Improved transdermal delivery of prostaglandin E1 through hairless mouse skin: combined use of carboxymethyl-ethyl-beta-cyclodextrin and penetration enhancers
| Autor: | Tadanori Yano, Kanji Noda, Hirotoshi Adachi, Tetsumi Irie, Kaneto Uekama, Masaru Saita |
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| Rok vydání: | 1992 |
| Předmět: |
Skin Absorption
Pharmaceutical Science Beta-Cyclodextrins Absorption (skin) Pharmacology Administration Cutaneous Dosage form Ointments chemistry.chemical_compound Mice Medicine Animals Pyrroles Alprostadil Prostaglandin E1 Transdermal Skin Cyclodextrins Drug Carriers Mice Hairless business.industry beta-Cyclodextrins Azepines Hairless chemistry Regional Blood Flow lipids (amino acids peptides and proteins) Female Drug carrier business Azone |
| Zdroj: | The Journal of pharmacy and pharmacology. 44(2) |
| ISSN: | 0022-3573 |
| Popis: | The optimal prescription of transdermal preparations of prostaglandin E1 (PGE1) for treatment of peripheral vascular diseases has been investigated. The chemical stability of PGE1 in fatty alcohol/propylene glycol (FAPG) ointment was markedly improved by carboxymethyl-ethyl-β-cyclodextrin (CME-β-CyD). Application of a PGE1 ointment containing the penetration enhancer, 1-dodecylazacycloheptane-2-one (Azone) or 1-[2-(decylthio)ethyl]azacyclopentane-2-one (HPE-101), onto the skin of hairless mice showed the increase of blood flow in the skin due to the vasodilating action of PGE1. In particular, the ointment containing a PGE1-CME-β-CyD complex supplemented with HPE-101 showed the most prominent increase of the blood flow. Compared with other ointments, this ointment was found to show significantly greater transfer of HPE-101 into in-vitro preparations of the skin of hairless mice. Transfer of PGE1 into the skin was thought to be facilitated by this increased transfer of HPE-101. These results suggest that a combination of CME-β-CyD and HPE-101 is useful for designing PGE1 ointments for topical application with good chemical stability and percutaneous permeability. |
| Databáze: | OpenAIRE |
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