to provide the capsule composed of sodium alginate and hydroxypropylmethyl cellulose (HPMC). The lipid nanoparticles were encapsulated into the polymeric emulsion bead with high drug loading efficiency, and lovastatin was used as a model drug. For the application as an oral drug delivery system, the enteric coating was performed with polymeric emulsion bead. The drug release pattern was controlled by the composition of capsule materials and environmental pH.     

pH响应性聚合物胶束及其在抗癌药物给药系统中的研究进展

 聚合物纳米粒作为一种有效的药物运送载体已经受到广泛的关注,具有环境响应性的聚合物胶束的制备及应用是目前引人瞩目的研究方向。最近,pH响应性聚合物胶束已被用作抗癌药物的运送载体,其显著的优势就是能够靶向给药于病灶部位,从而降低不良反应,提高抗癌药物的化疗指数。文中综述了pH值响应性的聚合物胶束的两种主要制备策略,即依赖于共聚物骨架中的“可滴定”基团;引入可被酸降解的连接臂,还介绍了pH值响应性聚合物胶束在抗癌药物给药系统中的应用。     

Nanocarriers for cancer-targeted drug delivery

Nanoparticles as drug delivery system have received much attention in recent years, especially for cancer treatment. In addition to improving the pharmacokinetics of the loaded poorly soluble hydrophobic drugs by solubilizing them in the hydrophobic compartments, nanoparticles allowed cancer specific drug delivery by inherent passive targeting phenomena and adopted active targeting strategies. For this reason, nanoparticles-drug formulations are capable of enhancing the safety, pharmacokinetic profiles and bioavailability of the administered drugs leading to improved therapeutic efficacy compared to conventional therapy. The focus of this review is to provide an overview of various nanoparticle formulations in both research and clinical applications with a focus on various chemotherapeutic drug delivery systems for the treatment of cancer. The use of various nanoparticles, including liposomes, polymeric nanoparticles, dendrimers, magnetic and other inorganic nanoparticles for targeted drug delivery in cancer is detailed.     

Nanoencapsulation II. Biomedical applications and current status of peptide and protein nanoparticulate delivery systems

The concept of polymeric nanoparticles for the design of new drug delivery systems emerged a few years ago, and recent rapid advances in nanotechnology have offered a wealth of new opportunities for diagnosis and therapy of various diseases. Recent progress has made possible the engineering of nanoparticles to allow the site-specific delivery of drugs and to improve the pharmacokinetic profile of numerous compounds with biomedical applications such as peptide and protein drugs. Biologically active peptides and their analogues are becoming an increasingly important class of drugs. Their use for human and animal treatment is problematic, however, because some of these drugs are generally ineffective when taken orally and thus have been administered chiefly by the parenteral route. This review covers some of the historical and recent advances of nanotechnology and concludes that polymeric nanoparticles show great promise as a tool for the development of peptide drug delivery systems.