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一种基于聚(乳酸-乙醇酸共聚物)微球和聚乙烯醇水凝胶纳米颗粒的异质结构复合材料,用于长期蛋白质药物递送。

A heterogeneously structured composite based on poly(lactic-co-glycolic acid) microspheres and poly(vinyl alcohol) hydrogel nanoparticles for long-term protein drug delivery.

作者信息

Wang N, Wu X S, Li J K

机构信息

Division of Pharmaceutics and Industrial Pharmacy, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, New York 11201, USA.

出版信息

Pharm Res. 1999 Sep;16(9):1430-5. doi: 10.1023/a:1018911411381.

Abstract

PURPOSE

To prepare a heterogeneously structured composite based on poly (lactic-co-glycolic acid) (PLGA) microspheres and poly(vinyl alcohol) (PVA) hydrogel nanoparticles for long-term protein drug delivery.

METHODS

A heterogeneously structured composite in the form of PLGA microspheres containing PVA nanoparticles was prepared and named as PLGA-PVA composite microspheres. A model protein drug, bovine serum albumin (BSA), was encapsulated in the PVA nanoparticles first. The BSA-containing PVA nanoparticles was then loaded in the PLGA microspheres by using a phase separation method. The protein-containing PLGA-PVA composite microspheres were characterized with regard to morphology, size and size distribution, BSA loading efficiency, in vitro BSA release, and BSA stability.

RESULTS

The protein-containing PLGA-PVA composite microspheres possessed spherical shape and nonporous surface. The PLGA-PVA composite microspheres had normal or Gaussian size distribution. The particle size ranged from 71.5 microm to 282.7 microm. The average diameter of the composite microspheres was 180 microm. The PLGA-PVA composite microspheres could release the protein (BSA) for two months. The protein stability study showed that BSA was protected during the composite microsphere preparation and stabilized inside the PLGA-PVA composite microspheres.

CONCLUSIONS

The protein-containing PLGA-PVA composite may be suitable for long-term protein drug delivery.

摘要

目的

制备基于聚(乳酸-乙醇酸共聚物)(PLGA)微球和聚乙烯醇(PVA)水凝胶纳米颗粒的异质结构复合材料,用于长效蛋白质药物递送。

方法

制备了一种含有PVA纳米颗粒的PLGA微球形式的异质结构复合材料,并将其命名为PLGA-PVA复合微球。首先将一种模型蛋白质药物牛血清白蛋白(BSA)包封在PVA纳米颗粒中。然后通过相分离法将含BSA的PVA纳米颗粒负载到PLGA微球中。对含蛋白质的PLGA-PVA复合微球进行形态、尺寸和尺寸分布、BSA负载效率、体外BSA释放以及BSA稳定性等方面的表征。

结果

含蛋白质的PLGA-PVA复合微球呈球形且表面无孔。PLGA-PVA复合微球具有正态或高斯尺寸分布。粒径范围为71.5微米至282.7微米。复合微球的平均直径为180微米。PLGA-PVA复合微球可释放蛋白质(BSA)达两个月。蛋白质稳定性研究表明,BSA在复合微球制备过程中得到保护,并在PLGA-PVA复合微球内部保持稳定。

结论

含蛋白质的PLGA-PVA复合材料可能适用于长效蛋白质药物递送。

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