Self-assembling peptide–etoposide nanofibers for overcoming multidrug resistance

2020 ◽  
Vol 56 (97) ◽  
pp. 15321-15324
Author(s):  
Li-Song Zhang ◽  
Li-Xin Yan ◽  
Shan Gao ◽  
Hui Long ◽  
Zhen Xi ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Cellular Uptake ◽  
Water Solubility ◽  
Anticancer Efficacy ◽  
Self Assembling ◽  
Speed Up

Nap-GFFpYK-etoposide1/2 (NFE1/2) increase the water solubility of etoposide, speed up its cellular uptake and protect the etoposide from MDR-mediated efflux, thus significantly improving the anticancer efficacy.

Rationally designed curcumin laden glycopolymeric nanoparticles: Implications on cellular uptake and anticancer efficacy

2020 ◽  
Vol 137 (32) ◽  
pp. 48954
Author(s):  
N. Naga Malleswara Rao ◽  
Shipra Sharma ◽  
Krushna Kaduba Palodkar ◽  
Veera Sadhu ◽  
Manu Sharma ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Anticancer Efficacy

HYALURONIC ACID-DOCETAXEL CONJUGATE LOADED NANOLIPOSOMES FOR TARGETING TUMOR CELLS

2020 ◽  
pp. 88-99
Author(s):  
MULUNEH FROMSA SEIFU ◽  
LILA KANTA NATH ◽  
DEBASHIS DUTTA
Keyword(s):  
Hyaluronic Acid ◽  
Glial Cells ◽  
Cellular Uptake ◽  
Drug Loading ◽  
Microscopic Investigation ◽  
In Vitro Cytotoxicity ◽  
Scanning Calorimetry ◽  
Anticancer Efficacy ◽  
Apoptotic Effect

Objective: Docetaxel (DTX), a potent anticancer drug, is suffering from non-specificity and drug resistance as major limitations. In this investigation, we developed Hyaluronic acid (HA)-Docetaxel conjugate (HA-DTX) loaded nanoliposomes to target cancer cells via passive and active targeting approaches. Methods: HA-DTX was synthesized and characterized by UV-Visible spectrophotometry, FT-IR spectroscopy, 1H NMR spectroscopy, Differential scanning calorimetry and X-ray diffraction and then loaded into nanoliposomes (L-NLs) by thin-film hydration method. L-NLs were characterized physicochemically and evaluated for anticancer efficacy by in vitro cytotoxicity study in glioma cells (C6 glial cells); cellular uptake and apoptotic effect were investigated by fluorescence microscopy. Results: HA-DTX was successfully synthesized; L-NLs had an average size of 123.0±16.53 nm, polydispersity index of 0.246±0.01 and zeta potential of 44.4±6.79 mV. Also, L-NLs exhibited 90.54%±4.22 of drug loading efficiency and 2.68%±0.12 of drug loading, releasing about 57.72%±1.17 at pH 5.2 and only 14.14%±1.32 at pH 7.4 after 48 h. No significant change instability was observed after storage at 5 °C±3 °C as well as at 25 °C±2 °C/60% RH±5% RH for 6 mo. The cytotoxicity effect of L-NLs was higher by 10% that of marketed formulation at 10 µg/ml docetaxel concentration. Fluorescence microscopic investigation showed that more cellular uptake and apoptotic effect were observed in L-NLs treated C6 glial cells than in those treated with the marketed formulation. Conclusion: HA-DTX loaded nanoliposomes enabled docetaxel to target C6 glial cells with better efficacy and might be effective to treat glioma.

scholarly journals Comparison of Chemotherapeutic Activities of Rhodamine-Based GUMBOS and NanoGUMBOS

Molecules ◽  
2020 ◽  
Vol 25 (14) ◽  
pp. 3272
Author(s):  
Nimisha Bhattarai ◽  
Mi Chen ◽  
Rocío L. Pérez ◽  
Sudhir Ravula ◽  
Robert M. Strongin ◽  
...  
Keyword(s):  
Cellular Uptake ◽  
Water Solubility ◽  
High Water ◽  
Acid Group ◽  
Ester Group ◽  
Mitochondrial Targeting ◽  
Organic Salts ◽  
Nanoparticle Formation ◽  
Rhodamine Derivatives ◽  
High Water Solubility

