Abstract
Objective: The object of our investigation was to develop and characterize nanoemulsion gel (NEG) as transdermal delivery systems for the poorly water soluble drug, Co-enzyme Q10 (CoQ10), to improve its solubility and skin permeability and thus improving its anti-wrinkle efficiency.Methods: An optimized nanoemulsion (NE) formula was chosen according to its particle size and stability and converted into nanoemulsion gel using different gelling agents, including; carbopol 934 (1%), xanthan gum (2%) and sodium carboxymethyl cellulose(NaCMC) (2%). Drug loaded nanoemulsion gels were characterized for particle size, zeta potential, viscosity and rheological behavior, conductivity, spreadability, drug content and permeation studies using Franz diffusion cell.Results: NEG containing 10% w/v isopropyl myristate (IPM) as oil, 60% w/v tween 80 and transcutol HP as surfactant/co-surfactant mixture (S/CoS), 30%w/v water, 2%w/v drug, and 1% w/v carbopol 934 as gelling gent was concluded as an optimized NEG formula. It exhibited pH, viscosity, drug content, particle size, zeta potential, polydispersity index(PDI) and spreadability, as 5.4±0.011, 27588±2034.34 cps,101.51±0.93%,120.5±1.19 nm,-29.8±1.46, 0.273 and 6.16±0.28 cm, respectively. Also, it showed significantly higher cumulative amount of drug permeated through dialysis membrane (281.71±0.97μg/cm2) and through rat skin (20.73±2.5 μg/cm2) than the other formulae and marketed formulation (P<0.001). In addition, its permeability parameters like drug flux (Jss), enhancement ratio (Er) and permeability coefficient (Kp) exhibited the highest values; 12.79µg/cm2/h, 95.92×10-4 cm2/h and 57.35, respectively for in vitro permeation study and 0.968µg/cm2/h, 7.26×10-4 cm2/h and 1.183, respectively for ex-vivo permeation study.Further histopathological evaluation test showed that CoQ10 NEG has a good anti-wrinkle efficacy compared to the conventional topical dosage form.Conclusion: These results judged NEG to be a promising alternative carrier for topical delivery of CoQ10 to enhance its solubility, skin permeability and thus anti-wrinkle efficiency.
Highlights
Topical delivery systems (TDSs) are self-contained discrete systems applied to the intact skin to deliver drugs at a controlled or sustainable rate [1]
In the surfactant/co-surfactant mixture (S/CoS) screening test, it was found that the system containing span 20 exhibited bad NE or gave NE with a high concentration of S/CoS (>60%) that made the risk of skin irritation, so it was excluded
This formula is composed of 10% w/v isopropyl myristate (IPM) as oil, 60% w/v tween 80 and transcutol HP as surfactant/co-surfactant mixture, 30% w/v water, 2% w/v drug
Summary
Topical delivery systems (TDSs) are self-contained discrete systems applied to the intact skin to deliver drugs at a controlled or sustainable rate [1]. Conventional topical dosage forms such as cream, ointments, and pastes have the disadvantage of being sticky for applying to the skin and having a low permeability for the drug For this reason, transparent gels are widely used in cosmetics and pharmaceutical preparations. Its vast network structure allows better drug loading capacity compared to other novel approaches like niosomes and liposomes avoiding the drug leakage and lesser entrapment efficiency They possess various advantages over emulsions and microemulsions, such as higher surface area (due to the smaller droplet size of the NE), higher skin permeation, higher retention potential and improved physical stability [5,6,7,8,9]. These NEG formulae were prepared using three types of hydrophilic polymers namely; xanthan gum, carbopol 934 and sodium carboxymethylcellulose (NaCMC)
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