| 摘要: | Glutathione作為抗白內障藥物時,其療效受限於藥物的輸移欠佳進而影響眼用藥物的生體可用率。在本研究中,含Glutathione之微脂粒是採用改良自乙醇注入法之製造技術製備,已負載Glutathione之微脂粒,其穿透豬眼角膜之藥物輸移則以體外實驗進行評估,隨後角膜與微脂粒間的交互作用是以熱分析法來檢測。經由上述之實驗設計,體外穿透實驗的結果顯示,微脂粒包覆型藥物的經角膜輸移量顯著高於游離型藥物溶液,由於磷脂質的不同其大小依序是DSPC>DPPC>DMPC,而且,相較於游離態之藥物溶液,微脂粒有較高的眼角膜內藥物負載量與較緩慢的藥物排除速率,微脂粒包覆能延長藥物在眼睛的留置時間而導致持續的治療效果。為了要傳輸藥物通過眼角膜,又不會造成眼角膜組織明顯的變化,採微脂粒包覆藥物的方式是極佳的選擇。
The effectiveness of glutathione as an anticataract agent is limited by poor drug delivery and limited ocular bioavailability. In this study, liposomes containing glutathione have been prepared from different phospholipids using a modification of the ethanol injection technique. The in vitro transcorneal delivery of liposomal glutathione through pig's eyes were studied. Then, the interaction occurring between liposome and pig's cornea was determined by DSC. In the in vitro perfusion studies, the results show that the transcorneal flux of the GSH-loaded liposomes was significantly (p<0.05) higher than that of the free drug solution. For the three lipids investigated drug corneal penetration decreased in the order DSPC>DPPC>DMPC. Moreover, the loading of the drug in the cornea with liposome was higher, and that drainage of the liposomal GSH from the cornea was slower than for the solution form. Liposome-encapsulation is able to prolong the residence time of drug in eye and that results in sustained therapeutic effect. To transfer the drug through the cornea did not cause significantly alternation in structure of the tissue and to maintain the pharmacological activity, liposome-encapsulation of the drug is a good choice. |
