Laurocapram

Transdermal permeation of drugs with differing lipophilicity: Effect of penetration enhancer camphor.[Pubmed:27154251]

Int J Pharm. 2016 Jun 30;507(1-2):90-101.

The aim of the present study was to investigate the potential application of (+)-camphor as a penetration enhancer for the transdermal delivery of drugs with differing lipophilicity. The skin irritation of camphor was evaluated by in vitro cytotoxicity assays and in vivo transdermal water loss (TEWL) measurements. A series of model drugs with a wide span of lipophilicity (logP value ranging from 3.80 to -0.95), namely indometacin, lidocaine, aspirin, antipyrine, tegafur and 5-fluorouracil, were tested using in vitro transdermal permeation experiments to assess the penetration-enhancing profile of camphor. Meanwhile, the in vivo skin microdialysis was carried out to further investigate the enhancing effect of camphor on the lipophilic and hydrophilic model drugs (i.e. lidocaine and tegafur). SC (stratum corneum)/vehicle partition coefficient and Fourier transform infrared spectroscopy (FTIR) were performed to probe the regulation action of camphor in the skin permeability barrier. It was found that camphor produced a relatively low skin irritation, compared with the frequently-used and standard penetration enhancer Laurocapram. In vitro skin permeation studies showed that camphor could significantly facilitate the transdermal absorption of model drugs with differing lipophilicity, and the penetration-enhancing activities were in a parabola curve going downwards with the drug logP values, which displayed the optimal penetration-enhancing efficiency for the weak lipophilic or hydrophilic drugs (an estimated logP value of 0). In vivo skin microdialysis showed that camphor had a similar penetration behavior on transdermal absorption of model drugs. Meanwhile, the partition of lipophilic drugs into SC was increased after treatment with camphor, and camphor also produced a shift of CH2 vibration of SC lipid to higher wavenumbers and decreased the peak area of the CH2 vibration, probably resulting in the alteration of the skin permeability barrier. This suggests that camphor might be a safe and effective penetration enhancer for transdermal drug delivery.

Transdermal delivery of dimethyl fumarate for Alzheimer's disease: Effect of penetration enhancers.[Pubmed:28709939]

Int J Pharm. 2017 Aug 30;529(1-2):465-473.

Dimethyl fumarate (DMF) is an orally administered drug with neuroprotective and immunomodulatory activities. It has potential uses in the treatment of neurodegenerative diseases such as Alzheimer's disease (AD). The objective of this study was to investigate the feasibility of transdermal delivery of DMF by studying the effect of different penetration enhancers on the skin permeation of DMF. The permeation of saturated DMF solutions was investigated in propylene glycol (PG) with varying concentrations of each of the following enhancers: Polysorbate 80 (T80), N-methyl pyrrolidone (NMP), Laurocapram (Azone((R))) (Az), Transcutol P (Tc), Terpineol (Terp), and cineole (Cin) using vertical Franz diffusion cells and human cadaver skin. The results showed that all penetration enhancers improved the rate of permeation of DMF. The rank order for the highest concentration of each enhancer was as follows: Cin > Az>TC > Terp>T80>/=NMP. The most effective penetration enhancer was shown to be 5% cineole with a 5.3-fold increase in the enhancement ratio (ER). The amounts of drug delivered suggest that DMF is a potential candidate for transdermal drug delivery.

Laurocapram is a absorption enhancer and has been one of the most effective for substances of both lipophilic and hydrophilic nature.

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