Rhodamine derivatives have been widely investigated for their mitochondrial targeting and chemotherapeutic properties that result from their lipophilic cationic structures. In previous research, we have found that conversion of Rhodamine 6G into nanoGUMBOS, i.e., nanomaterials derived from a group of uniform materials based on organic salts (GUMBOS), led to selective chemotherapeutic toxicity for cancer cells over normal cells. Herein, we investigate the chemotherapeutic activity of GUMBOS derived from four different rhodamine derivatives, two bearing an ester group, i.e., Rhodamine 123 (R123) and SNAFR-5, and two bearing a carboxylic acid group, i.e., rhodamine 110 (R110) and rhodamine B (RB). In this study, we evaluate (1) relative hydrophobicity via octanol–water partition coefficients, (2) cytotoxicity, and (3) cellular uptake in order to evaluate possible structure–activity relationships between these different compounds. Intriguingly, we found that while GUMBOS derived from R123 and SNAFR-5 formed nanoGUMBOS in aqueous medium, no distinct nanoparticles are observed for RB and R110 GUMBOS. Further investigation revealed that the relatively high water solubility of R110 and RB GUMBOS hinders nanoparticle formation. Subsequently, while R123 and SNAFR-5 displayed selective chemotherapeutic toxicity similar to that of previously investigated R6G nanoGUMBOS, the R110 and RB GUMBOS were lacking in this property. Additionally, the chemotherapeutic toxicities of R123 and SNAFR-5 nanoGUMBOS were also significantly greater than R110 and RB GUMBOS. Observed results were consistent with decreased cellular uptake of R110 and RB as compared to R123 and SNAFR-5 compounds. Moreover, these results are also consistent with previous observations that suggest that nanoparticle formation is critical to the observed selective chemotherapeutic properties as well as the chemotherapeutic efficacy of rhodamine nanoGUMBOS.

scholarly journals 2-Deoxyglucose-Modified Folate Derivative: Self-Assembling Nanoparticle Able to Load Cisplatin

Molecules ◽  
2019 ◽  
Vol 24 (6) ◽  
pp. 1084 ◽  
Author(s):  
Shaoming Jin ◽  
Zhongyao Du ◽  
Pengjie Wang ◽  
Huiyuan Guo ◽  
Hao Zhang ◽  
...  
Keyword(s):  
Folic Acid ◽  
Self Assembly ◽  
Water Solubility ◽  
Pure Water ◽  
The Self ◽  
Molar Ratio ◽  
Antineoplastic Drugs ◽  
Self Assembling ◽  
Bonding Interaction ◽  
Nano Drug Delivery

Folic acid has been widely introduced into nano-drug delivery systems to give nanoparticle-targeted characteristics. However, the poor water solubility of folic acid may hinder the exploitation of its ability to load antineoplastic drugs. In the present study, we designed a new folate derivative (FA-2-DG) synthesized from folic acid and 2-Deoxyglucose (2-DG). The aim of this study was to evaluate the self-assembly characteristics of FA-2-DG, and its ability of loading cisplatin. The critical micelle concentration was 7.94 × 10−6 mol L−1. Fourier transform infrared spectroscopy indicated that hydrogen bonding interaction is a main driving force for the self–assembly of FA-2-DG. The particle was stable in pure water or 0.5% bovine serum albumin dispersions. By forming a coordination bond, the particles assembled from FA-2-DG can load cisplatin. The loading efficiency was maximal when the molar ratio of FA-2-DG to cisplatin was 2:1.

scholarly journals In situ real-time tracing of hierarchical targeting nanostructures in drug resistant tumors using diffuse fluorescence tomography

2019 ◽  
Vol 10 (34) ◽  
pp. 7878-7886 ◽  
Author(s):  
Qianqian Guo ◽  
Yangyun Wang ◽  
Limin Zhang ◽  
Peng Zhang ◽  
Yunjian Yu ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Real Time ◽  
Cellular Uptake ◽  
Circulation Time ◽  
Drug Resistant ◽  
Fluorescence Tomography ◽  
Enhanced Permeability And Retention ◽  
Tumor Tissues ◽  
Diffuse Fluorescence Tomography

Nanoparticles that respond to specific endogenous or exogenous stimuli in tumor tissues are actively being developed to address multidrug resistance owing to multiple advantages, including a prolonged circulation time, enhanced permeability and retention effect, and superior cellular uptake.

Role of cellular uptake in the reversal of multidrug resistance by PEG-b-PLA polymeric micelles

Biomaterials ◽  
2011 ◽  
Vol 32 (22) ◽  
pp. 5148-5157 ◽  
Author(s):  
Ling Xiao ◽  
Xiaoqin Xiong ◽  
Xiaohui Sun ◽  
Yanhong Zhu ◽  
Hao Yang ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Cellular Uptake ◽  
Polymeric Micelles

One-Step Self-Assembling Nanomicelles for Pirarubicin Delivery To Overcome Multidrug Resistance in Breast Cancer

2016 ◽  
Vol 13 (11) ◽  
pp. 3934-3944 ◽  
Author(s):  
Yanping Li ◽  
Rui Li ◽  
Qinhui Liu ◽  
Wenyao Li ◽  
Ting Zhang ◽  
...  
Keyword(s):  
Breast Cancer ◽  
Multidrug Resistance ◽  
Self Assembling ◽  
One Step

