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1乳化蒸发结合高压均质法制备辅酶Q10前体纳米脂质体前体脂质体(proliposome),又称重建脂质体,系脂质体的前体形式,通常为干燥且具有良好流动性能的粉末,这种前体...
1 乳化蒸发结合高压均质法制备辅酶Q10前体纳米脂质体
前体脂质体(proliposome),又称重建脂质体,系脂质体的前体形式,通常为干燥且具有良好流动性能的粉末,这种前体脂质体一般不具备完整的脂质双分子膜.而是双分子脂质膜的碎片或是脂质膜材附着在支撑剂结晶上,或者与支撑剂均匀混合,应用前与水水合即可形成完整的脂质体。它具有脂质体制剂的一系列作用特点,又可解决其易水解、聚集、分层、药物渗漏和高温灭菌不稳定等问题,为脂质体的工业化生产奠定了设计基础,因而在国内外已引起广泛研究[120-121]。
前体脂质体的制备方法较简单,贮存稳定性比相应的脂质体混悬液提高,对脂质体的放大生产和应用都具有开拓性的实际意义。但前体脂质体商品化进程至今仍较缓慢的主要原因是
(1)前体脂质体的质量不易控制,如仅靠稀释或复水化操作制备的脂质体粒径分布不够均匀 (2)
药物的包封率常达不到要求。(3)靶向性有待提高,这主要是由于在生物体内, 脂质体粒径的大小决定了其在体内与细胞作用的部位以及在体内吸收和分布。如静脉注射条件下,小的脂质体能够很快到达肝细胞;中等大小的脂质体能在血液循环中保持相当一段时间;较大的脂质体则不能到达受药部位[122-123]。
综合以上原因,本研究决定采用乳化蒸发结合高压均质法制备辅酶Q10前体纳米脂质体。这种改良的方法是基于乳化蒸发法:即首先形成O/W型乳液,待有机溶剂减压挥尽后,药物析晶在单层磷脂膜的内部,由于这种结构并不稳定,而使膜一边内陷,最后两端融合成双层膜结构。所形成的脂质体经过高压均质改造粒径后,加入附加剂冷冻干燥后即获得干燥的前体脂质体粉末。这种工艺方法不仅可以获得纳米级的前体脂质体,用以提高靶向性和产品的质量稳定性,也具有防止磷脂空气氧化、操作简便,易于工业化生产的特点。
1.1 实验材料与设备RE-52AA型旋转蒸发仪,上海青浦沪西仪器厂;KQ-250DB型数控超声波清洗器,巩义市予华仪器有限责任公司;Scientz-10N型真空冷冻干燥机,宁波新芝生物科技股份有限公司;NS1001L
高压均质机,意大利 GEA Niro Soavi公司;Biofuge 22R型低温高速离心机,德国Heraeus公司
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前体脂质体(proliposome),又称重建脂质体,系脂质体的前体形式,通常为干燥且具有良好流动性能的粉末,这种前体脂质体一般不具备完整的脂质双分子膜.而是双分子脂质膜的碎片或是脂质膜材附着在支撑剂结晶上,或者与支撑剂均匀混合,应用前与水水合即可形成完整的脂质体。它具有脂质体制剂的一系列作用特点,又可解决其易水解、聚集、分层、药物渗漏和高温灭菌不稳定等问题,为脂质体的工业化生产奠定了设计基础,因而在国内外已引起广泛研究[120-121]。
前体脂质体的制备方法较简单,贮存稳定性比相应的脂质体混悬液提高,对脂质体的放大生产和应用都具有开拓性的实际意义。但前体脂质体商品化进程至今仍较缓慢的主要原因是
(1)前体脂质体的质量不易控制,如仅靠稀释或复水化操作制备的脂质体粒径分布不够均匀 (2)
药物的包封率常达不到要求。(3)靶向性有待提高,这主要是由于在生物体内, 脂质体粒径的大小决定了其在体内与细胞作用的部位以及在体内吸收和分布。如静脉注射条件下,小的脂质体能够很快到达肝细胞;中等大小的脂质体能在血液循环中保持相当一段时间;较大的脂质体则不能到达受药部位[122-123]。
综合以上原因,本研究决定采用乳化蒸发结合高压均质法制备辅酶Q10前体纳米脂质体。这种改良的方法是基于乳化蒸发法:即首先形成O/W型乳液,待有机溶剂减压挥尽后,药物析晶在单层磷脂膜的内部,由于这种结构并不稳定,而使膜一边内陷,最后两端融合成双层膜结构。所形成的脂质体经过高压均质改造粒径后,加入附加剂冷冻干燥后即获得干燥的前体脂质体粉末。这种工艺方法不仅可以获得纳米级的前体脂质体,用以提高靶向性和产品的质量稳定性,也具有防止磷脂空气氧化、操作简便,易于工业化生产的特点。
1.1 实验材料与设备RE-52AA型旋转蒸发仪,上海青浦沪西仪器厂;KQ-250DB型数控超声波清洗器,巩义市予华仪器有限责任公司;Scientz-10N型真空冷冻干燥机,宁波新芝生物科技股份有限公司;NS1001L
高压均质机,意大利 GEA Niro Soavi公司;Biofuge 22R型低温高速离心机,德国Heraeus公司
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翻译如下:Preparation of coenzyme Q10 precursor liposome 1 emulsion evaporation combined with high-pressure homogenization method
Precursor liposome (proliposome), also known as the reconstruction of liposome, the precursor form of liposome, usually dry and have good flow properties of the powder, the precursor liposome generally do not have the integrity of the bilayer lipid membrane. But the bilayer lipid membrane fragments or lipid membrane attached to a support agent crystallization, or with the support agent are evenly mixed, application and water hydration can form intact liposomes. It has a series of characteristics of liposome preparations, and can solve the problem of easy hydrolysis, aggregation, hierarchical, the drug leakage and high-temperature sterilization is not stable, laid the basis for the design for the industrial production of liposomes, so at home and abroad has aroused extensive research on [120-121].
