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<p>Omeprazole is the first in a class medication that inhibits gastric secretion. However, it has a low stability, low bioavailability, and a short half-life after peroral administration. In the current study, nonionic microemulsions containing omeprazole were formulated and characterized for transdermal and intranasal administration as alternative application routes. The droplet size, rheological characteristics, polydispersity index, permeability through rat and human skin, rat epidermis, and <i>in vivo</i> bioavailability in rats were studied. With these formulations with droplet sizes below 100&#xa0;nm, an omeprazole permeation with fluxes ranging from 0.86 to 9.945&#xa0;µg·cm<sup>−2</sup>&#xa0;h<sup>−1</sup> was observed for excised rat epidermis. However, the full-thickness human and rat skin exhibited drug entrapment. The <i>in vivo</i> study demonstrated that the relative bioavailabilities of the intranasal and transdermal administration were 332% and 103%, respectively, compared to an oral solution. Overall, the formulated microemulsions were stable and could serve as effective carriers, making them promising delivery systems for omeprazole delivery via transdermal and intranasal routes.</p> Graphical Abstract <p></p>

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Developing and Evaluating Stable Microemulsion Systems for Potential Intranasal and Transdermal Application of Omeprazole

  • 期刊论文

  • 发表日期：

    2026年3月4日

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  • Heba Hamid Hussein,
  • Jamal ِِAlyoussef Alkrad,
  • Loay Kahled Hassouneh,
  • Aktham Mestareehi,
  • Hatim S. AlKhatib,
  • Shereen M. Assaf,
  • Eman Zmaily Dahmash

摘要

Omeprazole is the first in a class medication that inhibits gastric secretion. However, it has a low stability, low bioavailability, and a short half-life after peroral administration. In the current study, nonionic microemulsions containing omeprazole were formulated and characterized for transdermal and intranasal administration as alternative application routes. The droplet size, rheological characteristics, polydispersity index, permeability through rat and human skin, rat epidermis, and in vivo bioavailability in rats were studied. With these formulations with droplet sizes below 100 nm, an omeprazole permeation with fluxes ranging from 0.86 to 9.945 µg·cm−2 h−1 was observed for excised rat epidermis. However, the full-thickness human and rat skin exhibited drug entrapment. The in vivo study demonstrated that the relative bioavailabilities of the intranasal and transdermal administration were 332% and 103%, respectively, compared to an oral solution. Overall, the formulated microemulsions were stable and could serve as effective carriers, making them promising delivery systems for omeprazole delivery via transdermal and intranasal routes.

Graphical Abstract