Chou Tzung-Han, Nugroho Daniel Setiyo, Chang Jia-Yaw, Cheng Yu-Shen, Liang Chia-Hua, Deng Ming-Jay
Department of Chemical and Materials Engineering, National Yunlin University of Science and Technology, Yunlin 64022, Taiwan.
Department of Chemical Engineering, National Taiwan University of Science and Technology, Taipei 10607, Taiwan.
Polymers (Basel). 2021 Mar 25;13(7):1016. doi: 10.3390/polym13071016.
Apigenin (Apig) is used as a model drug due to its many beneficial bio-activities and therapeutic potentials. Nevertheless, its poor water solubility and low storage stability have limited its application feasibility on the pharmaceutical field. To address this issue, this study developed nanoemulsions (NEs) using an anti-oxidative polymeric amphiphile, d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), hydrogenated soy lecithin (HL), black soldier fly larvae (BSFL) oil, and avocado (AV) oil through pre-homogenization and ultrasonication method. Addition of TPGS (weight ratios 100 and 50% as compared to HL) into NEs effectively reduced particle size and phase transition region area of NEs with pure HL. Incorporation of Apig into NEs made particle size increase and provided a disorder effect on intraparticle molecular packing. Nevertheless, the encapsulation efficiency of NEs for Apig approached to about 99%. The chemical stability of Apig was significantly improved and its antioxidant ability was elevated by incorporation with BSFL oil and AV oil NEs, especially for NEs with single TPGS. NEs with single TPGS also exhibited the best Apig skin deposition. For future application of topical Apig delivery, NEs-gel was formed by the addition of hyaluronic acid (HA) into NEs. Their rheological characteristics were dominated by the surfactant ratios of HL to TPGS.
芹菜素(Apig)因其具有多种有益的生物活性和治疗潜力而被用作模型药物。然而,其较差的水溶性和较低的储存稳定性限制了其在制药领域的应用可行性。为了解决这个问题,本研究通过预均质化和超声处理方法,使用抗氧化聚合物两亲物d-α-生育酚聚乙二醇1000琥珀酸酯(TPGS)、氢化大豆卵磷脂(HL)、黑水虻幼虫(BSFL)油和鳄梨(AV)油制备了纳米乳液(NEs)。在NEs中加入TPGS(与HL相比重量比为100%和50%)有效地降低了纯HL的NEs的粒径和相转变区域面积。将Apig掺入NEs中使粒径增加,并对颗粒内部分子堆积产生无序效应。然而,NEs对Apig的包封率接近99%。通过与BSFL油和AV油NEs结合,Apig的化学稳定性显著提高,其抗氧化能力增强,特别是对于含有单一TPGS的NEs。含有单一TPGS的NEs也表现出最佳的Apig皮肤沉积。为了未来局部递送Apig的应用,通过向NEs中添加透明质酸(HA)形成了NEs-凝胶。它们的流变学特性主要由HL与TPGS的表面活性剂比例决定。