医药用微纳米系统的显微表征

E. Esposito, M. Drechsler, R. Cortesi
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For scanning electron microscopyanalysis, microparticles were metallized by gold coating (Edwards Sputter coat-ing S150) and visualized at 15 – 20 kV with a 360 Stereoscan (Cambridge Instruments, Cambridge, UK). For Cryo-TEM ­analysis­ samples­were­ vitrified­ and­ transferred to a Zeiss EM922Omega (Zeiss SMT, Oberkochen, Germany). Images were recorded by a CCD digital camera (Ultrascan 1000, Gatan) and analyzed using a GMS 1.8 software (Gatan). Conclusion Microscopy is to be considered as an indispensable tool to study drug delivery systems. In particular, scanning electron microscopy is helpful in giving information about micro-sized powders, allowing to identify microspheres and microcapsules, as well as to obtain size distribution of the observed particles. Introduction Microand nanoparticles have attracted pharmaceutical interest in the last decades since they offer a number of advantages with respect to other delivery systems such as: (a) the ability to maintain unaltered physicochemical characteristics for long periods allowing long-term storage; (b) the possible administration through different ways (oral, intramuscular or subcutaneous) depending on their composition and (c) their suitability for industrial production1. Concerning nanosystems, lipid dispersions possess a potential use as matrixes able to dissolve and deliver active molecules in a controlled fashion, thereby improving their bioavailability and reducing side-effects2. In particular, solid lipid nanoparticles (SLN) are delivery systems in which the nano-dispersed phase has a matrix of crystalline solid lipids. SLN are able to protect encapsulated molecules from degradation and modulate their release3,4. Another generation of SLN is represented by nanostructured lipid carriers (NLC) whose matrix is composed of a mixture of solid–liquid lipids able to better solubilise lipophilic drugs5,6. Another type of lipid dispersion able to provide matrices for sustained­ drug­ release­ is­ typified­ by­ monooleine aqueous dispersions (MAD). MAD are heterogeneous systems generated by the dispersion of an amphiphilic lipid, such as monoolein, in water. They are constituted of complex lyotropic liquid crystalline nanostructures like micellar, lamellar, hexagonal and cubic phases, the predominance of one species over Abstract Introduction This review provides an overview of the use of microscopy as a tool to characterise shape and dimension of micro and nanoparticulate systems. In­ the­ pharmaceutical­ field,­ the­ use of microscopy has been exerted an important role since the advent of micro and nanotechnology. Indeed, the morphology of particles and their­ inner­ structure­ does­ influence­ the modalities of administration and release of encapsulated drugs. Scanning electron microscopy can be employed to study the morphology of dry powders. In particular microparticles made of polymers can be well visualised and their diameters can be measured. By cutting the powder during sample preparation, it is possible to obtain important information about the inner morphology of the microstructures, discriminating either the capsule or the sphere microstructure. Cryo transmission electron microscopy is a precious tool for characterising colloidal systems. In particular, external as well as internal shape of nanoparticulate systems such as solid lipid nanoparticles or lyotropic mesophases can be well identified.­Moreover,­size­of­disperse­ phase and the overall structure of the dispersion can be monitored. 