Preparation method is simple, storage stability than liposomes corresponding suspension to improve, will open up new practical significance of enlarging the production and application of liposomes. But the main reason proliposome commercialization process is still relatively slow is
(1) Proliposomes quality is difficult to control, such as by dilution or rehydration preparation of liposome size distribution is not uniform enough (2)
The drug entrapment efficiency is not up to the requirements. (3) targeting remains to be improved, this is mainly because in the organism, the size of liposome size determines its in vivo and cell function and the location of the in vivo absorption and distribution. Such as the condition of intravenous injection, liposomes small can reach the liver cells soon; liposome size to maintain a considerable period of time in the blood circulation; larger liposomes can not reach the part receiving the medicine [122-123].
For all of these reasons, we have decided to adopt emulsion evaporation to prepare coenzyme Q10 precursor liposome with high pressure homogenization method. This method is based on modified emulsion evaporation method: first the formation of O/W emulsion, the organic solvent volatile after decompression, internal medicine crystallization in single phospholipid membrane, because the structure is not stable, and the film side invagination, finally ends into a double membrane structure. The formation of the liposomes modified high pressure homogenization particle size, adding additional agent after freeze drying to obtain proliposome powder dry. This method can not only obtain the precursor liposome nanometer level, in order to improve the targeting and product quality stability, but also can prevent the lipid oxidation, simple operation, easy industrialization production.
1.1 experimental materials and equipment of RE-52AA type rotary evaporator, Shanghai Qingpu Huxi instrument factory; KQ-250DB NC Ultrasonic cleaner, Gongyi Yuhua Instrument Co., Ltd.; Scientz-10N type vacuum freezing dryer, Ningbo scientz biotechnology Polytron Technologies Inc; NS1001L
High pressure homogenizer, Italy GEA Niro Soavi; Biofuge 22R type low speed centrifuge, the German company Heraeus
Precursor liposome (proliposome), also known as the reconstruction of liposome, the precursor form of liposome, usually dry and have good flow properties of the powder, the precursor liposome generally do not have the integrity of the bilayer lipid membrane. But the bilayer lipid membrane fragments or lipid membrane attached to a support agent crystallization, or with the support agent are evenly mixed, application and water hydration can form intact liposomes. It has a series of characteristics of liposome preparations, and can solve the problem of easy hydrolysis, aggregation, hierarchical, the drug leakage and high-temperature sterilization is not stable, laid the basis for the design for the industrial production of liposomes, so at home and abroad has aroused extensive research on [120-121].