Design and Characterization of a Cancer-Targeted Drug Co-Delivery System Composed of Liposomes and Selenium Nanoparticles

2020 ◽  
Vol 20 (9) ◽  
pp. 5295-5304
Author(s):  
Guangshan Xuan ◽  
Min Zhang ◽  
Yang Chen ◽  
Shan Huang ◽  
Imshik Lee
Keyword(s):  
Folic Acid ◽  
Zeta Potential ◽  
Cellular Uptake ◽  
Delivery System ◽  
Mtt Assay ◽  
Hela Cells ◽  
Selenium Nanoparticles ◽  
Spherical Particles ◽  
Anticancer Efficacy ◽  
Targeted Drug

A drug co-delivery system composed of selenium nanoparticles (SeNPs) has attracted increasing interest due to its ability to increase the anticancer efficacy against multidrug-resistant cancer cells. In this study, a cancer-targeted drug co-delivery system combining fluorescein-loaded liposomes and SeNPs was designed and evaluated. The system was developed by coating SeNPs and fluorescein-loaded liposomes with folic acid-chitosan conjugates (FA-CS-SeNPs-Lips). Folic acid-chitosan conjugates (FA-CS) were synthesized by coupling folic acid (FA) with chitosan (CS), and the structure was confirmed by performing Fourier transform spectroscopy (FT-IR) and nuclear magnetic resonance (1H-NMR) spectroscopy. Dynamic light scattering (DLS) measurements and transmission electron microscopy (TEM) were used to evaluate the particle size, Zeta potential, and morphology. The cytotoxicity of SeNPs coated with FA-CS conjugates (FA-CS-SeNPs) toward A549 cells and HeLa cells was examined using the MTT assay. The cancer-targeting ability and drug release behaviors were evaluated in vitro by measuring the cellular uptake of fluorescein and dialysis, respectively. The FA-CS-SeNPs were uniform, spherical particles with a ~50 nm diameter and high positive Zeta potential (+57.7 mV). Based on the results of the MTT assay, FA-CS-SeNPs displayed a more significant increase in the anticancer efficacy in HeLa cells than CS-SeNPs. FA-CS-SeNPs-Lips not only slowly released fluorescein but also specifically targeted HeLa cells through selective binding between folate and folate receptors to increase the cellular uptake of fluorescein.

scholarly journals An 8-hydroxyquinoline–proline hybrid with multidrug resistance reversal activity and the solution chemistry of its half-sandwich organometallic Ru and Rh complexes

2020 ◽  
Vol 49 (23) ◽  
pp. 7977-7992
Author(s):  
János P. Mészáros ◽  
Jelena M. Poljarević ◽  
István Szatmári ◽  
Oszkár Csuvik ◽  
Ferenc Fülöp ◽  
...  
Keyword(s):  
Multidrug Resistance ◽  
Complex Formation ◽  
Anticancer Activity ◽  
Cellular Uptake ◽  
Solution Chemistry ◽  
Synthesis And Characterization ◽  
Resistance Reversal ◽  
Organometallic Cations ◽  
Half Sandwich

Synthesis and characterization of an 8-hydroxyquinoline–proline hybrid, and its complex formation with half-sandwich organometallic cations: aqueous chemistry, lipophilicity, cellular uptake and anticancer activity.

Quinolin-8-yloxy-substituted zinc(II) phthalocyanines for enhanced in vitro photodynamic therapy

2018 ◽  
Vol 22 (09n10) ◽  
pp. 807-813 ◽  
Author(s):  
Juanjuan Chen ◽  
Yuting Fang ◽  
Hong Liu ◽  
Naisheng Chen ◽  
Shengping Chen ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Singlet Oxygen ◽  
Clinical Application ◽  
Cellular Uptake ◽  
Culture Medium ◽  
Anticancer Agent ◽  
Quantum Yields ◽  
Anticancer Efficacy ◽  
Self Aggregation

Photodynamic therapy (PDT) is an innovative and promising modality to treat various tumors. In this study, two novel zinc(II) phthalocyanines substituted with quinolin-8-yloxy groups at the [Formula: see text]-position, namely mono(quinolin-8-yloxy) zinc(II) phthalocyanine (ZnPc-Q1) and tetra(quinolin-8-yloxy) zinc(II) phthalocyanine (ZnPc-Q4), have been synthesized and fully characterized. With quinolin-8-yloxy, these two phthalocyanines exhibit less self-aggregation in DMF and culture medium, high singlet oxygen quantum yields, mitochondria localization and high photodynamic activities (IC[Formula: see text] values as low as 2 nM). Compared to ZnPc-Q4, ZnPc-Q1 exhibits higher cellular uptake and lower IC[Formula: see text] values. Benefitting from its higher anticancer efficacy and lack of isomers, ZnPc-Q1 is a highly promising anticancer agent in clinical application.

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