Development of L-PLA based Intrascleral Implant for Sustained Intraocular Delivery of Dexamethasone Sodium Phosphate

Nazia Zaman, M. Talukder, T. Haque, K. Alam, K. Fatema
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引用次数: 1

Abstract

The present study was carried out to develop biodegradable intrascleral implants of Dexamethasone Sodium Phosphate and to evaluate the release pattern of the drug from the prepared implants. Intrascleral implants were prepared by using biodegradable polymer L-PLA (m.wt. 61,200 Da). Sodium chloride (NaCl), gelatin and glycerol monostearate (GMS) were used in various formulations to observe the effects of these additives on the release of Dexamethasone Sodium Phosphate from the prepared L-PLA based intrascleral implants. Five different formulations were prepared for this study and were coded as FD-1 (10%drug+L-PLA), FD-2 (20%drug+L-PLA), FD-3 (10%drug+L-PLA+5%NaCl), FD-4 (10%drug+L-PLA +5%Gelatin) and FD-5 (10%drug+L-PLA+10% GMS). Discs were prepared and made into appropriate shape before submerging into the buffer solution of pH 7.4 in different vials. The in vitro release profile of Dexamethasone Sodium Phosphate from the implants showed a biphasic release pattern with an initial burst followed by a diffusive phase. It was observed that FD-1 and FD-2 showed 19.63% and 29.87% release on the first day and 24.22% and 38.5% release respectively at day 30. The drug loading of FD-1 and FD-2 was 10% and 20% respectively. Among FD-3, FD-4 and FD-5; FD-3 showed highest release (32.1%) at day 30 in which 5% NaCl was used. FD-4 showed 27.45% release at day 30 where gelatin, a hydrophilic agent was used and FD-5 containing GMS, a lipid material, was found to be most retarding (19.22% at day 30). The results of the dissolution study provide an idea that L-PLA may be successfully used for the preparation of biodegradable intrascleral implant of Dexamethasone Sodium Phosphate. Key words: Dexamethasone Sodium Phosphate; Bioidegradable polymer; Intrascleral implants. DOI: 10.3329/sjps.v2i1.5817 Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 56-60
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L-PLA基巩膜内植入体用于持续眼内给药地塞米松磷酸钠的研制
本研究旨在制备可生物降解的地塞米松磷酸钠巩膜内植入物,并评价该药物在制备的植入物中的释放规律。采用可生物降解聚合物L-PLA (m.wt)制备巩膜内植入物。61200 Da)。采用氯化钠(NaCl)、明胶(明胶)和单硬脂酸甘油(GMS)配制不同配方,观察这些添加剂对制备的L-PLA基巩膜内植入物中地塞米松磷酸钠释放的影响。制备了5种不同的配方,分别编码为FD-1(10%药物+L-PLA)、FD-2(20%药物+L-PLA)、FD-3(10%药物+L-PLA+5%NaCl)、FD-4(10%药物+L-PLA+5%明胶)和FD-5(10%药物+L-PLA+10% GMS)。制备膜片,并将膜片制作成合适的形状,放入不同小瓶pH为7.4的缓冲液中浸泡。地塞米松磷酸钠的体外释放表现为两相释放模式,先是爆发期,然后是扩散期。观察发现,FD-1和FD-2在第1天的释放量分别为19.63%和29.87%,第30天的释放量分别为24.22%和38.5%。FD-1和FD-2的载药量分别为10%和20%。其中FD-3、FD-4、FD-5;在5% NaCl处理下,FD-3在第30天释放量最高,为32.1%。FD-4在第30天的释放率为27.45%,其中使用了亲水性明胶,而含有脂质材料GMS的FD-5在第30天的释放率为19.22%。溶出度研究结果为L-PLA可成功用于制备可生物降解的地塞米松磷酸钠巩膜内植入物提供了思路。关键词:地塞米松磷酸钠;Bioidegradable聚合物;Intrascleral植入物。DOI: 10.3329/sjps.v2i1.5817斯坦福药物科学杂志Vol.2(1) 2009: 56-60
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