Preparation method is simple, storage stability than liposomes corresponding suspension to improve, will open up new practical significance of enlarging the production and application of liposomes. But the main reason proliposome commercialization process is still relatively slow is
(1) Proliposomes quality is difficult to control, such as by dilution or rehydration preparation of liposome size distribution is not uniform enough (2)
The drug entrapment efficiency is not up to the requirements. (3) targeting remains to be improved, this is mainly because in the organism, the size of liposome size determines its in vivo and cell function and the location of the in vivo absorption and distribution. Such as the condition of intravenous injection, liposomes small can reach the liver cells soon; liposome size to maintain a considerable period of time in the blood circulation; larger liposomes can not reach the part receiving the medicine [122-123].
For all of these reasons, we have decided to adopt emulsion evaporation to prepare coenzyme Q10 precursor liposome with high pressure homogenization method. This method is based on modified emulsion evaporation method: first the formation of O/W emulsion, the organic solvent volatile after decompression, internal medicine crystallization in single phospholipid membrane, because the structure is not stable, and the film side invagination, finally ends into a double membrane structure. The formation of the liposomes modified high pressure homogenization particle size, adding additional agent after freeze drying to obtain proliposome powder dry. This method can not only obtain the precursor liposome nanometer level, in order to improve the targeting and product quality stability, but also can prevent the lipid oxidation, simple operation, easy industrialization production.
1.1 experimental materials and equipment of RE-52AA type rotary evaporator, Shanghai Qingpu Huxi instrument factory; KQ-250DB NC Ultrasonic cleaner, Gongyi Yuhua Instrument Co., Ltd.; Scientz-10N type vacuum freezing dryer, Ningbo scientz biotechnology Polytron Technologies Inc; NS1001L
High pressure homogenizer, Italy GEA Niro Soavi; Biofuge 22R type low speed centrifuge, the German company Heraeus
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等了很久都不见高手现身,只好由我献丑了!!
The preparation of coenzyme Q10 Pronanoliposomes by applying the combined methods of
emulsion solvent evaporation technique and high pressure homogenization.
Proliposome, also called Reconstituted Liposome, it is the precursor form of liposome, generally it is in dry powder form with excellent fluidity. This kind of proliposome usually does not have a complete bilayer lipoid membrane, rather, it is the fragments of double molecular lipoid membrane or lipoid membrane materials attached to propping agent crystals, or homogenizes with propping agent; before application, it hydrates with water to form
complete liposome. Proliposome possesses a series of action characteristics of liposome preparation, and solves the problems of easy hydrolysis, aggregation, stratification, drug leakage and unstable heat sterilization; these have laid the design foundation for the commercial production of liposome, and given rise to extensive researches here and abroad. [120-121]
The preparation method of proliposome is relatively simple; the storage stability is much better than liposome suspension, this has a practical pioneering significance on the expanded
production and application of liposome. However, the process of commercialization of proliposome is still very slow up to now, the reasons are: 1) The quality of proliposome is not easy to control; 2) The entrapment efficiency is often not up to requirements; 3) The targeting leaves much to be desired; this is mainly because in the body of living creatures, the particle size of liposome decides its action location with the cells in the body, as well as the absorption and distribution. For example, under the condition of intravenous injection, the smaller liposome can quickly reach the liver cells; the medium size liposome can remain in blood circulation for quite some time; but the larger liposome cannot reach the administration location [122-123].
Based on the above reasons, this research decides to prepare coenzyme Q10 Pronanoliposomes by adopting the combined methods of emulsion solvent evaporation technique and high pressure homogenization. This modified technique is based on emulsified evaporation method: Initially create o/w typed emulsion, after the complete decompression
of the organic solvent, due to the unstable structure, the drug crystallization within the phospholipid membrane causes one side of the membrane to invaginate, and finally the two ends fuse together and become a bi-layer membrane structure. After the created liposome has been subjected to high pressure homogenization and changed into grain sizes, and the proliposome in dry powder form is obtained after freeze-dried by adding additional agent. This process not only can obtain proliposome in nano-scale which can enhance the targeting and the stability of product quality, but can also prevent atmospheric oxidation of the phospholipid, and the operation is simple and convenient, suitable for industrial production.
1.1 Experiment materials and equipment: Rotary evaporator model RE-52AA (Shanghai Qingpu Huxi Instrument Factory), CNC Ultrasonic Cleaner model KQ-250DB (Gongyi Yuhua Instrument Co., Ltd.), vacuum freeze dryer model Scientz-10N (Ningbo scientz biotechnology Polytron Technologies Inc), High pressure homogenizer NS 1001L (GEA Niro Soavi Company, Italy), Hypothermic high speed centrifugal machine model Biofuge 22R (Heraeus Company, Germany).
