Formulation and evaluation of a testosterone transdermal spray

Impact of Antinucleants on Transdermal Delivery ofTestosterone from a Spray

“…As the idea was to formulate a spray, high-viscosity vehicles were clearly undesirable and, for this reason, the antinucleants were first included at a concentration of only 1% (w/v). The cosolvent mixture was selected from the results of an earlier, sophisticated experimental design strategy, 11 which identified this composition as optimal for the transdermal delivery of testosterone.…”

“…11 A mechanical spray, on the other hand, provides more reproducible dosing when the solution in the device has low viscosity. As polymers tend to increase significantly the viscosity of solutions, even when present at low concentrations, it was important to evaluate whether the ''lead'' antinucleants from the above experiments changed the viscosity of ethanol/PG/water in an important fashion.…”

“…In preliminary work, it had been thought that the 4:1:1 ethanol/ PG/water mixture was less effective than expected because of rapid crystallization and the nonattainment of a metastable, supersaturated state. 11 It was further believed, therefore, that an antinucleant would improve matters appreciably. However, despite the encouraging DSC results, this objective was not reached.…”

“…A number of saturated solutions, primarily based upon ethanol/propylene glycol (PG) mixtures, have been examined but no firm evidence that a supersaturation has persisted for a meaningful period of time has been obtained. 11 Indeed, significant crystallization of testosterone was observed, pointing to the necessity of improving the approach so as to stabilize (and prolong the duration of) the supersaturated state.…”

Oil-Frozen W1/O/W2 Double Emulsions for Dermal Biomacromolecular Delivery Containing Ethanol as Chemical Penetration Enhancer

“…14,15 Transdermal penetration enhancers are typically surface-active compounds and even organic solvents. [16][17][18] Ethanol has been extensively studied as a transcutaneous penetration enhancer for low-molecular-weight drugs, [19][20][21][22][23][24] and has been also used as a vehicle for such penetration enhancers as surfactants, 25 terpenes, 26 and biochemical enhancers, 27 as well as a constituent of microemulsions for topical genetic immunization. 28 Ethanol is readily absorbed into skin, 29 and its penetration enhancement is explained by SC intercellular lipid removal.…”