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In order to improve the physicochemical properties of puerarin and enhance its water solubility, membrane permeability and bioavailability, puerarin nanoparticles were prepared by subcritical water-anti-solvent method, and characterized by SEM, DSC, and FTIR. The effect of different factors for preparation of puerarin nanoparticles on the particle size and polydispersity index (PDI) of puerarin nanoparticles were evaluated via nanoparticle size and Zeta potential analyzer. The in vitro and in vivo properties of puerarin nanoparticles were analyzed through in vitro release and transdermal experiments. The results showed that under the optimal process conditions of liquid-material ratio (mL∶g) 220∶1, subcritical water temperature 125 ℃, extraction time 20 min, volume ratio of subcritical water to anti-solvent (ultrapure water containing stabilizer) 1∶1, and lactose with a mass fraction of 0.08% as stabilizer, the prepared puerarin nanoparticles exhibited an average particle size of 89.94 nm, a yield of 94.01%. The puerarin nanoparticles gel had a cumulative release rate of 90.0% within 12 h and up to 96.7% within 48 h with the release process conforming to the first-order release model, and a cumulative permeability of 1323.64 μg/cm² at 12 h. Its pharmacokinetic parameters were improved compared with those of puerarin, with the half-life prolonged and the peak mass fraction decreased.

, authors=Mengyu SUN¹, Bei LIU¹, Wenying ZHAO¹, Yu ZHANG¹, Qingshu ZHU^{2, *}, authorsList=Mengyu SUN, Bei LIU, Wenying ZHAO, Yu ZHANG, Qingshu ZHU, authorCompany=null, correspAuthors=Qingshu ZHU, authorNote=null, correspAuthorsNote=null, copyrightStatement=null, copyrightOwner=null, extLink=null, articleAbsUrl=null, sourceXml=null, magXml=null, pdfUrl=null, pdf=null, pdfFileSize=null, pdfExtLink=null, richHtmlUrl=null, mobilePdfUrl=null, reviewReport=null, pdfFirstPage=null, abstractGraph=null, abstractGraphContent=null, abstractVideo=null, citation=null, cebUrl=null, magXmlContent=null, mapNumber=null, fund=null), CN=ArticleExt(id=1297161260966109974, articleId=1297161259170947860, tenantId=1146029695717560320, journalId=1296125381406982186, language=CN, title=葛根素纳米粒的亚临界水-反溶剂制备及体内外性能, columnId=1297161243513615210, journalTitle=精细化工, columnName=医药与日化原料, runingTitle=null, highlight=null, articleAbstract=

为改善葛根素的理化性质，提高其水溶性、膜渗透性和生物利用度，采用亚临界水-反溶剂法制备了葛根素纳米粒。采用SEM、DSC、FTIR对其进行了表征。通过纳米粒度及Zeta电位分析仪考察了不同因素对葛根素纳米粒粒径和多分散指数（PDI）的影响。通过体外释放和透皮实验探究了葛根素纳米粒体内外性能。结果表明，在液料比（mL∶g）220∶1、亚临界水温度125 ℃、提取时间20 min、亚临界水与接收溶剂（含稳定剂的超纯水）体积比为1∶1、稳定剂为质量分数0.08%的乳糖的最佳工艺条件下，制得的葛根素纳米粒平均粒径为89.94 nm，得率为94.01%。葛根素纳米粒凝胶的12 h累积释放率为90.0%，48 h累积释放率升至96.7%，葛根素纳米粒凝胶的释放过程符合一级释放模型。葛根素纳米粒凝胶的12 h累积渗透量为1323.64 μg/cm²，其药代动力学参数比葛根素有所改善，半衰期延长，峰质量分数降低。

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孙梦雨（1999—），女，硕士生，E-mail: 1104664044@qq.com。

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孙梦雨（1999—），女，硕士生，E-mail: 1104664044@qq.com。

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