Discovery of Transdermal Penetration Enhancers by High-throughput Screening



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                Due to its effectiveness of the INSIGHT method, it is used to screen a large amount of chemical penetration enhancers. From this

population, the combinatory of CPEs generates even a greater number of SCOPEs. If the traditional method Franz Diffusion Cells (FDC) is used, it

would take a longer time and a greater effort to screen SCOPEs. Specifically, it is 100-fold more efficient than other methods. Therefore, INSIGHT

helps to discover enhancer library efficiently.



                                                            Fig8. The efficacy of INSIGHT as compared to FDC method


            Good SCOPES must have high potency and synergistic effect. The following results are done for the 4 candidates for CPEs (SLA, PP,

NLS, S20) screened from thousands of other CPEs. SCOPEs of these CPEs are generated in two pairs (SLA:PP and NLS:S20).


                                                                Fig9. SCOPEs Synergistic Effect


         Colored scale was generated using computer software that measures the permeability of pig skin stratum corneum layer with the x and y axis

represents each concentration CPEs used in the SCOPEs formula.


        Further irritation assessment testing using the discovered SCOPEs agreed with the synergistic effect of the combinatorial CPEs.


                                                             Fig10. CPE alone has very low Conductivity ER and even high irritation potential. However, the

                                                                       combinatorial effects of the two CPEs increase ER and lower the IP.


            In-vitro testing measures the drug concentration of transdermal drug using SCOPEs and non-chemical penetration enhancement shows a

            strong agreement with the computer generated result.


                                                  Fig11. Plasma concentration of transdermal drug leuprolide with the aid of SCOPE SLA:PP (close circles) is   significantly different from drug concentration of the unaided transdermal drug.



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