Correzioni

Development of a Sildenafil Citrate Microemulsion-Loaded Hydrog

• Bell, Brown and Ellis, 1998), they discovered that PDE5 was the dominant hydrolysis pre-enzyme in the cytosolic fraction of the cavernous human body and suggested that one of its synthesised inhibitors, Sildenafil, which is a potent, selective inhibitor PDE5 may be useful as an oral medicine in the treatment of erectile dysfunction.

• Sildenafil Citrate is known as a PDE5 enzyme-inhibiting drug.

• PDE5 is responsible for the degradation of cGMP in the cavernous body of the penis.

• The molecular structure of Sildenafil is very similar to cGMP, this ends up causing a mechanism of competition for PDE5.

• Sildenafil then binds to PDE5, which causes cGMP to circulate more. cGMP induces several reactions that cause a decrease in the amount of intracellular calcium and promote smooth muscle relaxation and improvement in blood flow and, consequently, penile erection.

• They said in the article that oral sildenafil has low availability and many side effects, for this reason, the authors and researchers have formulated a hydrogel microemulsion system to administer sildenafil transdermally.

• According Smith II et al., 2013, adverse effects most often reported with the use of PDE5 medications are: headache, flushing, dyspepsia, nasal congestion, visual disturbance and myalgia.

• In the same article, the authors say that sildenafil is only available in the form of pills and that some studies show that PDE-inhibiting drugs can be administered topically.

• One of the important aspects in pharmaceutical technology is the existence of the interaction of drugs with interfaces of supramolecular aggregates in compounds that are amphiphilic.

• This aspect is relevant due to the biological changes that take place in the presence of these compounds in pharmaceutical formulas.

• TDDS is an attractive alternative to traditional oral and hypodermic delivery, as it overcomes the limitation of first-pass hepatic metabolism found by oral administration and has many advantages, such as safe, painless and easy to use, in contrast to intravenous injection.

• With this in mind, the authors of the article formulated a microemulsion using isopropyl myristate, tween 80, PEG400, and water (30: 20: 40: 10) with 2% hydrogel w / w poloxamer 188.

• This would be a good alternative to oral administration.

• What attracted the researchers was the many advantages of micro emulsions such as thermodynamic stability, spontaneous formation, greater availability, appearance, penetration through biological membranes.

• They wanted to test different formulations for the microemulsion system and see which would be the most suitable in terms of solubility, spreadability, concentration, permeability, toxicity and other variants.

• Delivery of drugs directly to the penis in a controlled manner would be a good option for men who cannot for some reason use oral medications, such as men who have many adverse effects.

• The authors also took into account the fact that topical therapy in comparison with systemic therapy is less effective, which is an important limitation, especially in more severe cases.

• In the article evaluated in this dissertation, the researchers used a system of transdermal delivery system.

• It was made and analysed in the following steps: visual inspection, particle size, pH, spread ability, cell membrane permeability, sildenafil drug content and viscosity.

• It is very important to have knowledge about the mechanism of action of sildenafil to understand how to evaluate drug efficacy or how to develop formulations systems.

• In my personal opinion, the idea of develop a Sildenafil Micro emulsion is very good idea because in the market there is not transdermal formulation of sildenafil till date and has a good potency because take ral medicine brings different types of adverse effects, allergic reactions or interactions with other medications or long-term adverse effects., also, topic medicines have a lot advantages if we compare it with oral medicine, like I already wrote about above.

• A micro emulsion is easy to apply and easy to the patients understand how to administer it by themselves, besides being a way to administer a drug in a contr