scholarly journals Effects of Polyethylene Glycol Spacer Length and Ligand Density on Folate Receptor Targeting of Liposomal Doxorubicin In Vitro

2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
Kumi Kawano ◽  
Yoshie Maitani
Keyword(s):  
Polyethylene Glycol ◽  
Liposomal Doxorubicin ◽  
Folate Receptor ◽  
In Vitro Cytotoxicity ◽  
Receptor Targeting ◽  
Spacer Length ◽  
Ligand Density ◽  
Molecular Weights ◽  
Folate Receptor Targeting

The folate receptor is an attractive target for selective tumor delivery of liposomal doxorubicin (DXR) because it is abundantly expressed in a large percentage of tumors. This study examined the effect of polyethylene glycol (PEG) spacer length and folate ligand density on the targeting ability of folate-modified liposomes. Liposomes were modified with folate-derivatized PEG-distearoylphosphatidylethanolamine with PEG molecular weights of 2000, 3400, or 5000. The association of DXR-loaded liposomes with KB cells, which overexpress the folate receptor, was evaluated by flow cytometry at various ratios of folate modification. A low ratio of folate modification with a sufficiently long PEG chain showed the highest folate receptor-mediated association with the cells, but did not show the highest in vitro cytotoxicity. DXR release from folate-modified liposomes in endosomes might be different. These findings will be useful for designing folate receptor-targeting carriers.

scholarly journals Multifunctional folate receptor-targeting and pH-responsive nanocarriers loaded with methotrexate for treatment of rheumatoid arthritis

2017 ◽  
Vol Volume 12 ◽  
pp. 6735-6746 ◽  
Author(s):  
Jinlong Zhao ◽  
Menghui Zhao ◽  
Changhui Yu ◽  
Xueyan Zhang ◽  
Jiaxin Liu ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Folate Receptor ◽  
Ph Responsive ◽  
Receptor Targeting ◽  
Folate Receptor Targeting

Radiosynthesis and Preclinical Evaluation of 3′-Aza-2′-[18F]fluorofolic Acid: A Novel PET Radiotracer for Folate Receptor Targeting

2013 ◽  
Vol 24 (2) ◽  
pp. 205-214 ◽  
Author(s):  
Thomas Betzel ◽  
Cristina Müller ◽  
Viola Groehn ◽  
Adrienne Müller ◽  
Josefine Reber ◽  
...  
Keyword(s):  
Folate Receptor ◽  
Receptor Targeting ◽  
Preclinical Evaluation ◽  
Folate Receptor Targeting

scholarly journals Tumor imaging using P866, a high-relaxivity gadolinium chelate designed for folate receptor targeting

2008 ◽  
Vol 60 (6) ◽  
pp. 1337-1346 ◽  
Author(s):  
Claire Corot ◽  
Philippe Robert ◽  
Eric Lancelot ◽  
Philippe Prigent ◽  
Sébastien Ballet ◽  
...  
Keyword(s):  
Tumor Imaging ◽  
Folate Receptor ◽  
Receptor Targeting ◽  
Gadolinium Chelate ◽  
High Relaxivity ◽  
Folate Receptor Targeting

scholarly journals Assessment of Intracellular Delivery Potential of Novel Sustainable Poly(δ-decalactone)-Based Micelles

Pharmaceutics ◽  
2020 ◽  
Vol 12 (8) ◽  
pp. 726
Author(s):  
Kuldeep Kumar Bansal ◽  
Ezgi Özliseli ◽  
Gaurav Kumar Saraogi ◽  
Jessica M. Rosenholm
Keyword(s):  
Drug Delivery ◽  
Folic Acid ◽  
Folate Receptor ◽  
In Vitro Cytotoxicity ◽  
Uptake Efficiency ◽  
Drug Delivery Carrier ◽  
Intracellular Drug Delivery ◽  
Copolymer Micelles ◽  
Model Drug

Biodegradable polymers from renewable resources have attracted much attention in recent years within the biomedical field. Lately, poly(δ-decalactone) based copolymer micelles have emerged as a potential drug delivery carrier material as a sustainable alternative to fossil-based polymers. However, their intracellular drug delivery potential is not yet investigated and therefore, in this work, we report on the synthesis and cellular uptake efficiency of poly(δ-decalactone) based micelles with or without a targeting ligand. Folic acid was chosen as a model targeting ligand and Rhodamine B as a fluorescent tracer to demonstrate the straightforward functionalisation aspect of copolymers. The synthesis of block copolymers was accomplished by a combination of facile ring-opening polymerisation and click chemistry to retain the structure uniformity. The presence of folic acid on the surface of micelles with diameter ~150 nm upsurge the uptake efficiency by 1.6 fold on folate receptor overexpressing MDA-MB-231 cells indicating the attainment of targeting using ligand functionality. The drug delivery capability of these carriers was ascertained by using docetaxel as a model drug, whereby the in vitro cytotoxicity of the drug was significantly increased after incorporation in micelles 48 h post incubation. We have also investigated the possible endocytosis route of non-targeted micelles and found that caveolae-mediated endocytosis was the preferred route of uptake. This work strengthens the prospect of using novel bio-based poly(δ-decalactone) micelles as efficient multifunctional drug delivery nanocarriers towards medical applications.

scholarly journals Probing Critical Physical Properties of Lactose-Polyethylene Glycol Microparticles in Pulmonary Delivery of Chitosan Nanoparticles

Pharmaceutics ◽  
2021 ◽  
Vol 13 (10) ◽  
pp. 1581
Author(s):  
Nasser Alhajj ◽  
Idanawati Naharudin ◽  
Paolo Colombo ◽  
Eride Quarta ◽  
Tin Wui Wong
Keyword(s):  
Polyethylene Glycol ◽  
Surface Area ◽  
Chitosan Nanoparticles ◽  
Pulmonary Delivery ◽  
Drying Method ◽  
Adsorption Phenomenon ◽  
Molecular Weights ◽  
Nanoparticle Agglomeration ◽  
Peripheral Lung

Pulmonary delivery of chitosan nanoparticles is met with nanoparticle agglomeration and exhalation. Admixing lactose-based microparticles (surface area-weighted diameter~5 μm) with nanoparticles mutually reduces particle agglomeration through surface adsorption phenomenon. Lactose-polyethylene glycol (PEG) microparticles with different sizes, morphologies and crystallinities were prepared by a spray drying method using varying PEG molecular weights and ethanol contents. The chitosan nanoparticles were similarly prepared. In vitro inhalation performance and peripheral lung deposition of chitosan nanoparticles were enhanced through co-blending with larger lactose-PEG microparticles with reduced specific surface area. These microparticles had reduced inter-microparticle interaction, thereby promoting microparticle–nanoparticle interaction and facilitating nanoparticles flow into peripheral lung.

scholarly journals Folate Receptor-Targeting Gold Nanoclusters as Fluorescence Enzyme Mimetic Nanoprobes for Tumor Molecular Colocalization Diagnosis

Theranostics ◽  
2014 ◽  
Vol 4 (2) ◽  
pp. 142-153 ◽  
Author(s):  
Dehong Hu ◽  
Zonghai Sheng ◽  
Shengtao Fang ◽  
Yanan Wang ◽  
Duyang Gao ◽  
...  
Keyword(s):  
Folate Receptor ◽  
Gold Nanoclusters ◽  
Receptor Targeting ◽  
Enzyme Mimetic ◽  
Folate Receptor Targeting
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