원보 : 프로스타글란딘 E1 에칠에스테르의 외용 리오겔 제제 설계

External lyogels containing prostaglandin E₁ethyl ester(PGE₁-EE), a produrg of prostaglandin E₁(PGE₁) as a therapeutic agent for erectile dysfunction, were formulated to overcome the aqueous instability and enhance the percutaneous absorption. Lyogels of PGE₁-EE were prepared with ethanol (EtOH)/proplyene glycol (PG) cosolvent system as a vehicle, cineol as an enhancer, and hydroxypropylcellusose as a gelling agent. In vitro percutaneous absorption studies were performed to determine the rate of PGE₁ absorption through rat or hairless mouse skin. The permeability of PGE₁-EE lyogel with enhancer was 16-fold greater than that of lyogel without enhancer. Cosolvent produced 9-fold increase in percutaneous absorption. Pharmacodynamic effects of lyogels were evaluated in mature male cats in terms of intracavernosal pressure (ICP). Lyogles containing 0.01% of PGE₁-EE showed higher ICP compared to intraurethral preparation of PGE₁(1%) and enhancer-free control lyogel. The shelf-life (t_(10%) of lyogel at refrigerated condition (4℃) was calculated as 928 days, which is 4.2 times longer than that of control hydrogel. As a result, PGE₁-EE was formulated successfully to a lyogel system with a selective enhancer and cosolvent system for the topical delivery of PGE₁.