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Methodology Microparticles were produced by the ‘solvent evaporation method’. Solid lipid nanoparticlesand nanostructured lipid carriers were prepared by stirring, followed by ultrasonication. Monooleine aqueous dispersionswere produced by the hydrotrope or by the hot homogenization methods. For scanning electron microscopyanalysis, microparticles were metallized by gold coating (Edwards Sputter coat-ing S150) and visualized at 15 – 20 kV with a 360 Stereoscan (Cambridge Instruments, Cambridge, UK). For Cryo-TEM ­analysis­ samples­were­ vitrified­ and­ transferred to a Zeiss EM922Omega (Zeiss SMT, Oberkochen, Germany). Images were recorded by a CCD digital camera (Ultrascan 1000, Gatan) and analyzed using a GMS 1.8 software (Gatan). Conclusion Microscopy is to be considered as an indispensable tool to study drug delivery systems. In particular, scanning electron microscopy is helpful in giving information about micro-sized powders, allowing to identify microspheres and microcapsules, as well as to obtain size distribution of the observed particles. Introduction Microand nanoparticles have attracted pharmaceutical interest in the last decades since they offer a number of advantages with respect to other delivery systems such as: (a) the ability to maintain unaltered physicochemical characteristics for long periods allowing long-term storage; (b) the possible administration through different ways (oral, intramuscular or subcutaneous) depending on their composition and (c) their suitability for industrial production1. Concerning nanosystems, lipid dispersions possess a potential use as matrixes able to dissolve and deliver active molecules in a controlled fashion, thereby improving their bioavailability and reducing side-effects2. In particular, solid lipid nanoparticles (SLN) are delivery systems in which the nano-dispersed phase has a matrix of crystalline solid lipids. SLN are able to protect encapsulated molecules from degradation and modulate their release3,4. Another generation of SLN is represented by nanostructured lipid carriers (NLC) whose matrix is composed of a mixture of solid–liquid lipids able to better solubilise lipophilic drugs5,6. Another type of lipid dispersion able to provide matrices for sustained­ drug­ release­ is­ typified­ by­ monooleine aqueous dispersions (MAD). MAD are heterogeneous systems generated by the dispersion of an amphiphilic lipid, such as monoolein, in water. 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引用次数: 6

摘要

我们研究小组最近开发的表征微粒和纳米系统的技术。特别地,聚酯或丙烯酸聚合物微粒芬维甲酸管理提出了这里。此外,关于纳米系统,固体脂质纳米颗粒,纳米结构的脂质载体强的松和氯霉唑给药和单油胺水分散进行了讨论。方法采用“溶剂蒸发法”制备微颗粒。采用搅拌法制备固体脂质纳米颗粒和纳米结构脂质载体。单油胺水分散体采用水相法或热均质法制备。为了进行扫描电子显微镜分析,用金涂层(Edwards溅射涂层S150)将微粒金属化,并在15 - 20 kV下用360度立体扫描仪(Cambridge Instruments, Cambridge, UK)进行可视化。用于低温透射电镜分析-样品-玻璃化-并转移到蔡司EM922Omega(蔡司SMT, Oberkochen,德国)。图像由CCD数码相机(Ultrascan 1000, Gatan)记录,并使用gms1.8软件(Gatan)进行分析。结论显微镜是研究给药系统不可缺少的工具。特别是,扫描电子显微镜有助于提供有关微尺寸粉末的信息,允许识别微球和微胶囊,以及获得所观察颗粒的尺寸分布。在过去的几十年里,微纳米颗粒已经引起了制药领域的兴趣,因为它们提供了一些相对于其他递送系统的优势,例如:(a)能够长时间保持不变的物理化学特性,允许长期储存;(b)根据其成分,可能通过不同方式(口服、肌肉注射或皮下注射)给药;(c)它们是否适合工业生产。在纳米系统中,脂质分散体作为基质具有潜在的用途,能够以可控的方式溶解和输送活性分子,从而提高其生物利用度并减少副作用2。特别是,固体脂质纳米颗粒(SLN)是一种输送系统,其中纳米分散相具有结晶固体脂质的基质。SLN能够保护被封装的分子免受降解并调节其释放3,4。另一代SLN以纳米结构脂质载体(NLC)为代表,其基质由固体-液体脂质混合物组成,能够更好地溶解亲脂性药物5,6。另一种能够为药物缓释提供基质的脂质分散体是单油碱水相分散体(MAD)。MAD是由两亲性脂质(如单油质)在水中分散而产生的非均相系统。它们是由胶束相、片层相、六方相和立方相等复杂的溶致液晶纳米结构组成的,其中一种比另一种更占优势。摘要:本文综述了使用显微镜作为表征微观和纳米颗粒系统形状和尺寸的工具的概况。在制药领域,显微技术的应用自微纳米技术出现以来发挥了重要作用。事实上,颗粒的形态及其内部结构确实会影响胶囊化药物的给药和释放方式。扫描电镜可以用来研究干粉的形貌。特别是由聚合物制成的微粒可以很好地可视化,并且可以测量它们的直径。通过在样品制备过程中切割粉末,可以获得有关微观结构内部形态的重要信息,区分胶囊或球体微观结构。低温透射电子显微镜是表征胶体系统的宝贵工具。特别是,可以很好地识别固体脂质纳米颗粒或溶性中间相等纳米颗粒系统的外部和内部形状。此外,还可以监测分散相的大小和分散体的整体结构。我们提供了关于使用电子显微镜的概述
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Microscopy characterisation of micro- and nanosystems for pharmaceutical use
