Men suffering from Erection problems could someday have an innovative new way to recapture their mojo. Instead of popping the little blue pill, they may be able to adhere a uniquely designed Transdermal patch to their upper arm or abdomen that will quickly and painlessly infuse Viagra’s Active Ingredient into their bloodstream.
Although the medication itself isn’t new, its method of Delivery is, and the benefits of getting Sildenafil Citrate — Viagra’s active ingredient — by patch are likely to attract plenty of takers, particularly those who are bothered by Viagra’s side effects.
Would Work More Quickly
According to the medical researchers working on this project, the patch also would speed sildenafil citrate into the bloodstream much more quickly than the pill does. While men taking Viagra usually have to wait 30 to 60 minutes before the effects kick in, those getting the drug via patch would likely get results in only a few minutes. Even better, the duration of the patch’s effectiveness probably would increase significantly.
Additionally, the developers of the patch are hopeful that some of oral sildenafil’s side effects would be eliminated by bypassing the digestive tract route for the medication’s delivery. Such side effects include headache, indigestion, muscle pain, and blurred vision.
Alternative Delivery Systems
Scientists at universities in Egypt and Saudi Arabia have been investigating alternative delivery systems for sildenafil for several years now. Their quest for an alternative to oral administration of the drug is driven by the knowledge that less than 50 percent of the medication in a Viagra pill actually makes its way into systemic circulation. A number of factors account for sildenafil’s poor oral bioavailability. These include the drug’s low water solubility and the barriers to absorption caused by foods, most notably high-fat foods.
In an article published in a 2016 issue of “Drug Design, Development, and Therapy,” pharmaceutical researchers from Egypt’s Cairo and Minia universities and King Abdulaziz University in Saudi Arabia note that conventional transdermal patches have been tried before. Transdermal delivery of the medication bypasses presystemic metabolism of the drug, which prolongs the drug’s effects. However, these efforts have failed to achieve optimal results because of the barriers to the drug’s penetration through the stratum corneum, the tough outermost layer of skin.
In their search for a way to optimize transdermal delivery of the medication, researchers turned to transferome technology, which has shown great potential in getting drugs through multiple layers of skin and into systemic circulation with minimal loss of potency.
In preparation for animal testing of their optimized transdermal patch, researchers created a tiny patch — 1 square centimeter — containing minute particles of sildenafil citrate and coated with ultra-thin layers of fat and chemicals designed to maximize the drug’s absorption. The patch designed for animal testing contained the equivalent of 1 milligram of the active ingredient. For human use, the drug is available in strengths ranging from 25 to 100 milligrams.
These tiny patches were then tested on rats to determine how much of the sildenafil actually made its way into the systems of the animals. Results from the animal testing demonstrated that the sildenafil citrate successfully penetrated both the outer and inner layers of the epidermis and into systemic circulation.
Only Animals Tested
Although testing thus far has been limited to animals, researchers in their published report express optimism that these transdermal patches using transferome technology “could be a potential promising drug delivery system” for humans as well.
This new mode of delivering the medication might also prove effective in men who find that orally administered sildenafil simply doesn’t do the job for them. The percentage of men in whom these ED medications are ineffective runs somewhere between 20 and 33 percent, depending on the source of the data. With their ability to get the active ingredient into the system more rapidly and more completely, these new patches could help some men for whom the oral drug is ineffective.
More Expensive Than Pill
However, as a new technology, these transdermal patches using transferome technology undoubtedly would be relatively expensive if they clear all the regulatory hurdles and someday reach the market. The price gap between oral forms of the drug and the patch would be considerable, coming at a time when patents on the oral drugs are expiring, thus opening the door to generic competition.
Interviewed for an article posted at DailyMail.com, British urologist Geoff Hackett, M.D., a member of the board of the British Society for Sexual Medicine, said the patch might prove easier for some men to use. However, he warned that it would be an expensive alternative to the pills, which now go for as little as 42 cents each in the United Kingdom.
Viagra Was a Pioneer
Available in pill form since 1998, Viagra was the first drug of its kind to hit the market. Although a handful of others have followed, it remains one of the top-selling erectile dysfunction drugs. Viagra’s active ingredient, sildenafil citrate, belongs to a family of medications known collectively as PDE5 inhibitors, so-called because they temporarily disable the phosphodiesterase-5 enzyme. In men with compromised blood flow, the pesky PDE5 enzyme can make it difficult or even impossible to get and keep an erection strong enough for intercourse.
To understand how Viagra and the other PDE5 inhibitors work, it’s helpful to know a bit about the mechanics of the erectile process. Erections originate in the brain as feelings of sexual desire or a nervous system response to physical stimulation of the penis or other erogenous zones.
Nitric Oxide a Key Player
Once the brain detects such stimuli, it sends a flood of nitric oxide coursing toward the male genitals. The nitric oxide triggers secondary chemical reactions, one of which gives rise to a substance known as cyclic guanosine monophosphate, or cGMP. The primary job of cGMP is to relax the smooth muscles lining the blood vessels that supply the penis. As these arteries relax and expand, blood surges into the penis and creates an erection. At the same time, veins carrying blood away from the penis contract and temporarily keep the blood in place, maintaining the erection until sexual activity is complete.
For men whose vascular systems are already compromised, the PDE5 enzyme can be problematic. One of its primary functions is the chemical breakdown of cGMP. While this poses no real problem for men with strong blood flow, it can sabotage the erection process in men with vascular problems. By holding the PDE5 enzyme at bay for a matter of hours, sildenafil citrate and the other PDE5 inhibitors open a window of time during which such men can more readily get and keep an erection and enjoy sexual activity.
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