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�й�ҩѧ��־ 2012, Vol. 47 Issue (17) :1391-1395    DOI:
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GAO Ying1�� WU Yi-jun1�� LI Jie1��3�� JING Rong-rong2�� LI Wen-sheng1�� WEN Jun2

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ժҪ Ŀ�� �Ʊ���������������-�ǻ����Ṳ���PLGA��/Eudragit RS 100���û���΢�򣬲����б��������� ����O/W�ܼ��ӷ����Ʊ���������PLGA/Eudragit RS 100΢�򣬶�΢��ı�����̬����ҩ���������ʡ������ͷ��ص㡢�������л��ܼ��������������λ�����˱���������ʹ��������Ĥɫ����Ƥϸ����RPE cells�������հ�΢���ϸ�����ԡ���� �������PLGA��Eudragit RS 100������Ϊ1��3����������΢�򣬵羵�۲�����ֲ����ȣ�����⻬��ƽ������Ϊ��1 676.4±739.5��nm����ҩ��Ϊ��18.79±0.19��%��������Ϊ��98.25±2.11��%����1�����ͻ�ͣ������Ի����ͷ�һ�������ң��л�������ƽ��Ϊ��267.33±13.57��ppm���հ�΢������λΪ����ɣ��հ�΢����ϸ�����ԡ����� ��������PLGA/Eudragit RS 100���û���΢����а����ʸߣ�����խ�������ͷŻ�������ȫ�Ժõ��ص㣬���кܺõ��ٴ�Ӧ��ǰ����
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Abstract�� OBJECTIVE To obtain sustained-release indomethacin PLGA/Eudragit RS 100 microspheres for ophthalmic application and to evaluate its quality. METHODS The microspheres were prepared by O/W solvent evaporation using PLGA and Eudragit RS 100. The morphological�� drug content�� entrapment efficiency�� release behavior�� particle size�� residual organic solvent�� Zeta potential of indomethacin PLGA/Eudragit RS 100 microspheres were determined�� meanwhile�� the cytotoxicity of blank microspheres was evaluated using PRE cells. RESULTS Indomethacin microspheres containing PLGA and Eudragit RS 100 at the weight ratio of 1��3 had even particle size distribution�� and their surfaces were smooth under scan electronic microscope�� and the mean diameters were (1 676.4±739.5) nm. The drug content and entrapment efficiency of the microspheres were (18.79±0.19) % and (98.25±2.11) %�� respectively. Indomethacin was released slowly for a month from the microspheres�� though burst release was observed within 24 h. The mean residual organic solvent was (267.33±13.57) ppm. The zeta potential of all blank PLGA/ Eudragit RS 100 microspheres was positive. The blank microspheres showed no sign of toxicity. CONCLUSION Indomethacin PLGA/Eudragit RS 100 microspheres have a better clinical application prospect due to its high entrapment efficiency�� narrow distribution�� slow release and ocular safety.
Keywords�� indomethacin,   PLGA,   Eudragit RS 100,   sustained-release microspheres,   solvent evaporation     
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��ӱ, ���վ�, ��ܵ� .�����������û���΢����Ʊ�����������[J]  �й�ҩѧ��־, 2012,V47(17): 1391-1395
GAO Ying-, WU Yi-Jun-, LI Jie- etc .Preparation and Physicochemical Evaluation of Indomethacin Sustained-Release Microspheres for Ophthalmic Delivery[J]  Chinese Pharmaceutical Journal, 2012,V47(17): 1391-1395
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[1] BAUDOUIN C�� NORDMANN J P�� DENIS P�� et al. Efficacy of indomethacin 0.1% and fluorometholone 0.1% on conjunctival inflammation following chronic application of antiglaucomatous drugs [J]. Graefes Arch Clin Exp Ophthalmol�� 2002�� 240(11)��929-935.
[2] FRUCHT-PERY J�� SIGANOS C S�� SOLOMON A�� et al. Topical indomethacin solution versus dexamethasone solution for treatment of inflamed pterygium and pinguecula��a prospective randomized clinical study [J]. Am J Ophthalmol�� 1999�� 127(2)��148-152.
[3] ALLAIRE C�� LABLACHE C M�� TRINQUAND C�� et al. Comparative efficacy of 0.1% indomethacin eyedrops�� 0. 03% flurbiprofen eyedrops and placebo for maintaining peroperative mydriasis [J]. J Fr Ophtalmol�� 1994�� 17(2)��103-109.
[4] BAUDOUIN C�� NORDMANN J P�� DENIS P�� et al. Efficacy of indomethacin 0.1% and fluorometholone 0.1% on conjunctival inflammation following chronic application of antiglaucomatous drugs [J]. Graefes Arch Clin Exp Ophthalmol�� 2002�� 240(11)��929-935.
[5] LI W S�� JIANG D Y�� DING J G�� et al. Indomethacin induced apoptosis in cultured human fetal retinal pigment epithelium cells in vitro [J]. Rec Adv Ophthalmol(�ۿ��½�չ)�� 2003�� 23(2)��90-92.
[6] EUGEN BARBU�� LILIANA VERESTIUC�� THOMAS G�� et al. Polymeric materials for ophthalmic drug delivery��trends and perspectives [J]. J Mater Chem�� 2006�� 16��34����3439-3443.
[7] WEN J�� CHEN Z J�� LI W S. Pharmacokinety of intravitreous administration of indomethin [J]. Chin Ophthal Res(�ۿ��о�)�� 2006�� 24(2)��129-131.
[8] JENQUIN M R�� MCGINITY J W. Characterization of acrylic resin matrix films and mechanisms of drug-polymer interactions [J]. Int J Pharm�� 1994�� 101��1-2����23-24.
