Department of Pharmaceutics, College of Pharmacy, Shaanxi University of Chinese Medicine, Xianyang, Shaanxi 712046, P.R. China.
Shaanxi Province Key Laboratory of New Drugs and Chinese Medicine Foundation Research, College of Pharmacy, Shaanxi University of Chinese Medicine, Xianyang, Shaanxi 712046, P.R. China.
Mol Med Rep. 2020 Dec;22(6):4531-4540. doi: 10.3892/mmr.2020.11571. Epub 2020 Oct 8.
In order to improve the water solubility of the volatile oils extracted from Flos magnoliae (FM) and Centipeda minima (CM), they were prepared as a microemulsion (ME), which were then used in the development of an FM and CM volatile oil ME for the treatment of allergic rhinitis (AR). ME was prepared by phase inversion emulsification, and the prescription factors such as emulsifier, co‑emulsifier, oil phase, Km, which represents the ratio of the mass of emulsifier to that of the co‑emulsifier, and preparation factors such as temperature affecting the formation of the ME were selected according to the formation area of ME in a pseudo‑ternary phase diagram. The quality of the ME was evaluated based on its appearance, particle size, Zeta potential and stability. The content of eucalyptol in ME was determined by gas chromatography‑mass spectrometry (GC‑MS). The cumulative permeability of the ME within 24 h was measured with a transdermal diffusion tester. The results revealed that the best formula for preparation of the ME was as follows: Castor oil polyoxyethylene ether (EL‑40) was the emulsifier; the co‑emulsifier was anhydrous ethanol; the Km was 2:1; the mixed phase of volatile oil and isopropyl myristate with mass ratio of 1:1 was used as oil phase; and the preparation temperature was 25˚C. The content of eucalyptol in the ME was 2.57 mg/g, and the cumulative permeability of the ME in 24 h was significantly increased compared with that of the reference oil solution. The appearance of the ME was uniform, and the solution was transparent. In conclusion, compared with traditional preparations, FM and CM volatile oil ME is a novel, improved and more effective preparation for the treatment of AR.
为了提高从辛夷花和九里香中提取的挥发油的水溶性，将其制成微乳液（ME），并将其用于开发治疗过敏性鼻炎（AR）的辛夷花和九里香挥发油 ME。ME 通过相转变乳化法制备，根据伪三元相图中 ME 的形成区域，选择处方因素，如乳化剂、助乳化剂、油相、Km（代表乳化剂与助乳化剂质量比）以及影响 ME 形成的制备因素，如温度。根据外观、粒径、Zeta 电位和稳定性评价 ME 的质量。通过气相色谱-质谱（GC-MS）法测定 ME 中桉油精的含量。用透皮扩散仪测定 ME 在 24 小时内的累积透过量。结果表明，制备 ME 的最佳配方如下：蓖麻油聚氧乙烯醚（EL-40）为乳化剂；助乳化剂为无水乙醇；Km 为 2:1；混合油相为挥发油和肉豆蔻酸异丙酯，质量比为 1:1；制备温度为 25°C。ME 中桉油精的含量为 2.57mg/g，24 小时内 ME 的累积透过量明显高于对照油溶液。ME 的外观均匀，溶液透明。总之，与传统制剂相比，辛夷花和九里香挥发油 ME 是一种治疗 AR 的新型、改良且更有效的制剂。