【英语牛人团】
The preparation of coenzyme Q10 Pronanoliposomes by applying the combined methods of
emulsion solvent evaporation technique and high pressure homogenization.
Proliposome, also called Reconstituted Liposome, it is the precursor form of liposome, generally it is in dry powder form with excellent fluidity. This kind of proliposome usually does not have a complete bilayer lipoid membrane, rather, it is the fragments of double molecular lipoid membrane or lipoid membrane materials attached to propping agent crystals, or homogenizes with propping agent; before application, it hydrates with water to form
complete liposome. Proliposome possesses a series of action characteristics of liposome preparation, and solves the problems of easy hydrolysis, aggregation, stratification, drug leakage and unstable heat sterilization; these have laid the design foundation for the commercial production of liposome, and given rise to extensive researches here and abroad. [120-121]
The preparation method of proliposome is relatively simple; the storage stability is much better than liposome suspension, this has a practical pioneering significance on the expanded
production and application of liposome. However, the process of commercialization of proliposome is still very slow up to now, the reasons are: 1) The quality of proliposome is not easy to control; 2) The entrapment efficiency is often not up to requirements; 3) The targeting leaves much to be desired; this is mainly because in the body of living creatures, the particle size of liposome decides its action location with the cells in the body, as well as the absorption and distribution. For example, under the condition of intravenous injection, the smaller liposome can quickly reach the liver cells; the medium size liposome can remain in blood circulation for quite some time; but the larger liposome cannot reach the administration location [122-123].
Based on the above reasons, this research decides to prepare coenzyme Q10 Pronanoliposomes by adopting the combined methods of emulsion solvent evaporation technique and high pressure homogenization. This modified technique is based on emulsified evaporation method: Initially create o/w typed emulsion, after the complete decompression
of the organic solvent, due to the unstable structure, the drug crystallization within the phospholipid membrane causes one side of the membrane to invaginate, and finally the two ends fuse together and become a bi-layer membrane structure. After the created liposome has been subjected to high pressure homogenization and changed into grain sizes, and the proliposome in dry powder form is obtained after freeze-dried by adding additional agent. This process not only can obtain proliposome in nano-scale which can enhance the targeting and the stability of product quality, but can also prevent atmospheric oxidation of the phospholipid, and the operation is simple and convenient, suitable for industrial production.
1.1 Experiment materials and equipment: Rotary evaporator model RE-52AA (Shanghai Qingpu Huxi Instrument Factory), CNC Ultrasonic Cleaner model KQ-250DB (Gongyi Yuhua Instrument Co., Ltd.), vacuum freeze dryer model Scientz-10N (Ningbo scientz biotechnology Polytron Technologies Inc), High pressure homogenizer NS 1001L (GEA Niro Soavi Company, Italy), Hypothermic high speed centrifugal machine model Biofuge 22R (Heraeus Company, Germany).
【英语牛人团】
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1. Use the emulsification-evaporation process in combination with the high pressure homogenization (HPH) method to prepare the Q10 nano proliposome
The proliposome is also known as the reconstruction liposome and a pro form of liposome in a state of dry powder with good fluidity. Generally this type of proliposome doesn’t have complete lipid bi-layers but contains the fragments of it, or it is a kind of liposome with the membrane material adhering to the proppant crystallization, or which can be formed into the complete liposome when mixed uniformly with the proppant through hydration before being applied. It not only has the functions of other liposome preparations, but can also solve the instability problem caused by hydrolysis, aggregation, layering, drug leakage and high temperature sterilization. It has laid down the groundwork for industrial use of the liposome and led to extensive research both in China and the world.
The relatively simple method for preparing the proliposome as well as the higher storage stability than the liposome suspension is practically meaningful for the mass production and wider application of the liposome. As of now, however, the commercialization of the proliposome is still rather slow mainly for the following reasons: 1) the proliposome quality is hard to control. For example, the liposome may not have uniform particle size distribution (PSD) when made only through the dilution or rehydration process; 2) the drugs often fail to meet the required encapsulation efficiency, and 3) the drug targeting needs to be improved. This is because in organisms, where the liposome can take effect on cells and how fast it can distribute in and absorbed by the body are dependent on the particle size of the liposome. For example with intravenous injection, the small liposome particles can quickly reach the liver cells; the medium sized particles can remain in the blood circulation for a considerable length of time, but the large liposome can hardly get to the targeted area.
