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具有改善皮肤渗透性和抗皱效果的营养保健品辅酶Q10纳米乳剂的优化

Optimization of nutraceutical coenzyme Q10 nanoemulsion with improved skin permeability and anti-wrinkle efficiency.

作者信息

El-Leithy Eman S, Makky Amna M, Khattab Abeer M, Hussein Doaa G

机构信息

a Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA) , Cairo , Egypt.

b Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Helwan University, Ain Helwan , Cairo , Egypt.

出版信息

Drug Dev Ind Pharm. 2018 Feb;44(2):316-328. doi: 10.1080/03639045.2017.1391836. Epub 2017 Nov 2.

Abstract

Coenzyme Q10 (CoQ10) is an insoluble, poorly permeable antioxidant with great biological value which acts as anti-aging and anti-wrinkle agent. To improve its permeability through topical application, the current study aimed at formulating oil/water (o/w) nanoemulsion (NE) as an efficient vehicle for delivering (CoQ10) through the skin barriers. The solubility of (CoQ10) was tested for various oils, surfactants (S), and co-surfactants (CoS). The NE region was determined by constructing pseudoternary phase diagrams. NE formulae containing 1, 2, and 3% w/w drug have been subjected to thermodynamic stability test. The formulae that passed thermodynamic stability tests were characterized by physical properties as pH, viscosity, refractive index, droplet size, zeta-potential, TEM, electroconductivity, in vitro release, and ex vivo permeation. The formula 'F2' containing 10% w/w isopropyl myristate (oil phase), 60% w/w of Tween 80: Transcutol HP mixture (S/CoS) at ratio 2:1, 30% w/w water and 2% w/w drug was evaluated for its anti-wrinkle efficiency using an animal model. The 'F2' formula showed 11.76 ± 1.1 nm droplet size, 1.4260 ± 0.0016 refractive index, 0.228 PDI, -14.7 ± 1.23 mv zeta potential, 7.06 ± 0.051 pH, 199.05 ± 0.35 cp viscosity, and the highest percentage of drug release in the selected dissolution media. About 47.21% of the drug was released in phosphate buffer 7.4 containing 5% w/v Labrasol and 5% w/v isopropyl alcohol through 24 h. It also showed the highest drug flux (J = 3.164 µg/cm/h), enhancement ratio (E = 8.32), and permeability coefficient (K = 22.14 × 10 cm/h). CoQ10 NE reduced the skin wrinkles and gave the skin smooth appearance. Our investigation suggests the potential use of NE as a vehicle for enhancing solubility and permeability of CoQ10 and thus improving its anti-wrinkle efficiency.

摘要

辅酶Q10(CoQ10)是一种不溶性、渗透性差但具有重要生物学价值的抗氧化剂,具有抗衰老和抗皱作用。为了通过局部应用提高其渗透性,本研究旨在制备油/水(o/w)纳米乳剂(NE),作为一种通过皮肤屏障递送CoQ10的有效载体。测试了CoQ10在各种油、表面活性剂(S)和助表面活性剂(CoS)中的溶解度。通过构建伪三元相图确定NE区域。对含有1%、2%和3% w/w药物的NE配方进行了热力学稳定性测试。通过pH值、粘度、折射率、液滴大小、zeta电位、透射电子显微镜(TEM)、电导率、体外释放和离体渗透等物理性质对通过热力学稳定性测试的配方进行了表征。使用动物模型评估了含有10% w/w肉豆蔻酸异丙酯(油相)、60% w/w吐温80与二乙二醇单乙基醚混合物(S/CoS)(比例为2:1)、30% w/w水和2% w/w药物的“F2”配方的抗皱效果。“F2”配方的液滴大小为11.76±1.1nm,折射率为1.4260±0.0016,多分散指数(PDI)为0.228,zeta电位为-14.7±1.23mV,pH值为7.06±0.051,粘度为199.05±0.35cp,在选定的溶出介质中药物释放百分比最高。在含有5% w/v Labrasol和5% w/v异丙醇的磷酸盐缓冲液7.4中,约47.21%的药物在24小时内释放。它还显示出最高的药物通量(J = 3.164μg/cm/h)、增强比(E = 8.32)和渗透系数(K = 22.14×10 cm/h)。CoQ10纳米乳剂减少了皮肤皱纹,使皮肤外观光滑。我们的研究表明,纳米乳剂有潜力作为一种载体,提高CoQ10的溶解度和渗透性,从而提高其抗皱效果。

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