Electroporation-delivered transdermal neostigmine in rats: equivalent action to intravenous administration
| Autor: | Judit Bóta, Gábor Varju, Róbert Gáspár, Erzsébet Csányi, Mária Budai-Szűcs, Boglárka Balázs, Anita Sztojkov-Ivanov, Kálmán Ferenc Szűcs, Szilvia Berkó |
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| Jazyk: | angličtina |
| Rok vydání: | 2016 |
| Předmět: |
electroporation
Pharmaceutical Science Pharmacology Administration Cutaneous 030226 pharmacology & pharmacy Rats sprague dawley Gastrointestinal absorption smooth muscle Rats Sprague-Dawley 03 medical and health sciences 0302 clinical medicine Drug Delivery Systems Smooth muscle Drug Discovery medicine Animals plasma level Transdermal Original Research Drug Design Development and Therapy Dose-Response Relationship Drug business.industry Electroporation neostigmine Drug administration contraction Plasma levels Neostigmine Rats Gastrointestinal Absorption 030220 oncology & carcinogenesis Anesthesia transdermal Administration Intravenous business medicine.drug Muscle Contraction |
| Zdroj: | Drug Design, Development and Therapy |
| ISSN: | 1177-8881 |
| Popis: | Szilvia Berkó,1,* Kálmán F Szűcs,2,* Boglárka Balázs,1,3 Erzsébet Csányi,1 Gábor Varju,4 Anita Sztojkov-Ivanov,2 Mária Budai-Szűcs,1 Judit Bóta,2 Róbert Gáspár2 1Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Szeged, Hungary; 2Department of Pharmacodynamics and Biopharmacy, Faculty of Pharmacy, University of Szeged, Szeged, Hungary; 3Gedeon Richter Plc., Budapest, 4Dr Derm Clinic of Anti-Aging Dermatology, Aesthetic Laser and Plastic Surgery, Budapest, Hungary *These authors contributed equally tothis work Purpose: Transdermal electroporation has become one of the most promising noninvasive methods for drug administration, with greatly increased transport of macromolecules through the skin. The cecal-contracting effects of repeated transdermal electroporation delivery and intravenous administration of neostigmine were compared in anesthetized rats. Methods: The cecal contractions were detected with implantable strain gauge sensors, and the plasma levels of neostigmine were followed by high-performance liquid chromatography. Results: Both intravenously and EP-administered neostigmine (0.2–66.7 µg/kg) increased the cecal contractions in a dose-dependent manner. For both the low doses and the highest dose, the neostigmine plasma concentrations were the same after the two modes of administration, while an insignificantly higher level was observed at a dose of 20 µg/kg after intravenous administration as compared with the electroporation route. The contractile responses did not differ significantly after the two administration routes. Conclusion: The results suggest that electroporation-delivered neostigmine elicits action equivalent to that observed after intravenous administration as concerning both time and intensity. Electroporation permits the delivery of even lower doses of water-soluble compounds through the skin, which is very promising for clinical practice. Keywords: transdermal, electroporation, neostigmine, smooth muscle, contraction, plasma level |
| Databáze: | OpenAIRE |
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