Eperon S, Bossy-Nobs L, Petropoulos I K, Gurny R, Guex-Crosier Y
Jules Gonin Eye Hospital, Lausanne University, 15, Avenue de France, 1000 Lausanne 7, Switzerland.
Int J Pharm. 2008 Mar 20;352(1-2):240-7. doi: 10.1016/j.ijpharm.2007.10.054. Epub 2007 Nov 17.
Cataract surgery is often performed in patients suffering from associated pathologies. Our goal is to develop a biodegradable drug delivery system (DDS) combined with the artificial intraocular lens (IOL). DDS were manufactured using poly(D,L-lactide-co-glycolide), or PLGA, and were loaded with triamcinolone acetonide (TA). The loading capacity was approximately 1050 microg of TA per DDS. The higher the molecular weight of PLGA (34,000, 48,000 and 80,000Da), the slower was the release of TA in vitro. Cataract surgery was performed on the right eye of rabbits. IOL was inserted with (i) no DDS, (ii) unloaded DDS PLGA48000, (iii) one loaded DDS PLGA48000, (iv) two loaded DDS. The number of inflammatory cells and the protein concentration were measured in the aqueous humor (AH). Unloaded DDS showed good ocular biocompatibility. One DDS PLGA48000 loaded with TA significantly reduced postoperative ocular inflammation. Two loaded DDS PLGA48000 was even more effective in inhibiting such inflammation. On long-term observation (days 63 and 84), reduction of inflammation could be obtained by insertion of one DDS PLGA48000 and a second DDS PLGA80000. Therefore, our "all in one" system is very promising since it could replace oral treatment and reduce the number of intraocular injections.
白内障手术通常在患有相关病症的患者中进行。我们的目标是开发一种与人工晶状体(IOL)相结合的可生物降解药物递送系统(DDS)。DDS采用聚(D,L-丙交酯-共-乙交酯)或PLGA制造,并负载曲安奈德(TA)。每个DDS的载药量约为1050微克TA。PLGA的分子量越高(34000、48000和80000Da),TA在体外的释放速度就越慢。对兔子的右眼进行白内障手术。植入IOL时分别为:(i)不使用DDS,(ii)未负载的DDS PLGA48000,(iii)一个负载的DDS PLGA48000,(iv)两个负载的DDS。测量房水(AH)中的炎症细胞数量和蛋白质浓度。未负载的DDS显示出良好的眼生物相容性。一个负载TA的DDS PLGA48000显著减轻了术后眼部炎症。两个负载的DDS PLGA48000在抑制这种炎症方面甚至更有效。在长期观察(第63天和第84天)中,通过植入一个DDS PLGA48000和第二个DDS PLGA80000可以减轻炎症。因此,我们的“一体化”系统非常有前景,因为它可以替代口服治疗并减少眼内注射的次数。