Synergistic combinations of penetration enhancers

Synergistic Combinations of Penetration Enhancers and Their Discovery by High-Throughput Screening... 

The lack of significant impact of CPEs on transdermal delivery vehicles is related to the inherent nonspecific activity of CPEs in the different strata of the skin, as discussed earlier. This limitation may be overcome by utilization of mixtures of CPEs. Research has already shown that binary mixtures of CPEs provide increased permeation enhancement as well as increased safety compared to single enhancers. Such unique chemical combinations, called synergistic combinations of penetration enhancers or SCOPE formulations, offer new opportunities in transdermal drug delivery (46). 

Figure 8 (A) In vitro permeability of candidate drug molecules in the presence of synergistic combinations of penetration enhancers (SCOPE) formulations. Open circles indicate passive skin permeability and closed circles indicate skin permeability in the presence of SCOPE formulations as a function of the molecular weight of the solute. (B) In vivo delivery of leuprolide acetate, a synthetic analogue of LHRH in hairless rat model, y-axis shows blood plasma concentration of leuprolide acetate as a function of time for control formulation (open circles) and SCOPE formulation (closed circles). Abbreviation-. LHRH, luteinizing hormone-releasing hormone.

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