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

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

Author information

1
a Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, October University for Modern Sciences and Arts (MSA) , Cairo , Egypt.
2
b Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Helwan University, Ain Helwan , Cairo , Egypt.
3
c Department of Pharmaceutics and Industrial Pharmacy , Faculty of Pharmacy, Cairo University , Cairo , Egypt.
4
d National Organization for Drug Control and Research , Cairo , Egypt.

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/CoSmix) 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 (Jss = 3.164 µg/cm2/h), enhancement ratio (Er = 8.32), and permeability coefficient (Kp = 22.14 × 10-4 cm2/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.

KEYWORDS:

Coenzyme Q10; anti-wrinkle; nanoemulsion; permeability; phase diagram

PMID:
29096550
DOI:
10.1080/03639045.2017.1391836
[Indexed for MEDLINE]

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