[9] CHEN Y�� WANG B H�� WU D. Pharmaceutical application of polyacrylic resin [J]. China Pharm(�й�ҩҵ)�� 2007�� 16(14)��25-27.
[10] OTH M P�� MOES A J. Sustained release solid dispersions of indomethacin with Eudragit RS and RL [J]. Int J Pharm�� 1989�� 55��2-3����157-164.
[11] YEN S Y�� SUNG K C�� WANG J J�� et al. Controlled release of nalbuphine propionate from biodegradable microspheres��in vitro and in vivo studies [J]. Int J Pharm�� 2001�� 220(1-2)��91-99.
[12] ANANCHARUNGSUK W�� POLPANICH D�� JANGPATARAPONGSA K�� et al. In vitro cytotoxicity evaluation of natural rubber latex film surface coated with PMMA nanoparticles [J]. Colloids Surf B Biointerfaces�� 2010�� 78(2)��328-333.
[13] XU G M�� ZHANG C X�� NING L��et al. Evaluation on the cytotoxicity of Gallium alloy by MTT-assay [J]. Chin J Stomatol(�л���ǻҽѧ��־)�� 2001�� 36(3)��28-31.
[14] LU B. New Techniques and New Dosage Forms of Drugs(ҩ���¼������¼���) [M]. Beijing��People′s Medical Publishing House�� 1998��415-433.
[15] PIGNATELLO R�� BUCOLO C�� FERRARA P�� et al. Eudragit RS100 nanosuspensions for the ophthalmic controlled delivery of ibuprofen [J]. Eur J Pharm Sci�� 2002�� 16(1-2)��53-61.
[16] ADIBKIA K�� JAVADZADEH Y�� DASTMALCHI S��et al. Naproxen-eudragit RS100 nanoparticles��preparation and physicochemical characterization [J]. Colloids Surf B Biointerfaces�� 2011�� 83(1)��155-159.
[17] SINHA V R�� TREHAN A. Formulation�� characterization�� and evaluation of ketorolac tromethamine-loaded biodegradable microspheres [J]. Drug Deliv�� 2005�� 12(3)��133-139.
[18] SHIVE M S�� ANDERSON J M. Biodegradation and biocompatibility of PLA and PLGA microspheres [J]. Adv Drug Deliv Rev�� 1997�� 28(1)��5-24.
[19] SHI H J�� WEI K�� NAN K H��et al. Ofloxacin-loaded PLGA Microcapsules��Preparation�� characterization and the factors affecting loading efficiency [J]. J Mater Sci Eng(���Ͽ�ѧ�빤��ѧ��)�� 2009�� 27(2)��282-287.
[20] ZHANG S�� DENG H�� BAI H F�� et al. CGC Detection of residual dichloromethane in nestorone microspheres [J]. Chin J Mod Drug(�й��ִ�ҩ��Ӧ��)�� 2009�� 3(15)��282-287.
[21] TABATA Y�� IKADA Y. Effect of the size and surface charge of polymer microspheres on their phagocytosis by macrophage [J]. Biomaterials�� 1988�� 9(4)��356-362.
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[3] �����࣬���������������������������ܣ��ߴ���.�����������ܻ���ԭλ�������Ʊ��;ֲ��̼����о�[J]. �й�ҩѧ��־, 2012,47(16): 1313-1317
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[5] ֣��Ƽ �ܵ�Ӣ ��ܿ�� ���� ������ �ィ��.�Ǿ������ε����ȵ��ؾ�����-�ǻ����Ṳ����������������𤸽�Լ���������[J]. �й�ҩѧ��־, 2010,45(13): 1005-1010
[6] ���� ;������ ;��ѧũ; . ˫�ȷ�����˿�ص��� - �Ǿ��ǻ���΢����Ʊ�������������[J]. �й�ҩѧ��־, 2009,44(21): 1642-1647
[7] ����;����;����;������.���γɵ���΢����������������ϵͳ���Ʊ�����ҩ�����о�[J]. �й�ҩѧ��־, 2009,44(13): 1005-1008
[8] ���˽�;������;��ѩӥ;�߾�;����;����.���͹�΢�����жԻ�ѧҩ��ľ�Ƥ��͸����[J]. �й�ҩѧ��־, 2008,43(12): 914-917
[9] ��ޱ;����÷;�Ų�ϼ;������;������.����������С��Ѫ������������������ҩ��ѧ�о�[J]. �й�ҩѧ��־, 2008,43(01): 48-50
[10] ����;÷�˹�.������������΢����Ʊ��������ͷŵ��о�[J]. �й�ҩѧ��־, 2007,42(11): 836-838
[11] ��־ƽ;����;÷�˹�.ע���ô���������ɻ���΢�����������ۼ����������Կ���[J]. �й�ҩѧ��־, 2006,41(17): 1320-1323
[12] ����ΰ;�ƺ���;����;������;�Ӵ��.��������ҩ���лøCYP2C9���Ե�΢����ģ��[J]. �й�ҩѧ��־, 2006,41(07): 551-555
[13] ����;�ņ�;������.��ЧҺ��ɫ�׷��ⶨ��������˨�ĺ������й�����[J]. �й�ҩѧ��־, 2005,39(15): 1176-1177
[14] ����;��Ƽ;��ʤԴ;������;�����;�Թ���;��ϣ��;����Ȩ.��SARS-CoV�����򵰰�����-�����Ṳ����΢����Ʊ�������[J]. �й�ҩѧ��־, 2005,39(14): 1077-1079
[15] �ܽ�;½����.��������ø���ͽ᳦����ѹ�ư���Ƭ������[J]. �й�ҩѧ��־, 2005,39(05): 367-370
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