Caballero-Román Aitor, Nardi-Ricart Anna, Vila Roser, Cañigueral Salvador, Ticó Josep R, Miñarro Montserrat
Departament de Farmàcia i Tecnologia Farmacèutica, i Fisicoquímica, Facultat de Farmàcia i Ciències de l'Alimentació, Universitat de Barcelona (UB), Avinguda Joan XXIII, 27-31, 08028 Barcelona, Spain.
Unitat de Farmacologia, Farmacognòsia i Terapèutica, Facultat de Farmàcia i Ciències de l'Alimentació, Universitat de Barcelona (UB), Avinguda Joan XXIII, 27-31, 08028 Barcelona, Spain.
Pharmaceutics. 2024 Sep 26;16(10):1251. doi: 10.3390/pharmaceutics16101251.
Eugenol is a colourless or yellowish compound whose presence in clove essential oil surpasses the 75% of its composition. This phenylpropanoid, widely used as an antiseptic, anaesthetic and antioxidant, can be extracted by steam distillation from the dried flower buds of (L.). Due to its chemical instability in presence of light and air, it should be protected when developing a formulation to avoid or minimise its degradation. A promising approach would be encapsulation by spray drying, using natural coating products such as maltodextrin, gum arabic, and soy lecithin. To do so, a factorial design was carried out to evaluate the effect of five variables at two levels (inlet temperature, aspirator and flow rate, method of homogenisation of the emulsion and its eugenol:polymers ratio). Studied outcomes were yield and outlet temperature of the spray drying process, eugenol encapsulation efficiency, and particle size expressed as d. The best three formulations were prepared by using a lower amount of eugenol than polymers (1:2 ratio), homogenised by Ultra-Turrax, and pumped to the spray dryer at 35 m/h. Inlet temperature and flow rate varied in the top three formulations, but their values in the best formulation (DF22) were 130 °C and 4.5 mL/min. These microcapsules encapsulated between 47.37% and 65.69% of eugenol and were spray-dried achieving more than a 57.20% of product recovery. Their size, ranged from 22.40 μm to 55.60 μm. Overall, the whole spray drying process was optimised, and biodegradable stable polymeric microcapsules containing eugenol were successfully prepared.
丁香酚是一种无色或淡黄色化合物,其在丁香精油中的含量超过其成分的75%。这种苯丙烷类化合物广泛用作防腐剂、麻醉剂和抗氧化剂,可通过水蒸气蒸馏从丁香(L.)的干燥花蕾中提取。由于其在光和空气存在下化学性质不稳定,在开发制剂时应加以保护,以避免或尽量减少其降解。一种有前景的方法是通过喷雾干燥进行包封,使用麦芽糊精、阿拉伯胶和大豆卵磷脂等天然包衣产品。为此,进行了析因设计,以评估两个水平的五个变量(进口温度、吸气器和流速、乳液均质化方法及其丁香酚与聚合物的比例)的影响。研究结果包括喷雾干燥过程的产率和出口温度、丁香酚包封效率以及以d表示的粒径。最佳的三种制剂是使用比聚合物含量低的丁香酚(1:2比例)制备的,通过Ultra-Turrax均质化,并以35 m/h的速度泵入喷雾干燥器。进口温度和流速在最佳的三种制剂中有所不同,但最佳制剂(DF22)中的值分别为130℃和4.5 mL/min。这些微胶囊包封了47.37%至65.69%的丁香酚,并通过喷雾干燥实现了超过57.20%的产品回收率。它们的尺寸范围为22.40μm至55.60μm。总体而言,整个喷雾干燥过程得到了优化,并成功制备了含有丁香酚的可生物降解稳定聚合物微胶囊。