Novel PEG-graft-PLA nanoparticles with the potential for encapsulation and controlled release of hydrophobic and hydrophilic medications in aqueous medium.

Novel PEG-graft-PLA nanoparticles with the potential for encapsulation and controlled release of hydrophobic and hydrophilic medications in aqueous medium.
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DOI:
10.2147/ijn.s19765
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发表时间:
2011
影响因子:
8
通讯作者:
Pan J
Pan J
中科院分区:
医学2区
文献类型:
--
作者:
Wang B;Jiang W;Yan H;Zhang X;Yang L;Deng L;Singh GK;Pan J

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这项研究涉及用一种聚合物包裹和控制释放疏水性和亲水性药物,这些药物作为治疗患病组织的联合疗法一起输送。为了验证我们的假设,即新型PEG-接枝-PLA(PEG,聚乙二醇; PLA,聚乳酸)由于其两亲性、电荷和接枝结构可以递送疏水和亲水药物,合成了具有非常低的临界胶束浓度的PEG-接枝-PLA(PEG的分子量= 1900)。一种亲水性(胰岛素)和一种疏水性(萘普生)模型药物在其在水溶液中的自组装期间被分别加载。所得纳米颗粒(NPs)分布窄且呈球形,平均粒径约为200 nm,zeta电位>-10 mV,包封率> 50%。纳米粒实现了胰岛素和萘普生的控制释放,分别超过24和160小时。具体地,从NP释放的胰岛素的生物活性得以保持。由于包封,无论是疏水性和亲水性药物,和纳米粒子获得类似的大小和zeta电位,以及保持负载蛋白的生物活性,我们期待的PEG-接枝-PLA纳米粒子在联合治疗中的应用。
This study concerns the encapsulation and controlled release of both hydrophobic and hydrophilic medications with one polymer, which are delivered together as a combined therapy to treat diseased tissue. To test our hypothesis that the novel PEG-graft-PLA (PEG, polyethylene glycol; PLA, polylactic acid) can deliver both the hydrophobic and hydrophilic medications on account of its amphiphility, charge, and graft structure, PEG-graft-PLA (molecular weight of PEG = 1900) with very low critical micelle concentration was synthesized. One hydrophilic (insulin) and one hydrophobic (naproxen) model medication were loaded in separately during its self-assembly in aqueous solution. The resulting nanoparticles (NPs) were narrowly distributed and spherical, with average particle size around 200 nm, zeta potential >−10 mV, and encapsulation efficiency >50%. The NPs realized controlled release of insulin and naproxen for over 24 and 160 hours, respectively. Specifically, the bioactivity of the insulin released from the NPs was maintained. Owing to encapsulation, both for hydrophobic and hydrophilic medicines, and NPs obtained with similar size and zeta potential, as well as maintenance of bioactivity of loaded protein, we expect the applications of PEG-graft-PLA NPs in combination therapy.
DOI: 10.1155/2009/363914
发表时间: 2009
影响因子: --
作者:
Kamrava M;Tsang KY;Madan RA;Kaushal A;Coleman CN;Gulley J
通讯作者: Gulley J