A poloxamer/chitosan in situ forming gel with prolonged retention time for ocular delivery
A poloxamer/chitosan in situ forming gel with prolonged retention time for ocular delivery
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DOI：
10.1016/j.ejpb.2010.02.011
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发表时间：
2010-06-01
影响因子：
4.9
通讯作者：
Vianna Lopez, Renata Fonseca
中科院分区：
文献类型：
--
作者：
Gratieri, Tais;Gelfuso, Guilherme Martins;Vianna Lopez, Renata Fonseca
本工作的目的是获得一种具有改进的机械和粘附性的眼部给药系统，该系统可以为眼部疾病的治疗提供更长的保留时间。为此，研制了一种由热固性聚合物聚环氧乙烷-聚环氧丙烷-聚环氧乙烷(PEO-PPO-PEO，泊洛沙姆)与粘附剂(壳聚糖)组合而成的原位凝胶。通过振荡流变学、质构和粘附性分析评价了不同的聚合物比例。在人体内进行了闪烁成像研究，以验证所开发的配方的保留时间。结果表明，壳聚糖改善了泊洛沙姆制剂的机械强度和质构性能，并以浓度依赖的方式赋予粘附性。泊洛沙姆/壳聚糖16：1配方滴眼10分钟后，50%-60%的凝胶仍与角膜表面接触，与传统溶液相比，保留量增加了四倍。因此，开发的配方具有足够的机械和感官性能，并与眼睛表面保持较长时间的接触。综上所述，泊洛沙姆/壳聚糖组成的原位凝胶是眼科疾病局部治疗的一种很有前途的工具。(C)2010爱思唯尔B.V.保留所有权利。
The aim of the present work was to obtain an ophthalmic delivery system with improved mechanical and mucoadhesive properties that could provide prolonged retention time for the treatment of ocular diseases. For this, an in situ forming gel comprised of the combination of a thermosetting polymer, poly (ethylene oxide)-poly (propylene oxide)-poly (ethylene oxide) (PEO-PPO-PEO, poloxamer), with a mucoadhesive agent (chitosan) was developed. Different polymer ratios were evaluated by oscillatory rheology, texture and mucoadhesive profiles. Scintigraphy studies in humans were conduced to verify the retention time of the formulations developed. The results showed that chitosan improves the mechanical strength and texture properties of poloxamer formulations and also confers mucoadhesive properties in a concentration-dependent manner. After a 10-min instillation of the poloxamer/chitosan 16:1 formulation in human eyes, 50-60% of the gel was still in contact with the cornea surface, which represents a fourfold increased retention in comparison with a conventional solution. Therefore, the developed formulation presented adequate mechanical and sensorial properties and remained in contact with the eye surface for a prolonged time. In conclusion, the in situ forming gel comprised of poloxamer/chitosan is a promising tool for the topical treatment of ocular diseases. (C) 2010 Elsevier B.V. All rights reserved.