Khumpirapang Nattakanwadee, Klayraung Srikanjana, Tima Singkome, Okonogi Siriporn
Department of Pharmaceutical Chemistry and Pharmacognosy, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok 65000, Thailand.
Program in Biotechnology, Faculty of Science, Maejo University, Chiang Mai 50290, Thailand.
Pharmaceutics. 2021 Feb 15;13(2):265. doi: 10.3390/pharmaceutics13020265.
The aim of the present study was to develop a microemulsion (ME) containing oil (AGO), 1,8-cineole (C), or methyl eugenol (M) as an active pharmaceutical ingredient (API) for enhancing their antimicrobial activities. Agar diffusion, broth microdilution, and killing kinetics were used for antimicrobial evaluations. The ME composed of 30% API, 33.4% Tween 80, 16.6% ethanol, and 20% water appeared as translucent systems with droplet size and polydispersity index of 101.1 ± 1.3 nm and 0.3 ± 0.1, 80.9 ± 1.1 nm and 0.4 ± 0.1, and 96.6 ± 2.0 nm and 0.2 ± 0.1 for ME-AGO, ME-C, and ME-M, respectively. These ME formulations showed minimum bacterial concentrations of 3.91-31.25 µg/mL and 50% fungal inhibition concentrations of 1.83 ± 0.27-0.46 ± 0.13 µg/mL, 2-4 times stronger, and faster kinetic killing rate than their respective API alone. Keeping the ME formulations at 4 °C, 25 °C, and 40 °C for 12 weeks did not affect their activities against fungi and Gram-negative bacteria, but the high temperature of 40 °C decreased their activities against Gram-positive bacteria. It is concluded that ME is a promising delivery system for AGO and its major compounds to enhance their water miscibility and antimicrobial activities.
本研究的目的是开发一种含有莪术油（AGO）、1,8-桉叶素（C）或甲基丁香酚（M）作为活性药物成分（API）的微乳剂（ME），以增强其抗菌活性。采用琼脂扩散法、肉汤微量稀释法和杀菌动力学法进行抗菌评估。由30% API、33.4%吐温80、16.6%乙醇和20%水组成的ME，对于ME-AGO、ME-C和ME-M，分别呈现为半透明体系，液滴尺寸和多分散指数为101.1±1.3 nm和0.3±0.1、80.9±1.1 nm和0.4±0.1、96.6±2.0 nm和0.2±0.1。这些ME制剂的最低细菌浓度为3.91-31.25 µg/mL，50%真菌抑制浓度为1.83±\u200b0.27-0.46±0.13 µg/mL，比各自单独的API抗菌活性强2-4倍，且杀菌动力学速率更快。将ME制剂分别在4℃、25℃和40℃下保存12周，对其抗真菌和革兰氏阴性菌活性没有影响，但40℃的高温会降低其对革兰氏阳性菌的活性。得出的结论是，ME是一种有前景的AGO及其主要化合物递送系统，可增强其与水的混溶性和抗菌活性。