technique for characterising microparticles and nanosystems recently developed by our research group. In particular, polyester or acrylic polymer microparticles for fenretinide administration are presented here. Moreover, with regard to nanosystems, solid lipid nanoparticles, nanostructured lipid carriers for prednisone and clotrimazole administration and monooleine aqueous dispersion are discussed. Methodology Microparticles were produced by the ‘solvent evaporation method’. Solid lipid nanoparticlesand nanostructured lipid carriers were prepared by stirring, followed by ultrasonication. Monooleine aqueous dispersionswere produced by the hydrotrope or by the hot homogenization methods. For scanning electron microscopyanalysis, microparticles were metallized by gold coating (Edwards Sputter coat-ing S150) and visualized at 15 – 20 kV with a 360 Stereoscan (Cambridge Instruments, Cambridge, UK). For Cryo-TEM ­analysis­ samples­were­ vitrified­ and­ transferred to a Zeiss EM922Omega (Zeiss SMT, Oberkochen, Germany). Images were recorded by a CCD digital camera (Ultrascan 1000, Gatan) and analyzed using a GMS 1.8 software (Gatan). Conclusion Microscopy is to be considered as an indispensable tool to study drug delivery systems. In particular, scanning electron microscopy is helpful in giving information about micro-sized powders, allowing to identify microspheres and microcapsules, as well as to obtain size distribution of the observed particles. Introduction Microand nanoparticles have attracted pharmaceutical interest in the last decades since they offer a number of advantages with respect to other delivery systems such as: (a) the ability to maintain unaltered physicochemical characteristics for long periods allowing long-term storage; (b) the possible administration through different ways (oral, intramuscular or subcutaneous) depending on their composition and (c) their suitability for industrial production1. Concerning nanosystems, lipid dispersions possess a potential use as matrixes able to dissolve and deliver active molecules in a controlled fashion, thereby improving their bioavailability and reducing side-effects2. In particular, solid lipid nanoparticles (SLN) are delivery systems in which the nano-dispersed phase has a matrix of crystalline solid lipids. SLN are able to protect encapsulated molecules from degradation and modulate their release3,4. Another generation of SLN is represented by nanostructured lipid carriers (NLC) whose matrix is composed of a mixture of solid–liquid lipids able to better solubilise lipophilic drugs5,6. Another type of lipid dispersion able to provide matrices for sustained­ drug­ release­ is­ typified­ by­ monooleine aqueous dispersions (MAD). MAD are heterogeneous systems generated by the dispersion of an amphiphilic lipid, such as monoolein, in water. They are constituted of complex lyotropic liquid crystalline nanostructures like micellar, lamellar, hexagonal and cubic phases, the predominance of one species over Abstract Introduction This review provides an overview of the use of microscopy as a tool to characterise shape and dimension of micro and nanoparticulate systems. In­ the­ pharmaceutical­ field,­ the­ use of microscopy has been exerted an important role since the advent of micro and nanotechnology. Indeed, the morphology of particles and their­ inner­ structure­ does­ influence­ the modalities of administration and release of encapsulated drugs. Scanning electron microscopy can be employed to study the morphology of dry powders. In particular microparticles made of polymers can be well visualised and their diameters can be measured. By cutting the powder during sample preparation, it is possible to obtain important information about the inner morphology of the microstructures, discriminating either the capsule or the sphere microstructure. Cryo transmission electron microscopy is a precious tool for characterising colloidal systems. In particular, external as well as internal shape of nanoparticulate systems such as solid lipid nanoparticles or lyotropic mesophases can be well identified.­Moreover,­size­of­disperse­ phase and the overall structure of the dispersion can be monitored. We provide an overview about the use of electron microscopy as
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