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功能化脂质体及其在植物源天然产物递送中的应用

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植物源天然产物具有广泛的药理特性,在药物发现中占据关键地位,同时以植物膳食补充剂的形式满足人体营养需求。植物源天然产物功效强大,但普遍存在溶解性低、稳定性差、缺乏靶向性、有毒副作用、有特殊气味等限制因素,为临床药物转化带来了挑战。近年来,纳米技术的发展为植物源天然产物的应用提供了新途径。其中,脂质体是一种由两亲性物质合成的双分子层纳米囊泡,具有高载药量、稳定性强等优势。与其他纳米颗粒相比,脂质体易于制备和扩展,它的扩展基于脂质体能被灵活修饰的表面特性。通过在脂质体表面修饰具备不同功能的元件可以使脂质体功能化,这些功能体现在靶向递送、药物控释、局部释放、改善药代动力学等。使用不同类型的功能化脂质体负载植物源天然产物不仅可以增强天然产物的稳定性、提高靶向性、减少副作用,还可以掩盖天然产物的刺激性气味,提升大众的接受度。本综述围绕当前植物源天然产物面临的典型问题,结合功能化脂质体在其中的具体应用做出总结。此外,本文还将回顾功能化脂质体进入临床治疗所面临的机遇和挑战,并探讨克服这些问题的机会,以期更好地实现植物纳米药物的精准控制,为相关领域研究人员及相关产业工作人员提供思路与启发。
Application of Functionalized Liposomes in The Delivery of Natural Products
Plant natural products have a wide range of pharmacological properties,not only can they be used as plant dietary supplements to meet the nutritional needs of the human body in the accelerated pace of life,but also occupy an important position in the research and development of therapeutic drugs for the treatment of tumors,inflammation and other diseases,and have been widely accepted by the public due to their good safety.However,despite the above advantages of plant natural products,limiting factors such as low solubility,poor stability,lack of targeting,high toxicity and side effects,and unacceptable odor have greatly impeded their conversion to clinical applications.Therefore,the development of new avenues for the application of new natural products has become an urgent problem to be solved at present.In recent years,with the continuous development of research,various strategies have been developed to improve the bioavailability of natural products.Among them,nanocarrier delivery system is one of the most attractive strategies at present.In past studies,a large number of nanomaterials(organic,inorganic,etc.)have been developed to encapsulate plant-derived natural products for their efficient delivery to specific organs and cells.Up to now,nanotechnology has not only been limited to pharmaceutical applications,but is also competing in the fields of nanofood processing technology and nanoemulsions.Among the various nanocarriers,liposomes are the largest nanocarriers with the largest market share at present.Liposomes are bilayer nanovesicles synthesized from amphiphilic substances,which have advantages such as high drug loading capacity and stability.Attractively,the flexible surface of liposomes can be modified with various functional elements.Functionalized modification of liposomes with different functional elements such as antibodies,nucleic acids,peptides,and stimuli-responsive moieties can bring out the excellent drug delivery function of liposomes to a greater extent.For example,the modification of functional elements with targeting function such as nucleic acids and antibodies on the surface of liposomes can deliver natural products to the target location and improve the bioavailability of drugs;the modification of stimulus-responsive groups such as photosensitizers,magnetic nanoparticles,pH-responsive groups,and temperature sensitizers on the surface of liposomes can achieve controlled release of drugs,localized targeting,and synergistic thermotherapy.In addition to the above properties,by using functionalized liposomes to encapsulate natural products with irritating properties can also effectively mask the irritating properties of natural products,improve public acceptance,and increase the possibility of application of irritating natural products.There are various strategies for modifying liposomes with functional elements,and the properties of functionalized liposomes constructed by different construction strategies differ.The commonly used construction strategies for functionalized liposomes include covalent modification and non-covalent modification.These two types of construction strategies have their own advantages and disadvantages.Covalent modification has better stability than non-covalent modification,but its operation is cumbersome.With the above background,this review focuses on the three typical problems faced by plant natural products at present,and summarizes the specific applications of functionalized liposomes in them.In addition,this paper summarizes the construction strategies for building different types of functionalized liposomes.Finally,this paper will also review the opportunities and challenges faced by functionalized liposomes to enter clinical therapy,and explore the opportunities to overcome these problems,with a view to better realizing the precise control of plant nanomedicines,and providing ideas and inspirations for researchers in related fields as well as relevant industrial staff.

natural productfunctionalized liposomesstimulus responsetargetlong cycle

王程蕴、兰欣悦、顾家璇、高欣茹、朱龙佼、李军、方冰、许文涛、田洪涛

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河北农业大学食品科技学院,保定 071000

中国农业大学营养与健康系,食品精准营养与质量控制教育部重点实验室,北京 100191

中国农业大学食品科学与营养工程学院,北京 100083

河北科技师范学院食品科技学院暨葡萄酒学院,秦皇岛 066004

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天然产物 功能化脂质体 刺激响应 靶向 长循环

2024

生物化学与生物物理进展
中国科学院生物物理研究所,中国生物物理学会

生物化学与生物物理进展

CSTPCD北大核心
影响因子:0.476
ISSN:1000-3282
年,卷(期):2024.51(11)