目的 采用紫苏Perilla frutescens为模型药，制备紫苏精油纳米乳，进行处方工艺研究与初步质量评价。方法 根据紫苏精油在各辅料中的溶解量确定助表面活性剂，采用亲水亲油平衡值（HLB）值法初步筛选适宜水包油型（O/W）纳米乳的表面活性剂，进一步筛选具备用量安全性的表面活性剂，确定纳米乳处方组成。通过绘制伪三元相图，综合比较纳米乳区域大小、载药量、含水量，以及电导率、黏度、粒径及分布、稳定性等优化处方；研究对优化处方工艺的紫苏精油纳米乳的外观质量与形态、相关理化性质（黏度、pH值、电导率、Zeta电位、粒径及分布）、稳定性、体外渗透性以及鼻黏膜刺激性进行考察。结果 优化的紫苏精油纳米乳处方为14.3%紫苏精油-9.5% Transcutol P-19.1% Labrasol-57.1%水；根据优化的处方制备的紫苏精油纳米乳均一、透明、澄清，流动性良好，黏度（3.68±0.17）mPa·s；pH值为6.18±0.03，电导率为（109.61±0.89）μS/cm，Zeta电位为（-7.08±1.82）mV；平均粒径为（49.98±1.55）nm；透射电镜实验结果表明，紫苏精油纳米乳乳滴为球形，粒径大小均在100 nm以内；紫苏精油纳米乳具备离心稳定性、稀释稳定性、长期稳定性以及温度稳定性；于常温未密封的条件下储存1个月与6个月后紫苏精油纳米乳与紫苏精油的平均紫苏醛含量变化百分比分别为1.8%和17.48%；鼻黏膜刺激性实验结果表明，紫苏精油纳米乳给药组与空白生理盐水组无显著差异。结论 研究制备优化处方工艺的紫苏精油纳米乳，其外观形态、相关理化性质符合纳米乳质量要求，具备药物稳定性、药物渗透性以及安全性。

Objective Using Perilla frutescens as a model drug, the nanoemulsion of Perilla frutescens essential oil (PFEO) were prepared, and the formulation process research and preliminary quality evaluation were carried out. Methods The cosurfactants were determined according to the amount of PFEO dissolved in various excipients. The HLB value method was used to preliminarily screen surfactants suitable for oil-in-water (O/W) nanoemulsions, and the surfactants with dosage safety were further screened to determine the composition of nanoemulsion formulations. By drawing a pseudo-ternary phase diagram, the nanoemulsion region size, drug loading, water content, and conductivity, viscosity, particle size, distribution, and stability was comprehensively compared to optimize the prescription. This study investigated the appearance, physicochemical properties (viscosity, pH value, conductivity, electrical conductivity, particle size, Zeta potential), stability, in vitro permeability properties and nasal mucosa irritation of the nanoemulsion of PFEO. Results The final optimized nanoemulsion formulation was 14.3% PFEO-9.5% Transcutol P-19.1% Labrasol-57.1% water. The nanoemulsion of PFEO prepared according to the optimized prescription was uniform, transparent, clear, with good fluidity. The viscosity was (3.68±0.17) mPa·s, pH value was (6.18±0.03), the electrical conductivity was (109.61±0.89) μS/cm, the Zeta potential was (-7.08±1.82) mV, and the particle size was (49.98±1.55) nm. The results of transmission electron microscope experiment showed that, the droplets of PFEO nanoemulsion were spherical with the particle size within 100 nm. The stability test results showed that the nanoemulsion of PFEO had centrifugal stability, dilution stability, long-term stability and temperature stability. After storage at room temperature and unsealed for one month and six months, the percentage change of the average perillaldehyde content of PFEO nanoemulsion and PFEO was 1.8% and 17.48%, respectively. The nasal mucosal irritation test results showed that the PFEO nanoemulsion administration group had no significant difference from the blank saline group. Conclusion The appearance and related physical and chemical properties of PFEO nanoemulsion prepared by optimized prescription process meet the quality requirements of nanoemulsion, with drug stability, drug permeability and safety.

R283.6

江西省科技创新人才重点项目（“5511”工程专项）（20171BCB18001）；中药精油关键技术与中医香疗健康产品研发及产业化项目（20194ABC28009）；江西省一流学科项目（JXSYLXK-ZHYA0091）；江西省一流学科项目（JXSYLXK-ZHYA0092）；江西省大学生创新创业训练计划项目（S202010412062，S202010412052）