Abstract
Thymoquinone (TQ) is a quinone-based phytochemical that was first identified in 1963 in Nigella sativa (black cumin seed) by El-Dakhakhany. Based on the ideal characteristics of transdermal delivery, TQ is potentially an attractive candidate for transdermal drug delivery. The aim of this study was to investigate the feasibility of transdermal delivery of TQ and to assess the effect of an ethanol and propylene glycol donor solvent system along with various compositions of receptor solvents. The effects of penetration enhancers on the in vitro skin permeation and TQ skin absorption were studied using human cadaver skin in Franz diffusion cells. The permeation of saturated solutions of TQ was investigated with 5% v/v of each of the following enhancers: Azone (laurocapram), Transcutol® P (Tc), oleic acid, ethanol, Polysorbate 80 (Tween 80), and N-methyl-pyrrolidone (NMP). The results indicated that Azone, oleic acid, and Tc were able to provide adequate TQ flux and may be the agents of choice for use in a novel transdermal formulation of TQ. These penetration enhancers were also able to generate TQ reservoirs in the skin that may be useful to provide sustained release of TQ from the stratum corneum over longer periods of time.
Highlights
IntroductionAlternative routes to oral drug administration such as the transdermal route are becoming even more popular in recent years
There are several advantages associated with transdermal drug delivery systems (TDDS)
The results show that highest TQ solubility can be achieved with ethanol (19 ± 2.6 mg/ml)
Summary
Alternative routes to oral drug administration such as the transdermal route are becoming even more popular in recent years. It was found that approximately 74% of orally administered drugs failed to exert desired pharmacological effectiveness (Marwah et al, 2016). In such cases, transdermal delivery should be considered as an alternative route to oral delivery. There are several advantages associated with transdermal drug delivery systems (TDDS) This delivery system can be very beneficial in avoiding hepatic first-pass effect (Jung et al, 2013) and gastrointestinal environment with its varying pH and a potential site for drug degradation (Singh et al, 2012b). It can provide steady-state plasma levels, improved bioavailability, decreased side effects, and can improve patient compliance (Samad et al, 2009; Marwah et al, 2016).
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