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    Home > Active Ingredient News > Drugs Articles > Research and application status of liposome injection

    Research and application status of liposome injection

    • Last Update: 2021-07-02
    • Source: Internet
    • Author: User
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    The concept of liposome was proposed by Alec Bangham in 1965.
    It is a bilayer structure formed by the assembly of hydrophilic and hydrophobic groups.
    Because of its plastic particle size, good biocompatibility, toxicity and immunogenicity Low advantages, and the ability to load hydrophilic and hydrophobic drugs, as a new type of drug carrier in the pharmaceutical field has received more and more attention in recent years
    .

    In 1990, the world's first nanoliposome injection product AmBisome (Liposome lyophilized powder for amphotericin B injection) developed by NeXstar in the United States was launched on the market, which binds amphotericin B to a lipid bimolecular membrane through electrostatic action on the slow release of amphotericin B, amphotericin B reduce nephrotoxicity of
    .


    Subsequently, liposome products such as doxorubicin liposomes and doxorubicin hydrochloride liposomes have come out one after another, playing an irreplaceable role in anti-tumor, vaccine and other fields


    Research hotspots of liposome injection

    Long-circulating liposomes: Long-circulating liposomes are one of the most widely studied liposomes.
    The surface of the liposomes is mixed with the PEGylated derivative of distearoylphosphatidylethanolamine to make it staggered and overlapped to form a certain The steric hindrance, the high hydrophilicity and flexibility of the derivative will interfere with the hydrophobic interaction between liposomes and plasma proteins, thereby reducing the absorption of liposomes by the reticuloendothelial system and realizing liposomes in vivo Long loop function
    .

    The world's first anti-tumor liposome product Doxil (adriamycin liposome injection), the elimination half-life of free adriamycin is 0.
    2h, AUC is 3.
    81μg·h/mL, and the elimination half-life of Doxil can reach 41~ 70h, AUC is 902µg·h/mL, and clinical studies have shown that it can reduce the release of drugs in the myocardium to reduce the cardiotoxicity of doxorubicin
    .


    The film dispersion and extrusion method was used to prepare voriconazole long-circulating liposomes using polyethylene glycol and distearoyl phosphatidylethanolamine.


    Cationic liposomes: Cationic lipids are generally composed of cationic hydrophilic lipids and neutral lipids.
    Their structure and properties are important factors affecting cytotoxicity and transfection efficiency
    .


    Among them, cationic lipids carry nucleic acids through electrostatic action, and neutral lipids act as auxiliary stabilizers through functionalization


           Alnylam used cationic lipid MC3 to prepare the world's first siRNA drug Onpattro (Patisiran cationic liposome injection) with microfluidic mixing technology, which was approved for marketing in 2018
    .


    In recent years, research on cationic liposomes has mainly focused on the modification of targeting ligands, and the co-delivery of nucleic acids and chemical drugs


           Micro-environment-sensitive liposomes: With the rise of new nano-carrier materials, liposome formulations that release drugs responsively at specific sites are widely used through changes in the microenvironment such as pH and enzymes in the body, or the control of physical conditions such as light and heat effects.
    Research and report
    .

           Celsion’s ThermoDox (adriamycin thermosensitive liposome) is the first thermosensitive liposome preparation that can be used clinically.
    When heated to the phase transition temperature, pore channels will be formed on the lipid bilayer to release more effectively.
    Medicine (for example, 80% of the medicine can be released within 20s at 42°C)
    .


    Based on the difference in pH between tumors and normal tissues, pH-sensitive liposomes can be used for targeted delivery of anti-tumor drugs.


           Liposome injections approved for marketing at home and abroad

           Advantages of liposome injection

           High load and high biocompatibility: About 40% of the global marketed drugs are class II or class IV drugs in the biopharmaceutical classification system, with solubility or permeability defects
    .


    Liposome injections can increase the solubility of the drug and improve the stability of the drug by loading the poorly soluble drug in a lipid nanostructure in a packaged form or by covalently conjugating it with the drug to form a drug-lipid complex, and the lipid structure can be used in the body.


           Efficient targeting: Liposomes can be used for particle size control and functional modification.
    The body organs have different retention capacities for particles of different sizes.
    The particle size control of liposome injections can achieve passive drug targeting effects; at the same time, lipids The lipid surface of the plastid injection can modify membrane proteins, sugars and other ligands that have related receptors in the body, guide the drug-containing lipid nanoparticles to actively target specific sites, and increase the concentration of the drug in the lesion area
    .

           Large-scale production: The preparation technology of liposome injections is simple and easy to implement and easy to scale-up production
    .


    Various methods have been developed for mass production of liposome injections


           As a new type of nano-drug delivery system, liposome injection has the advantages of good targeting and tissue affinity, improving the solubility and penetration of poorly soluble drugs, and improving drug stability
    .


    Liposome injections can overcome the clinical application bottleneck of traditional injections, and can be used in the diagnosis and treatment of major clinical diseases, providing new directions and new ideas for the research and development of complex injections


           references:

           [1] Xiang Xinyan, Du Shuang, Ding Yang, et al.
    Application status and development trend of liposome injections[J].
    Journal of China Pharmaceutical University, 2020, 51(04): 383-393.

           [2] Zhang Xue, Qi Yiguang, Wu Yujie, et al.
    Research and development progress of new injections at home and abroad[J].
    Progress in Pharmaceutical Sciences, 2018, 42(12): 897-904.

           [3] Gao Xie, Ding Yang, Zhou Jianping.
    Research and application prospects of lipid nanoinjections[J].
    Chinese Journal of Pharmaceuticals, 2019, 50(10):1098-1112.

           About the author: Sha Luo, a Chinese medicine researcher and master of Chinese pharmacy, now works in a large domestic drug research and development company, and is committed to the research and development of new Chinese medicines
    .

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