Bioavailability enhancement of sildenafil citrate via hydrogel-forming microneedle strategy in combination with cyclodextrin complexation

[Display omitted] Sildenafil citrate (SIL) as a first-line treatment for erectile dysfunction is currently reported to have poor solubility and bioavailability. Moreover, SIL undergoes first-pass metabolism when taken orally and its injection can lead to discomfort. In this study, we introduce a nov...

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Veröffentlicht in:International journal of pharmaceutics 2024-04, Vol.655, p.124053-124053, Article 124053
Hauptverfasser: Sulistiawati, Sulistiawati, Kristina Enggi, Cindy, Wiyulanda Iskandar, Israini, Rachmad Saputra, Rizki, Sartini, Sartini, Rifai, Yusnita, Rahman, Latifah, Aswad, Muhammad, Dian Permana, Andi
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Sprache:eng
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Zusammenfassung:[Display omitted] Sildenafil citrate (SIL) as a first-line treatment for erectile dysfunction is currently reported to have poor solubility and bioavailability. Moreover, SIL undergoes first-pass metabolism when taken orally and its injection can lead to discomfort. In this study, we introduce a novel transdermal delivery system that integrates hydrogel-forming microneedles with the inclusion complex tablet reservoir. The hydrogel-forming microneedle was prepared from a mixture of polymers and crosslinkers through a crosslinking process. Importantly, the formulations showed high swelling capacity (>400 %) and exhibited adequate mechanical and penetration properties (needle height reduction  100 %. Therefore, the approach developed in this study could potentially increase the efficacy of SIL in treating erectile dysfunction by being non-invasive, safe, avoiding first-pass metabolism, and increasing drug bioavailability.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2024.124053