Synthesis and In Vitro Evaluation of Defined HPMA Folate Conjugates: Influence of Aggregation on Folate Receptor (FR) Mediated Cellular Uptake

2010 ◽  
Vol 11 (9) ◽  
pp. 2274-2282 ◽  
Author(s):  
Matthias Barz ◽  
Fabiana Canal ◽  
Kaloian Koynov ◽  
R. Zentel ◽  
María J. Vicent
Keyword(s):  
Cellular Uptake ◽  
Folate Receptor ◽  
In Vitro Evaluation

In vitro evaluation of actively targetable superparamagnetic nanoparticles to the folate receptor positive cancer cells

2016 ◽  
Vol 69 ◽  
pp. 1147-1158 ◽  
Author(s):  
Rozita Nasiri ◽  
Javad Hamzehalipour Almaki ◽  
Ani Binti Idris ◽  
Fadzilah Adibah Abdul Majid ◽  
Mahtab Nasiri ◽  
...  
Keyword(s):  
Cancer Cells ◽  
Folate Receptor ◽  
Superparamagnetic Nanoparticles ◽  
In Vitro Evaluation

Dual-functional carbon dots–silver@zinc oxide nanocomposite: in vitro evaluation of cellular uptake and induction of apoptosis

2015 ◽  
Vol 3 (7) ◽  
pp. 1217-1229 ◽  
Author(s):  
Abhay Sachdev ◽  
Ishita Matai ◽  
P. Gopinath
Keyword(s):  
Zinc Oxide ◽  
Cellular Uptake ◽  
Carbon Dots ◽  
In Vitro Evaluation ◽  
Dual Functional ◽  
Induction Of Apoptosis

We report here the devleopment of novel CDs decorated on a silver–zinc oxide (CD–Ag@ZnO) nanocomposite (NC) consisting of highly fluorescent CDs and Ag@ZnO.

scholarly journals Folate Receptor-Targeting and Reactive Oxygen Species-Responsive Liposomal Formulation of Methotrexate for Treatment of Rheumatoid Arthritis

Pharmaceutics ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 582 ◽  
Author(s):  
Chen ◽  
Amerigos J.C. ◽  
Su ◽  
Guissi ◽  
Xiao ◽  
...  
Keyword(s):  
Rheumatoid Arthritis ◽  
Reactive Oxygen Species ◽  
Hydrogen Peroxide ◽  
Drug Release ◽  
Cellular Uptake ◽  
Folate Receptor ◽  
Oxygen Species ◽  
Activated Macrophages

Multifunctional nanomedicines with active targeting and stimuli-responsive drug release function utilizing pathophysiological features of the disease are regarded as an effective strategy for treatment of rheumatoid arthritis (RA). Under the inflammatory environment of RA, activated macrophages revealed increased expression of folate receptor and elevated intracellular reactive oxygen species (ROS) level. In this study, we successfully conjugated folate to polyethylene glycol 100 monostearate as film-forming material and further prepared methotrexate (MTX) and catalase (CAT) co-encapsulated liposomes, herein, shortened to FOL-MTX&CAT-L, that could actively target to activated macrophages. Thereafter, elevated intracellular hydrogen peroxide, the main source of ROS, diffused into liposomes and encapsulated CAT catalyzed the decomposition of hydrogen peroxide into oxygen and water. Continuous oxygen-generation inside liposomes would eventually disorganize its structure and release the encapsulated MTX. We characterized the in vitro drug release, cellular uptake and cytotoxicity studies as well as in vivo pharmacokinetics, biodistribution, therapeutic efficacy and safety studies of FOL-MTX&CAT-L. In vitro results revealed that FOL-MTX&CAT-L possessed sufficient ROS-sensitive drug release, displayed an improved cellular uptake through folate-mediated endocytosis and exhibited a higher cytotoxic effect on activated RAW264.7 cells. Moreover, in vivo results showed prolonged blood circulation time of PEGylated liposomes, enhanced accumulation of MTX in inflamed joints of collagen-induced arthritis (CIA) mice, reinforced therapeutic efficacy and minimal toxicity toward major organs. These results imply that FOL-MTX&CAT-L may be used as an effective nanomedicine system for RA treatment.

In Vitro and In Vivo Evaluation of Novel DTX-Loaded Multifunctional Heparin-Based Polymeric Micelles Targeting Folate Receptors and Endosomes

2020 ◽  
Vol 15 (4) ◽  
pp. 341-359
Author(s):  
Moloud Kazemi ◽  
Jaber Emami ◽  
Farshid Hasanzadeh ◽  
Mohsen Minaiyan ◽  
Mina Mirian ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Antitumor Activity ◽  
Cellular Uptake ◽  
Folate Receptor ◽  
Chemotherapeutic Agents ◽  
Water Soluble ◽  
Growth Monitoring ◽  
Tumor Bearing

Background: The development of biocompatible tumor-targeting delivery systems for anticancer agents is essential for efficacious cancer chemotherapy. Nanoparticles, as drug delivery cargoes for cancer therapy, are rapidly improving to overcome the limitations of conventional chemotherapeutic agents. Heparin–modified nanoparticles are currently being considered as one of the favorable carriers for the delivery of chemotherapeutics to cancer tissues. Objective: This study was aimed at evaluating the in vitro and in vivo antitumor activity of a novel targeted, pH-sensitive, heparin-based polymeric micelle loaded with the poorly water-soluble anticancer drug, docetaxel (DTX). The micelles could overcome the limited water solubility, non-specific distribution, and insufficient drug concentration in tumor tissues. Methods: DTX-loaded folate targeted micelles were prepared and evaluated for physicochemical properties, drug release, in vitro cellular uptake and cytotoxicity in folate receptor-positive and folate receptor-negative cells. Furthermore, the antitumor activity of DTX-loaded micelles was evaluated in the tumor-bearing mice. Some related patents were also studied in this research. Results: The heparin-based targeted micelles exhibited higher in vitro cellular uptake and cytotoxicity against folate receptor over-expressed cells due to the specific receptor-mediated endocytosis. DTX-loaded micelles displayed greater antitumor activity, higher anti-angiogenesis effects, and lower systemic toxicity compared with free DTX in a tumor-induced mice model as confirmed by tumor growth monitoring, immunohistochemical evaluation, and body weight shift. DTX-loaded targeting micelles demonstrated no considerable toxicity on major organs of tumor-bearing mice compared with free DTX. Conclusion: Our results indicated that DTX-loaded multifunctional heparin-based micelles with desirable antitumor activity and low toxicity possess great potential as a targeted drug delivery system in the treatment of cancer.

ENHANCING DELIVERY OF GADOLINIUM-LOADED, TARGETED NANOPARTICLES: EFFECT OF STERIC HINDRANCE ON FOLATE RECEPTOR-MEDIATED CELLULAR UPTAKE IN VITRO

2014 ◽  
Vol 30 (10) ◽  
pp. S217
Author(s):  
C.D. Sarsons ◽  
A.L. Doiron ◽  
H.I. Labouta ◽  
R.D. Shepherd ◽  
L.B. Andersen ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Steric Hindrance ◽  
Folate Receptor ◽  
Targeted Nanoparticles
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