提高伊维菌素水溶性方法的研究进展

doi:10.16431/j.cnki.1671-7236.2023.10.043

摘要/Abstract

摘要： 伊维菌素因其广谱抗寄生虫的作用,被广泛应用于畜禽寄生虫病和人类河盲症的治疗。有研究发现,其还具有抗病毒、抗肿瘤和免疫调节等作用,有很大的开发利用潜能。但伊维菌素因其水溶性差,在临床上的应用受到了很大的限制。近年来制成纳米给药系统、环糊精包合物、固体分散体和自乳化给药系统是提高伊维菌素水溶性的常见方法,并可作为潜在的药物载体。纳米给药系统包括纳米混悬液、微乳液、纳米颗粒和混合胶束,通常需要添加表面活性剂或纳米载体来制备,主要是通过降低药物的粒径来提高其水溶性。环糊精包合物是用环糊精(主体分子)将药物(客体分子)包嵌形成,可提高药物的水溶性和稳定性,降低药物的毒副作用,同时还具有控制药物释放的能力。固体分散体是通过保持药物的非晶态来增加药物的溶解度,但非晶态的药物处于高能状态,有聚集的倾向。自乳化给药系统属于各向同性系统,由油、乳化剂、助乳化剂和药物组成,在体外加水搅拌或者体内水性环境中蠕动的状态下可自发地进行乳化形成乳液。作者就近年来提高伊维菌素水溶性的方法研究展开阐述,以期为伊维菌素制剂的制备工艺和临床开发应用提供理论依据。

关键词: 伊维菌素; 水溶性; 载体; 制剂; 制备工艺

Abstract: Ivermectin is widely used in the treatment of livestock and poultry parasitic diseases and human river blindness because of its broad-spectrum antiparasitic effect.Some studies have found that it also has antiviral,antitumor and immunomodulatory effects,and has great potential for exploitation.However,the clinical application of ivermectin has been greatly restricted due to its poor water solubility.In recent years making nano-delivery systems,cyclodextrin inclusion compounds,solid dispersions and self-emulsifying delivery systems are common methods to improve the water solubility of ivermectin and can be used as potential drug carriers.Nanodelivery systems include nanosuspensions,microemulsions,nanoparticles and hybrid micelles,which usually require the addition of surfactants or nanocarriers to prepare them,mainly by reducing the particle size of the drug to improve its aqueous solubility.Cyclodextrin inclusion compounds are formed by embedding the drug (guest molecule) with cyclodextrin (main molecule),which can improve the water solubility and stability of the drug,reduce the toxic side effects of the drug,and also have the ability to control the drug release.Solid dispersions are used to increase drug solubility by maintaining the amorphous state of the drug,but the amorphous state of the drug is in a high-energy state and has the tendency to aggregate.Self-emulsifying drug delivery systems are isotropic systems,consisting of oil,emulsifier,co-emulsifier and drug,which can spontaneously emulsify to form emulsions in a state of in vitro agitation with water or in vivo peristalsis in an aqueous environment.The authors describe the research on improving the aqueous solubility of ivermectin in recent years,with the aim of providing a theoretical basis for the preparation process and clinical development and application of ivermectin formulations.

Key words: ivermectin; water solubility; carrier; formulation; preparation process

中图分类号:

S859.79^＋5

聂结华, 马艳芝, 张志远, 徐淑凤, 廖洁丹. 提高伊维菌素水溶性方法的研究进展[J]. 中国畜牧兽医, 2023, 50(10): 4292-4300.

NIE Jiehua, MA Yanzhi, ZHANG Zhiyuan, XU Shufeng, LIAO Jiedan. Research Progress on Methods for Improving the Water Solubility of Ivermectin[J]. China Animal Husbandry and Veterinary Medicine, 2023, 50(10): 4292-4300.

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