Mucoadhesive microdiscs engineered for ophthalmic drug delivery: effect of particle geometry and formulation on preocular residence time.
Mucoadhesive microdiscs engineered for ophthalmic drug delivery: effect of particle geometry and formulation on preocular residence time.
复制标题
用于眼科药物输送的粘膜粘附微盘：颗粒几何形状和配方对眼前停留时间的影响。
DOI：
10.1167/iovs.08-2515
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发表时间：
2008
影响因子：
4.4
通讯作者：
Prausnitz,MarkR
中科院分区：
文献类型：
--
作者：
Choy,YoungBin;Park,Jung-Hwan;McCarey,BernardE;Edelhauser,HenryF;Prausnitz,MarkR
目的.为了测试的假设，粘膜粘附微盘配制在一个快速溶解的片剂可以增加眼前停留时间。直径小于10 μm的微粒通过乳化制备，其中聚（乳酸-共-乙醇酸）作为核心材料，在某些情况下，聚（乙二醇）作为粘膜粘附促进剂。为了检查颗粒几何形状的影响，还将微粒切割成具有平坦表面（即，微盘），并与球形颗粒（即，微球）进行比较。在剪切应力下的粘膜层上测试微粒的体外粘膜粘附，模仿人类眨眼。所得的微粒也被配制成两种剂型，水悬浮液和干片剂，以测试制剂对兔体内眼前空间微粒的保留能力的影响。粘膜粘附微盘粘附更好地模拟眼表比其他类型的微粒。当在体内兔眼盲囊中给予包埋有粘膜粘附微盘的干燥片剂时，这些微盘表现出比本研究中测试的其他制剂更长的保留时间。在给药后10分钟和30分钟，分别有超过40%和17%的粘膜粘附微盘保留在眼前表面上。从眼睛表面的荧光图像显示，粘膜粘附的microdiscs保持至少1小时，在较低的穹窿。这项研究表明，粘膜粘附微盘配制成干片剂可以实现延长的停留时间在眼前表面，因此是一个有前途的药物输送系统的眼科应用。
purpose. To test the hypothesis that mucoadhesive microdiscs formulated in a rapidly dissolving tablet can increase preocular residence time.methods. Microparticles smaller than 10 μm in diameter were fabricated by emulsification with poly (lactic-co-glycolic acid) as a core material and, in some cases, poly (ethylene glycol) as a mucoadhesion promoter. To examine the effect of particle geometry, microparticles were also cut to have flat surfaces (ie, microdiscs) and were compared with spherical particles (ie, microspheres). In vitro mucoadhesion of microparticles was tested on a mucous layer under shear stress, mimicking the human blink. The resultant microparticles were also formulated in two dosage forms, an aqueous suspension and a dry tablet, to test the effect of formulation on the retention capacity of microparticles on the preocular space of rabbits in vivo.results. Mucoadhesive microdiscs adhered better to the simulated ocular surface than did other types of microparticles. When a dry tablet embedded with mucoadhesive microdiscs was administered in the cul-de-sac of the rabbit eye in vivo, these microdiscs exhibited longer retention than the other formulations tested in this study. More than 40% and 17% of mucoadhesive microdiscs remained on the preocular surface at 10 minutes and 30 minutes after administration, respectively. Fluorescence images from the eye surface showed that mucoadhesive microdiscs remain for at least 1 hour in the lower fornix.conclusions. This study demonstrated that mucoadhesive microdiscs formulated in a dry tablet can achieve a prolonged residence time on the preocular surface and thus are a promising drug delivery system for ophthalmic applications.