摘要
目的 制备包载异戊酰紫草素的脂质体制剂,对其制备工艺进行优化,并研究其理化性质,为后期药理学研究提供基础。方法 采用薄膜分散法制备异戊酰紫草素脂质体(IsoSHK-lip),对异戊酰紫草素进行精密度、稳定性、回收率的考察并绘制标准曲线,采用响应面优化法,以卵磷脂-胆固醇质量比(A):卵磷脂-异戊酰紫草素质量比以及(B):水和介质体积(C)为三个因素,进行三因素三水平的制备方案优化,并对最优方案制得的IsoSHK-lip进行粒径、多分散系数(PDI)、Zeta电位、形态表征以及稳定性考察。结果 响应面优化预测IsoSHK-lip最优制备条件为:卵磷脂-胆固醇质量比为8.82∶1,卵磷脂-异戊酰紫草素质量比为30.65∶1,水和介质体积为29.22 mL。重复制备最优结果的IsoSHK-lip得到平均包封率为90.03%,粒径均值为117.48 nm, PDI均值为0.246,Zeta电位均值为-13.59 mV。并且稳定性实验表明,4℃放置7 d, IsoSHK-lip粒径、PDI、Zeta电位没有明显变化。透射电镜结果表明脂质体为近球形,粒径在100~200 nm之间。结论 IsoSHK-lip采用响应面法优化得到的最优结果重复制备3次后,得到了近球形、粒径较小、粒径分布均匀、稳定性较好的IsoSHK-lip,为后续的药理学研究提供了剂型研究基础。
OBJECTIVE To prepare liposome formulations encapsulating isovaleryl shikonin,to optimise the preparation process.METHODS The isovalerylshikonin-liposome(IsoSHK-lip)were prepared by the thin film dispersion method.The UV absorption,standard curve,precision,stability and recovery of IsoSHK-lip were investigated.A response surface optimization method was used to optimize a 3-factor,3-level preparation scheme with A:lecithin-cholesterol mass ratio,B:lecithin-isovalerylshikonin mass ratio and C:volume of hydrated solvent as the three factors.The particle size,polymer dispersity index(PDI),Zeta potential,morphological characterisation and stability of IsoSHK-lip were also investigated for the optimal solution.RESULTS The response surface optimization predicted that the optimal preparation conditions for IsoSHK-lip were:lecithin-cholesterol mass ratio of 8.82∶1,lecithin-isovalerylshikonin mass ratio of 30.65∶1,and volume of hydrated solvent of 29.22 mL.Repeated preparation of the optimal IsoSHK-lip resulted in an average encapsulation rate of 90.03%,a mean particle size of 117.48 nm,a mean PDI of 0.246,and a mean Zeta potential of-13.59 mV.The stability experiments showed that the particle size,PDI and Zeta potential of IsoSHK-lip did not change significantly after 7 d at 4℃.Transmission electron microscopy showed that the IsoSHK-lip was subspherical with particle sizes in the range of 100-200 nm.CONCLUSION IsoSHK-lip is prepared by repeating the optimal results obtained by response surface methodology three times,resulting in a near spherical shape,smaller particle size,uniform particle size distribution and better stability of IsoSHK-lip,which provides the basis for subsequent pharmacological studies of dosage forms.
作者
陈卫军
秦冬梅
孟凌宇
高月锋
CHEN Weijun;QIN Dongmei;MENG Lingyu;GAO Yuefeng(MOE Key Laboratory of Xinjiang Phytomedicine Resource and Utilization,School of Pharmacy,Shihezi University,Shihezi 832002,China;School of Traditional Chinese Medicine,Xinjiang Second Medical Collage,Karamay 834000,China;Department of Pharmacy,The Seventh Affiliated Hospital of Xinjiang Medical University,Urumuqi 830028,China;College of Applied Engineering,Henan University of Science and Technology,Sanmenxia 472000,China)
出处
《中国药学杂志》
CAS
CSCD
北大核心
2024年第19期1843-1852,共10页
Chinese Pharmaceutical Journal
基金
国家自然科学基金项目资助(81860730)。
关键词
异戊酰紫草素
脂质体
薄膜分散法
响应面优化法
包封率
isovalerylshikonin
liposome
thin film dispersion
response surface optimization
encapsulation efficiency
作者简介
陈卫军,男,硕士,副主任药师研究方向:中药民族药对代谢性疾病机制及新药研究;通信作者:秦冬梅,女,博士,教授研究方向:中药民族药分离及其药效作用机制研究。
