Cellular uptake pathway and drug release characteristics of drug-encapsulated glycol chitosan nanoparticles in live cells

2010 ◽  
Vol 73 (9) ◽  
pp. 857-865 ◽  
Author(s):  
Sangjin Park ◽  
So Jin Lee ◽  
Hyunjin Chung ◽  
Songwook Her ◽  
Yongseok Choi ◽  
...  
2017 ◽  
Vol 37 (suppl_1) ◽  
Author(s):  
Richard Nho ◽  
Ji-Young Yhee

Idiopathic pulmonary fibrosis (IPF) is a fatal lung disease characterized by the presence of persistent fibrotic fibroblasts which have apoptosis-resistant properties in response to cell death inducing conditions including type I collagen rich matrix. Although selective targeting of fibrotic fibroblasts is a feasible concept for the effective therapy of IPF, no reliable drug carriers for targeting IPF fibroblasts have been reported. To address this limitation, biodegradable glycol chitosan nanoparticles (CNPs) were utilized as a carrier system for selective targeting of IPF patients-derived fibroblasts. Primary human lung fibroblasts from non-IPF and IPF patients (n = 6/group) were treated with various doses (50–450 μg/ml) of CNPs, and the subcellular localization of CNPs was examined as a function of time (3, 6, and 30 h) with a confocal microscope. CNPs were found in the cytoplasm of fibroblasts at 30 h post-treatment on tissue culture plates in the absence of collagen while the intracellular CNPs were clearly observed at 3 h post-treatment. Importantly, the cellular uptake of the CNPs was significantly increased at 3, 6, and 30 h post-treatment, when control and IPF fibroblasts were cultured on collagen, suggesting that fibroblast and collagen interaction promotes the CNP’s cellular internalization process. Clathrin-mediated endocytosis, caveolae-mediated endocytosis, and macropinocytosis were then suppressed by chlorpromazine (30 μM), genistein (100 μM), or amiloride (50 μM), respectively to elucidate the underlying mechanism of cellular uptake of CNPs in fibroblasts on the collagen matrix. Amiloride pre-treatment remarkably reduced the cellular internalization of CNPs in fibroblasts cultured on the collagen matrix. Furthermore, additional results also showed that sodium-hydrogen exchanger 1 (NHE-1) and PI3K play important roles in the increased cellular uptake of CNPs in the lung fibroblasts on the collagen matrix, suggesting that the subcellular localization of CNPs is largely due to the macropinocytosis. We propose that our approach can be a promising tactic for targeted delivery of therapeutics to the fibrotic fibroblasts residing in collagen matrix, which may lead to the improved treatment outcomes of this deadly disease.


2009 ◽  
Vol 135 (3) ◽  
pp. 259-267 ◽  
Author(s):  
Hae Yun Nam ◽  
Seok Min Kwon ◽  
Hyunjin Chung ◽  
Seung-Young Lee ◽  
Seung-Hae Kwon ◽  
...  

2019 ◽  
Vol 9 (2) ◽  
pp. 89-96
Author(s):  
Abbaraju Krishna Sailaja ◽  
Juveria Banu

Aim: The aim of this investigation was to develop and characterize naproxen loaded chitosan nanoparticles by emulsion interfacial reaction method. Methodology: For emulsion interfacial reaction method chitosan was used as a polymer. In this method, eight formulations were prepared by varying drug to polymer concentration. Discussion: Out of eight formulations prepared using emulsion interfacial reaction method EI8 formulation was found to be the best formulation. The drug content was observed as 94.4%, entrapment efficiency and loading capacity were found to be 87.5% and 75%, respectively. The mean particle diameter was measured as 324.6nm and the Zeta potential value was found to be -42.4mv. In vitro drug release data showed 97.2% of drug release rate sustained up to 12hrs. Conclusion: The results clearly reveal that EI8 formulation having the highest amount of drug was considered as the best formulation because of its small mean particle diameter, good entrapment efficiency, and stability.


2016 ◽  
Vol 7 (12) ◽  
pp. 2202-2208 ◽  
Author(s):  
Shuai Li ◽  
Zhouxiang Zhao ◽  
Wei Wu ◽  
Chunmei Ding ◽  
Jianshu Li

Two types of diblock copolymers are synthesized to construct dual pH-responsive micelles with a charge-conversional property for effective drug delivery.


2014 ◽  
Vol 2014 ◽  
pp. 1-8 ◽  
Author(s):  
Yixiang Shi ◽  
Ajun Wan ◽  
Yifei Shi ◽  
Yueyue Zhang ◽  
Yupeng Chen

The study of drug release dynamic is aiming at understanding the process that drugs release in human body and its dynamic characteristics. It is of great significance since these characteristics are closely related to the dose, dosage form, and effect of the drugs. The Noyes-Whitney function is used to represent how the solid material is dissolved into solution, and it is well used in study of drug dynamic. In this research, aspirin (acetylsalicylic acid (ASA)) has been encapsulated with different grades of chitosan (CS) varying in molecular weight (Mw) for the purpose of controlled release. The encapsulation was accomplished by ionic gelation technology based on assembly of positively charged chitosan and negatively charged sodium tripolyphosphate (TPP). The encapsulation efficiency, loading capacity, and drug release behavior of aspirin loaded chitosan nanoparticles (CS-NPs) were studied. It was found that the concentration of TPP and Aspirin, molecular weights of chitosan have important effect on the drug release patterns from chitosan nanoparticles. The results for simulation studies show that the Noyes-Whitney equation can be successfully used to interpret the drug release characteristics reflected by our experimental data.


Small ◽  
2017 ◽  
Vol 13 (27) ◽  
pp. 1700569 ◽  
Author(s):  
Peiyan Yuan ◽  
Xin Mao ◽  
Kok Chan Chong ◽  
Jiaqi Fu ◽  
Sijun Pan ◽  
...  

2012 ◽  
Vol 163 (2) ◽  
pp. 249-255 ◽  
Author(s):  
Jaehong Key ◽  
Christy Cooper ◽  
Ah Young Kim ◽  
Deepika Dhawan ◽  
Deborah W. Knapp ◽  
...  

2015 ◽  
Vol 12 (6) ◽  
pp. 1970-1979 ◽  
Author(s):  
Paula Pereira ◽  
Sílvia S. Pedrosa ◽  
Jennifer M. Wymant ◽  
Edward Sayers ◽  
Alexandra Correia ◽  
...  

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