New route to enhance drug permeation

Published: 9-Nov-2011

The permeation enhancing features of the NexACT technology has been demonstrated in the delivery of alprostadil (Vitaros), a topical drug recently approved by Health Canada to treat erectile dysfunction. The leading molecule of the NexACT technology, dodecyl-2-N,N-dimethylamino propionate hydrochloride (DDAIP.HCl), has been listed in regulatory filings as a functional non-active excipient. Application of this technology to optimise the pharmacokinetic parameters of a given drug has a tremendous commercial potential in the development of new and improved products with increased bioavailability. The mechanism of action, chemistry, toxicology and safety of these excipients along with typical examples for different routes of administration are reviewed in this paper.

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A permeation enhancing technology developed by Apricus Bioscience and NexMed USA has recently been used in a drug approved by Health Canada. Richard Martin, Bassam Damaj and Dan Frank explain its use in optimising pharmacokinetics


The NexACT technology developed by NexMed consists of proprietary chemical entities that improve solubility and permeation of drugs through tissue and cell membranes resulting in enhanced drug permeation1,2 and/or oral absorption. These permeation enhancers temporarily change the permeation dynamics of the lipid bilayer and loosen the tight junctions between the cells, which enables an increased absorption of drug into the systemic circulation or an increase in local absorption (see Figures 1a & b).


Fig. 1b: Mechanism of enhanced permeation. Real-time confocal microscopy of the DDAPI on uptake of Green Nucleic Acid Stain compared with control

Fig. 1b: Mechanism of enhanced permeation. Real-time confocal microscopy of the DDAPI on uptake of Green Nucleic Acid Stain compared with control


The NexACT multi-route drug delivery platform consists of more than 100 different skin permeation enhancer molecules that could be used in drug formulation to increase permeation and achieve higher bioavailability.


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