With the above reasons summarized, the researcher has decided to use the emulsification-evaporation process together with the HPH method to prepare the coenzyme Q10 nano proliposome. This improved method is based on the emulsification-evaporation process: first we prepare the O/W type emulsion, and then wait for the drug to crystallize inside the lecithoid monolayer when the organic solvent is completely evaporated. Because this is an instable structure which causes one side of the layer to invaginate, finally both ends will fuse to form a bi-layer structure. The dry proliposome powder can be obtained from the liposome thus produced with its particles resized through the HPH process and frozen dried by additives. The process can not only produce the nano-level proliposome to improve targeting and product quality, but also has advantages such as protecting phospholipids against oxidation, simple to handle and easy for industrial production.
1.1 Material and equipment used in experiments: RE-52AA Rotary Evaporator (Shanghai Qingpu Huxi Instrument Plant); KQ-250DB NC Ultrasonic Cleaner (Gonyi Yuhua Instrument Co., Ltd.); Scientz-10N Vacuum Freeze Drier (Ningbo Xinzhi Biotech Co., Ltd.); NS1001L High Pressure Homogenizer(GEA Niro Soavi, Italy); Biofuge 22R Low-temperature High Speed Centrifuge (Heraeus, Germany)
The proliposome is also known as the reconstruction liposome and a pro form of liposome in a state of dry powder with good fluidity. Generally this type of proliposome doesn’t have complete lipid bi-layers but contains the fragments of it, or it is a kind of liposome with the membrane material adhering to the proppant crystallization, or which can be formed into the complete liposome when mixed uniformly with the proppant through hydration before being applied. It not only has the functions of other liposome preparations, but can also solve the instability problem caused by hydrolysis, aggregation, layering, drug leakage and high temperature sterilization. It has laid down the groundwork for industrial use of the liposome and led to extensive research both in China and the world.
The relatively simple method for preparing the proliposome as well as the higher storage stability than the liposome suspension is practically meaningful for the mass production and wider application of the liposome. As of now, however, the commercialization of the proliposome is still rather slow mainly for the following reasons: 1) the proliposome quality is hard to control. For example, the liposome may not have uniform particle size distribution (PSD) when made only through the dilution or rehydration process; 2) the drugs often fail to meet the required encapsulation efficiency, and 3) the drug targeting needs to be improved. This is because in organisms, where the liposome can take effect on cells and how fast it can distribute in and absorbed by the body are dependent on the particle size of the liposome. For example with intravenous injection, the small liposome particles can quickly reach the liver cells; the medium sized particles can remain in the blood circulation for a considerable length of time, but the large liposome can hardly get to the targeted area.
With the above reasons summarized, the researcher has decided to use the emulsification-evaporation process together with the HPH method to prepare the coenzyme Q10 nano proliposome. This improved method is based on the emulsification-evaporation process: first we prepare the O/W type emulsion, and then wait for the drug to crystallize inside the lecithoid monolayer when the organic solvent is completely evaporated. Because this is an instable structure which causes one side of the layer to invaginate, finally both ends will fuse to form a bi-layer structure. The dry proliposome powder can be obtained from the liposome thus produced with its particles resized through the HPH process and frozen dried by additives. The process can not only produce the nano-level proliposome to improve targeting and product quality, but also has advantages such as protecting phospholipids against oxidation, simple to handle and easy for industrial production.
1.1 Material and equipment used in experiments: RE-52AA Rotary Evaporator (Shanghai Qingpu Huxi Instrument Plant); KQ-250DB NC Ultrasonic Cleaner (Gonyi Yuhua Instrument Co., Ltd.); Scientz-10N Vacuum Freeze Drier (Ningbo Xinzhi Biotech Co., Ltd.); NS1001L High Pressure Homogenizer(GEA Niro Soavi, Italy); Biofuge 22R Low-temperature High Speed Centrifuge (Heraeus, Germany)
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不行,跳过了。准确翻译可能得要4-10个小时,除非是双语专业人士。
追问
可以先用谷歌翻译,在调整一下语法顺序,可以给你300分
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分是挺高啊,不过翻译挺费劲,建议使用机器翻译的基础上自己在进行修改,这样会比较快一些!
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