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血浆和聚乙烯醇水凝胶中聚合物囊泡的钙黄绿素释放。

Calcein release from polymeric vesicles in blood plasma and PVA hydrogel.

作者信息

Litvinchuk S, Lu Z, Rigler P, Hirt T D, Meier W

机构信息

Department of Chemistry, University of Basel, Klingelbergstr. 80, 4056 Basel, Switzerland.

出版信息

Pharm Res. 2009 Jul;26(7):1711-7. doi: 10.1007/s11095-009-9881-7. Epub 2009 Apr 21.

Abstract

PURPOSE

The main goal of this study was to show the long-term stability of vesicles from poly(2-methyl oxazoline-block-polydimethylsiloxane-block poly(2-methyl oxazoline) (PMOXA-PDMS-PMOXA) in PBS, blood plasma and the feasibility to use these vesicles for drug release from PVA hydrogels.

METHODS

The vesicle formation properties and loading efficiency was evaluated using fluorescent dyes. The stability of the vesicles was evaluated in buffer at pH 7 at room temperature and in 50% blood plasma at 37 degrees C. The calcein loaded vesicles were dispersed in a UV crosslinked PVA hydrogel. The stability of the vesicles in the hydrogel was observed over one week, before the vesicles were ruptured with Triton X-100.

RESULTS

The vesicles are very stable in buffer, blood plasma, and the PVA hydrogel. In plasma 50% of the calcein is released in 48 h in the presence of sodium azide. The vesicles can be evenly dispersed in PVA and are stable. The release can be triggered and the calcein diffuses afterwards quickly throughout the gel.

CONCLUSION

Polymeric vesicles can be used as diffusion barrier in hydrogels for the controlled release of water soluble drugs.

摘要

目的

本研究的主要目标是展示聚(2-甲基恶唑啉-嵌段-聚二甲基硅氧烷-嵌段-聚(2-甲基恶唑啉))(PMOXA-PDMS-PMOXA)形成的囊泡在磷酸盐缓冲液(PBS)、血浆中的长期稳定性,以及使用这些囊泡从聚乙烯醇(PVA)水凝胶中释放药物的可行性。

方法

使用荧光染料评估囊泡的形成特性和负载效率。在室温下pH 7的缓冲液中以及37℃的50%血浆中评估囊泡的稳定性。将负载了钙黄绿素的囊泡分散在紫外线交联的PVA水凝胶中。在用曲拉通X-100使囊泡破裂之前,观察囊泡在水凝胶中一周的稳定性。

结果

囊泡在缓冲液、血浆和PVA水凝胶中非常稳定。在叠氮化钠存在的情况下,血浆中50%的钙黄绿素在48小时内释放。囊泡可以均匀地分散在PVA中且稳定。释放可以被触发,随后钙黄绿素迅速扩散到整个凝胶中。

结论

聚合物囊泡可作为水凝胶中的扩散屏障用于水溶性药物的控释。

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