電促進法對 Buspirone 微米乳劑經皮輸送之作用   全文下載

Electrically-Assisted Skin Delivery of Buspirone Submicron Emulsions

本研究之目的為評估電促進法包括離子電透入法（iontophoresis）和電迫法（electroporation）對buspirone hydrochloride微米乳劑之經皮穿透效果。 實驗結果顯示相對於對照組，使用離子電透入法（0.5 mA/cm2, 3小時）和電迫法（1個脈衝，300伏特、200 毫秒；每個脈衝間隔0.5分鐘，共通電10分鐘）分別可增加buspirone在第10小時的累積穿透量2.4和2.1倍。合併使用離子電透入法和電迫法時並沒有產生加乘之效果。長時間使用離子電透入法時，發現在使用後期時，離子電透入法之經皮促進效果會下降，這可能與長時間使用離子電透入法造成皮膚極化有關。間斷性離子電透入法，則有較佳之經皮促進效果。相對於對照組，二種電促進法均可縮短藥物經皮輸送時之延滯時間（lag time）（由3小時可縮短至0.5小時），而獲得較快速的藥理作用。"

The aim of this study was to demonstrate the potential application of electrically-assisted methods, including iontophoresis and electroporation, on the transdermal delivery of buspirone hydrochloride from a submicron emulsion-based system. The results showed that by applied iontophoresis at 0.5 mA/cm2 for 3 h or electroporation at 1 pulse, 300 V, 200 ms, 0.5 min spacing for 10 min, increased the cumulative amount of buspirone at 10 h by 2.4 and 2.1 folds, respectively, compared to passive diffusion. The combination of iontophoresis and electroporation did not show synergistic effects. For long-time application of iontophoresis, the enhancement effect decreased in the later stage due to skin polarization. The duty cycle of current applied was found to increase iontophoretic efficiency. When compared to passive diffusion, the lag time of buspirone-loaded submicron emulsion permeated through skin was shortened from 3 h to 0.5 h with the use of both electrically-assisted methods, indicating that more rapid onset of buspirone could be obtained by using electrically-assisted methods.