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abstract:
Nano-emulsification technology is the abbreviation of Nano-emulsion technology, which is a pharmaceutical technology to obtain nano-sized drug particles by emulsifying water phase and oil phase under the action of emulsifier. It has many advantages in clinical application of veterinary drugs, such as integrating oil phase and water phase, increasing drug solubility, improving drug bioavailability and avoiding first-pass effect of liver. However, there are also some shortcomings, such as high drug cost, short shelf life, and affecting standard testing. It is believed that with the development of science and technology, the problem that nano-emulsion technology is difficult to popularize due to its shortcomings will be gradually solved and can be widely used in aquaculture in the near future.
Key words:
Nanoemulsion; Nanotechnology; Veterinary drugs; Promotion; Application;
Introduction:
Nano-emulsification technology is the abbreviation of nano-emulsification technology. Nano-emulsion is essentially a kind of emulsion, which is a technology that uses a special' emulsification' process to prepare drugs into nano-sized small emulsified particles under the action of emulsifier [1]. Compared with ordinary dosage forms, nano-emulsion drug particles are smaller, the specific surface area is larger, the bioavailability is higher, and the drug effect is more ideal. In order to help you know more about nano-emulsion technology, the author communicates with you on this topic.
1, nanoemulsion
Nano-emulsion is a dosage form of medicine, which consists of water phase, oil phase and surfactant. Some drugs also add cosurfactants to make the system more stable [2]. Nano-emulsion was used in veterinary drug products by enterprises as early as 1990s, but it was not widely used in veterinary drug clinic at that time due to various reasons, such as insufficient advanced emulsification equipment, high manufacturing cost and low market acceptance. With the development of animal husbandry and the continuous progress of the times, the supervision of veterinary drugs has increased unprecedentedly, and there are fewer and fewer irregular veterinary drugs on the market. More than 90% of them are national standard drugs made according to national, local or industry standards. In order to fully reflect the clinical effect of national standard drugs, the first is the compatibility technology of drugs, and the second is the need to improve the bioavailability of drugs themselves. Based on the above background, nano-emulsion technology came into being in recent years, and it has been applied in chemical medicine, Chinese and veterinary drugs, feed additives and other fields.
2. Advantages of nanoemulsion
Nano-emulsion has many advantages in clinical application of veterinary drugs, such as integrating oil phase and water phase, increasing drug solubility, improving drug bioavailability and avoiding first-pass effect of liver.
2. 1, making the oil phase and water phase * * * as a whole.
Nanoemulsion system consists of oil phase, water phase, surfactant and cosurfactant, among which surfactant is also called emulsifier. In its molecular structure, one end is hydrophilic and the other end is lipophilic. This special structure can make the system dissolve the oil phase in water or the water phase in oil under the action of surfactant. The former is also called "oil-in-water" nanoemulsion, and the latter is called "water-in-oil" nanoemulsion. As long as the appropriate formula is selected, and the hydrophilic-lipophilic balance value (HLB value) of the surfactant itself is the same or similar to that required for oil phase emulsification, the prepared system is relatively stable, and the oil phase and the water phase can be very evenly blended, instead of the oil phase floating on the water phase and delaminating.
2.2, increase drug solubility
Some drugs are insoluble in water, but can be dissolved in some oils. Using this principle, drugs can be dissolved in oil first, and then the oil phase can be dissolved in water under the action of surfactants through nano-emulsification technology, thus increasing the solubility of drugs in water. Generally speaking, the drug loading of drugs prepared with nanoemulsion as carrier is usually between 0. 1% ~ 5%. Too low drug loading rate will lose its meaning, and too high drug loading rate will lead to system instability. Drugs are easy to precipitate during later storage, especially when they are resistant to low temperature and easy to precipitate in winter. However, compared with ordinary dosage forms, nano-emulsion significantly improves the solubility of drugs in water.
2.3, improve the bioavailability of drugs.
