中草药2026，Vol.57Issue(6)：2098-2108,11.DOI:10.7501/j.issn.0253-2670.2026.06.009
柚皮素胶束温敏凝胶的制备、质量评价及药效学研究
Preparation,quality evaluation and pharmacodynamic study of naringenin micellar thermosensitive gel
摘要
Abstract
Objective To prepare naringenin micelles-loaded thermosensitive gel(NMTG),evaluate its biological safety and anti-inflammatory activity,and investigate its therapeutic effects on dry eye disease(DED)induced by benzalkonium chloride(BAC)in rats.Methods Naringenin micelles(NM)were prepared by the thin-film dispersion method.Quality evaluations of the prepared NM included appearance,particle size,ζ potential,transmission electron microscopy,encapsulation efficiency,drug loading and stability.Concentrations of Poloxamer 188(P188)and Poloxamer 407(P407)were optimized based on the phase transition temperatures(Tgel and Tatd gel)of NMTG before and after dilution with tear fluid.Optimal concentrations of P188 and P407 were dissolved in NM to form NMTG.Biological safety,anti-inflammatory activity,and therapeutic effects on BAC-induced DED rats were investigated.Results Prepared NM was clear and transparent.Transmission electron microscopy showed near-spherical particles with an average particle size of(21.56±0.16)nm,a polydispersity index(PDI)value of 0.053±0.033,and a ζ potential of(-18.63±1.94)mV.Encapsulation efficiency and drug loading were(73.96±0.24)%and(7.34±0.38)%,respectively,and the stability was good within 14 d.The optimal NMTG was achieved with concentrations of 5.29%P188 and 16.24%P407.NMTG demonstrated good biological safety and anti-inflammatory activity.Pharmacological experiments indicated that NMTG showed favorable therapeutic effects on DED rats.Conclusion The successful preparation of NMTG improve the solubility of naringenin,which endow it with good DED therapeutic effects.This will provide support for new indications of naringenin in ocular applications and offer candidate solutions for the development of new naringenin dosage forms.关键词
柚皮素/胶束/温敏凝胶/干眼症/薄膜分散法/星点设计-效应面法/药效学/生物安全性/抗炎活性Key words
naringenin/micelles/thermosensitive gel/dry eye disease/thin-film dispersion method/star-point design-response surface method/pharmacodynamics/biological safety/anti-inflammatory activity分类
医药卫生引用本文复制引用
罗倩菲,崔腾,王慧云,马若馨,孙文进,刘庭宇,张浩琛,靳茗扬,周俊芳,王建辉,刘树玲..柚皮素胶束温敏凝胶的制备、质量评价及药效学研究[J].中草药,2026,57(6):2098-2108,11.基金项目
山东省自然科学基金项目(ZR2019BH070) （ZR2019BH070）
济宁医学院大学生创新创业训练计划项目重点项目(cx2024018z) （cx2024018z）
