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波棱瓜子新型自组装纳米粒的构建及评价

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中药在煎煮过程中化学成分会发生分子识别形成自组装纳米粒(self-assembled nanoparticles,SAN)业已成为行业共识。煎煮液中难溶性成分多以纳米颗粒的形式存在,在一定程度上改善低溶解度的问题,但难溶性成分在煎煮液中的转移率依旧很低,限制了药效的发挥。本研究对传统中药煎煮自组装现象进行改良,将波棱瓜子的水煎液和醇提液以微沉淀的方式构建自组装纳米粒(micro-precipitation self-assembled nanoparticles,MP-SAN),开展形貌学表征,利用现代光谱和热分析技术检验MP-SAN的形成及其理化性质的变化,用高效液相色谱法研究MP-SAN中木脂素类成分的量值传递规律。MP-SAN呈现类球状结构,形态均匀,粒径为(245。3±3。2)nm,多分散性指数为(0。13±0。03),zeta电位为(-48。9±5。9)mV,稳定系数为(86。05%±2。27%);综合紫外-可见光谱、傅里叶变换红外光谱、差示扫描量热法等技术研究表明,水煎液和醇提液间发生分子识别,在非共价键的作用下发生电子云的重排,所形成的MP-SAN具有更好的热稳定性;经高效液相色谱仪测定,MP-SAN中去氢双松柏醇、波棱内酯A、波棱甲素包封率分别为77。00%、78。57%、94。53%,转移率分别为96。01%、67。86%、65。55%,相较于传统水煎液的转移率分别提高了 1。34、1。38、4。81倍。综上,本研究基于微沉淀法成功构建MP-SAN,实现中药汤剂中难溶性成分的高转移率和高包封率,为中药药效物质基础的高效利用提供了制剂学思路。
Construction and evaluation of novel self-assembled nanoparticles of Herpetospermum caudigerum Wall.
It has become an industry consensus that self-assembled nanoparticles(SAN)are formed by molecular recognition of chemical components in traditional Chinese medicine during the decoction process.The insoluble components in the decoction are mostly in the form of nanoparticles,which can improve the problem of poor water solubility.However,the transfer rate of these insoluble components in the decoction is still very low,which limits the efficacy of the drug.This study aimed to refine the traditional decoction self-assembly phenomenon.The self-assembled nanoparticles were constructed by micro-precipitation method(MP-SAN),and characterized by particle size,zeta potential,stability index and morphology.The formation of MP-SAN and alterations in related physicochemical properties were evaluated using modern spectroscopic and thermal analysis techniques.The quality value transmitting pattern of lignan components within the MP-SAN was assessed via high performance liquid chromatography(HPLC).The MP-SAN showed sphere-like structure with uniform morphology,particle size of(245.3±3.2)nm,polydispersity index(PDI)of(0.13±0.03),zeta potential of(-48.9±5.9)mV and stability index(SI)of(86.05%±2.27%).Comprehensive analyses using ultraviolet visible spectroscopy,Fourier transform infrared spectroscopy,differential scanning calorimetry,and other techniques confirmed molecular recognition between the decoction and ethanol extraction,leading to electron rearrangement under the influence of non-covalent bonding.This resulted in the formation of nanoparticles possessing superior thermal stability.As determined by HPLC,the encapsulation rates of the index components in the MP-SAN were all greater than 75%(dehydrodico-niferyl alcohol:77.00%;herpetolide A:78.57%;herpetrione:94.53%),and the transfer rates were all higher than 65%(dehydrodiconiferyl alcohol:96.01%;herpetolide A:67.86%;herpetrione:65.55%),which were 1.34,1.38 and 4.81 times compared with those of the traditional decoction.In summary,this study successfully constructed the MP-SAN based on micro-precipitation method to achieve high transfer rate and high encapsulation rate of insoluble components in docoction,which provides a pharmaceutics idea for the efficient utilization of pharmacodynamic substance basis of traditional Chinese medicine.

Herpetospermum caudigerum Wall.micro-precipitation methodself-assembleddecoctionnanoparticle

朱煜文、邓翔、陈莉、宁建涛、薛玉叶、申宝德、杭凌宇、袁海龙

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空军军医大学,空军特色医学中心药学部,北京 100142

江西中医药大学现代中药制剂教育部重点实验室,江西南昌 330004

波棱瓜子 微沉淀法 自组装 汤剂 纳米粒

国家自然科学基金面上项目国家自然科学基金面上项目

8217407481873092

2024

药学学报
中国药学会 中国医学科学院药物研究所

药学学报

CSTPCD北大核心
影响因子:1.274
ISSN:0513-4870
年,卷(期):2024.59(2)
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