In vitro evaluation of 5-aminolevulinic acid (ALA) loaded PLGA nanoparticles.
In vitro evaluation of 5-aminolevulinic acid (ALA) loaded PLGA nanoparticles.
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DOI：
10.2147/ijn.s45821
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发表时间：
2013
影响因子：
8
通讯作者：
Wang H
中科院分区：
文献类型：
--
作者：
Shi L;Wang X;Zhao F;Luan H;Tu Q;Huang Z;Wang H;Wang H
5-氨基乙酰丙酸（ALA）是一种用于局部光动力治疗的前药。局部ALA的有效性可能受到其生物利用度的限制。本研究的目的是利用聚乳酸-羟基乙酸（PLGA）纳米颗粒（NPs）开发一种新的ALA递送方法。采用改进的双乳液溶剂蒸发法制备ALA负载PLGA NPs （ALA PLGA NPs）。研究了ALA PLGA NPs的特性、摄取、原卟啉IX荧光动力学和对人皮肤鳞状细胞癌细胞的细胞毒性。球形ALA PLGA NPs的平均粒径为65.6 nm±26 nm，多分散性指数为0.62。包封率为65.8%±7.2%，ALA装载量为0.62%±0.27%。当ALA分散在PLGA NPs中时，它变成无定形相。ALA PLGA NPs可被鳞状细胞癌细胞吸收并定位于细胞质中。原卟啉IX荧光动力学和3-[4,5-二甲基噻唑-2-基]-2,5-二苯基溴化四唑测定表明，ALA PLGA NPs比相同浓度的游离ALA更有效。PLGA NPs为局部ALA光动力治疗皮肤鳞状细胞癌提供了一种有前途的ALA递送策略。
5-Aminolevulinic acid (ALA) is a prodrug for topical photodynamic therapy. The effectiveness of topical ALA can be limited by its bioavailability. The aim of this study was to develop a novel ALA delivery approach using poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs). A modified double emulsion solvent evaporation method was used to prepare ALA loaded PLGA NPs (ALA PLGA NPs). The characteristics, uptake, protoporphyrin IX fluorescence kinetics, and cytotoxicity of ALA PLGA NPs toward a human skin squamous cell carcinoma cell line were examined. The mean particle size of spherical ALA PLGA NPs was 65.6 nm ± 26 nm with a polydispersity index of 0.62. The encapsulation efficiency was 65.8% ± 7.2% and ALA loading capacity was 0.62% ± 0.27%. When ALA was dispersed in PLGA NPs, it turned into an amorphous phase. ALA PLGA NPs could be taken up by squamous cell carcinoma cells and localized in the cytoplasm. The protoporphyrin IX fluorescence kinetics and 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay showed that ALA PLGA NPs were more effective than free ALA of the same concentration. PLGA NPs provide a promising ALA delivery strategy for topical ALA-photodynamic therapy of skin squamous cell carcinoma.