The droplet size of nanoemulsion is generally below 100nm, and some drugs can even reach 10nm. With such a small particle size, it is easy to penetrate the cell membrane or intercellular space after oral administration and enter the systemic circulation. This small size effect is an important point that distinguishes nanoemulsion from other dosage forms. In addition, the specific surface area of the drug is greatly increased after the particle size is reduced, and the contact area with target organs and cells is also increased, which finally improves the bioavailability of the drug. Taking tilmicosin, a commonly used veterinary drug in clinic, as an example, it was found that the dosage form of ordinary oral liquid was only about 0.6 ~ 0.7 times that of nano-emulsion. The improvement of drug bioavailability is conducive to reducing the dosage and shortening the course of treatment, thus reducing the treatment cost, reducing the drug resistance of pathogenic bacteria and solving the food safety problems caused by veterinary drug residues.
2.4. Avoid the first-pass effect of liver.
Nanoemulsion is different from other preparations. Because the drug is dissolved in the oil phase, and the oil phase is divided into lipid substances, after entering the intestine, its absorption does not pass through the small intestinal blood vessels, but first enters the intestinal lymphatic vessels, and then flows into the blood through lymphatic circulation. In this way, drugs do not enter the portal vein of the liver through the intestinal vein, and then enter the systemic circulation through the liver, thus avoiding the inactivation of liver drug enzymes and effectively avoiding the first-pass effect of the liver. This special absorption method makes it unnecessary to double the first dose, which not only saves the cost of medication, but also reduces the damage to the liver, killing two birds with one stone.
3. Disadvantages of nanoemulsion
Although nano-emulsion has many advantages in clinical application, it also has some inevitable disadvantages. For example, the preparation cost is relatively high. The technology of nano-emulsion is mostly prepared by high-speed emulsifying machine, which requires high equipment investment and process requirements. In addition, the market price of its own surfactant is not low. The content of surfactant in the actual nano-emulsion stock solution can account for 65,438+08% ~ 36%. These costs add up. In addition, nanoemulsion is a liquid preparation, and its stability is worse than that of solid preparation. The shelf life of drugs is usually 6 ~ 18 months, while the shelf life of solid preparations is 2 ~ 3 years. In traditional Chinese medicine preparations, especially oral liquid preparations and injection preparations, there is a thin-layer test in the process of testing products according to national standards, in which the quality of products can be judged by comparing the positions of strips, but the existence of surfactants will affect the results of thin-layer test, which is also the reason why many traditional Chinese medicine liquid preparations can not use nano-emulsion technology. Although there are still many difficulties in the popularization and application of nano-emulsion technology, I believe that with the continuous development of science and technology, the difficulties in the popularization of this technology will be gradually overcome.
4. Summary
Nano-emulsification technology is a new pharmaceutical preparation technology, which belongs to nano-technology. Because the drug particles reach the nanometer level, this small size effect directly solves many problems that traditional technology can't solve [3]. At present, many veterinary drug giants have made florfenicol, tilmicosin, oxytetracycline, erythromycin and other drugs into nano-emulsions for clinical use, and nano-vitamins are the most widely used in the field of additives. In the field of plant essential oils, peppermint oil, oregano oil, carvacrol, forsythia oil and eucalyptus oil are also made into nanoemulsions, which are used in the field of antibiotic-free cultivation. It is believed that the continuous popularization of product-based nano-emulsification technology will surely bring revolutionary changes to the veterinary drug industry in the near future.
refer to
Wu, Ouyang Wuqing, Zhu, et al. Preparation of Baicalin Nanoemulsion [J]. Fine Chemical Industry, 2007(5):470-472.
[2] Liu Yue, Cao Dandan. Application of Nanoemulsion in Veterinary Pharmacy [J]. Animal Husbandry and Veterinary Science and Technology Information, 2018 (10):155.
Hu Hongwei, Li Jianyong, Wu Peixing, et al. Research progress of nanoemulsion and its application in pharmacy [J]. Hubei Agricultural Science, 2009,48 (3): 747-750.
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