Hydrogel forming microneedle-mediated transdermal delivery of sildenafil citrate from polyethylene glycol reservoir: An ex vivo proof of concept study

Erectile dysfunction (ED) is a disorder that often occurs in men worldwide. One of the drugs used as the first-line therapy for erectile dysfunction is sildenafil citrate (SC). Unfortunately, SC was commonly found in oral, injection, and transdermal dosage forms with some limitations, mainly related to low oral bioavailability caused by the occurrence of first-pass metabolism in the liver, and poor patient comfort and compliance. Therefore, it was essential to develop dosage forms to overcome these limitations. We developed hydrogel-forming microneedles (HFM) that can facilitate transdermal delivery of SC by penetrating the stratum corneum. HFM was made using polyvinyl alcohol (PVA) and polyvinyl pyrrolidone (PVP) as polymers and several variations of tartaric acid as crosslinking agents. The evaluation of swelling properties, mechanical resistance, and penetration ability showed that the HFM produced had good insertion properties and swelling capabilities ranging from 300% to 700%. This HFM was designed to be integrated with a polyethylene glycol (PEG) reservoir prepared using several types of PEG with different molecular weights. The ex vivo permeation study showed that up to 80% of SC (equivalent to 20.2 & PLUSMN; 0.29 mg/mL) was delivered transdermally from this combined dosage form. For the first time, SC has been successfully developed into an HFM that was integrated with a PEG reservoir which was non-irritating, safe, and painless. It also had promising results for increasing the effectiveness of ED therapy.