Department of Pharmaceutical Sciences Eugene Applebaum College of Pharmacy & Health Sciences, Wayne State University, Detroit, Michigan 48201, USA.
Pharm Res. 2013 Feb;30(2):424-34. doi: 10.1007/s11095-012-0884-4. Epub 2012 Sep 20.
Pulmonary administration of polymeric nanoparticle drug delivery systems is of great interest for both systemic and local therapies. However, little is understood about the relationship of particle size and pulmonary absorption. We investigated uptake and biodistribution of polystyrene nanoparticles (PN) of 50 nm, 100 nm, 250 nm, and 900 nm diameters in mice following administration to lungs via pharyngeal aspiration.
The amount of PN in tissues was analyzed by gel permeation chromatography (GPC).
At 1 h, larger diameter PN (250 nm and 900 nm) had the highest total uptake at around 15% of administered dose, whereas the smaller diameter PN (50 nm and 100 nm) had uptake of only 5-6%. However, at 3 h, the 50 nm PN had the highest total uptake at 24.4%. For each size tested, the highest nanoparticle deposition was observed in the lymph nodes (LN) as compared to other tissues accounting for a total of about 35-50% of absorbed nanoparticles.
PN size impacts the rate and extent of uptake from lungs and, further, the extent of LN deposition. The extent of uptake and lymph distribution of the model, non-degradable PN lends potential to pulmonary administered, biodegradable polymeric nanoparticles for delivery of therapeutics to regional lymph nodes.
聚合物纳米颗粒药物传递系统经肺部给药,无论是用于全身治疗还是局部治疗,都具有很大的吸引力。然而,人们对粒径与肺部吸收之间的关系知之甚少。我们通过经口咽吸入的方式将粒径分别为 50nm、100nm、250nm 和 900nm 的聚苯乙烯纳米颗粒(PN)递送至肺部,研究了这些纳米颗粒在小鼠体内的摄取和生物分布情况。
通过凝胶渗透色谱(GPC)分析组织中的 PN 含量。
在 1 小时时,较大直径的 PN(250nm 和 900nm)的总摄取量最高,约为给药剂量的 15%,而较小直径的 PN(50nm 和 100nm)的摄取量仅为 5-6%。然而,在 3 小时时,50nm PN 的总摄取量最高,达到 24.4%。对于每种测试的尺寸,在淋巴结(LN)中观察到最高的纳米颗粒沉积,与其他组织相比,占吸收的纳米颗粒总量的约 35-50%。
PN 的尺寸影响从肺部摄取的速率和程度,以及 LN 沉积的程度。该模型非降解性 PN 的摄取和淋巴分布程度为可生物降解的聚合物纳米颗粒经肺部给药用于向区域淋巴结递送电疗药物提供了潜力。