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.

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.

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.

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.

Rational design and fabrication of a cancer-targeted chitosan nanocarrier to enhance selective cellular uptake and anticancer efficacy of selenocystine

2015 ◽  
Vol 3 (12) ◽  
pp. 2497-2504 ◽  
Author(s):  
Bo Yu ◽  
Hong Li ◽  
Jinhui Zhang ◽  
Wenjie Zheng ◽  
Tianfeng Chen
Keyword(s):  
Cellular Uptake ◽  
Rational Design ◽  
Anticancer Efficacy

A cancer-targeted chitosan nanocarrier has been rationally designed to enhance the selective cellular uptake and anticancer efficacy of selenocystine.

scholarly journals Folated Synperonic-Cholesteryl Hemisuccinate Polymeric Micelles for the Targeted Delivery of Docetaxel in Melanoma

2015 ◽  
Vol 2015 ◽  
pp. 1-17 ◽  
Author(s):  
Jaleh Varshosaz ◽  
Somayeh Taymouri ◽  
Farshid Hassanzadeh ◽  
Shaghayegh Haghjooy Javanmard ◽  
Mahboobeh Rostami
Keyword(s):  
Cellular Uptake ◽  
Targeted Delivery ◽  
Polymeric Micelles ◽  
Fluorescent Microscopy ◽  
Melanoma Tumor ◽  
Anticancer Efficacy ◽  
Solvent Type ◽  
Dialysis Method ◽  
Cholesteryl Hemisuccinate

The objective of this study was the synthesis of folic acid- (FA-) targeted polymeric micelles of Synperonic PE/F 127-cholesteryl hemisuccinate (PF127-Chol) for specific delivery of docetaxel (DTX). Targeted or nontargeted micelles loaded with DTX were prepared via dialysis method. The effects of processing variables on the physicochemical properties of targeted micelles were evaluated using a full factorial design. After the optimization of the polymer/drug ratio, the organic solvent type used for the preparation of the micelles, and the temperature of dialyzing medium, thein vitrocytotoxicity and cellular uptake of the optimized micelles were studied on B16F10 melanoma cells by flow cytometry and fluorescent microscopy. The anticancer efficacy of DTX-loaded FA-PF127-Chol was evaluated in mice bearing melanoma tumor. Optimized targeted micelles had the particle size of 171.3 nm, zeta potential of −7.8 mV, PDI of 0.325, and a high encapsulation efficiency that released the drug within 144 h. The MTT assay indicated that targeted micelles carrying DTX were significantly more cytotoxic, had higher cellular uptake, and reduced the tumor volume significantly more than the nontargeted micelles and the free drug. FA-PF127-Chol could be, therefore, a promising biomaterial for tumors overexpressing folate receptors.

Positive Surface Charge Enhances Selective Cellular Uptake and Anticancer Efficacy of Selenium Nanoparticles

2012 ◽  
Vol 51 (16) ◽  
pp. 8956-8963 ◽  
Author(s):  
Bo Yu ◽  
Yibo Zhang ◽  
Wenjie Zheng ◽  
Cundong Fan ◽  
Tianfeng Chen
Keyword(s):  
Surface Charge ◽  
Cellular Uptake ◽  
Selenium Nanoparticles ◽  
Anticancer Efficacy ◽  
Positive Surface Charge

Tumor-targeted co-delivery of mitomycin C and 10-hydroxycamptothecin via micellar nanocarriers for enhanced anticancer efficacy

RSC Advances ◽  
2015 ◽  
Vol 5 (29) ◽  
pp. 23022-23033 ◽  
Author(s):  
Jinyan Lin ◽  
Yang Li ◽  
Hongjie Wu ◽  
Xiangrui Yang ◽  
Yanxiu Li ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Mitomycin C ◽  
Cellular Uptake ◽  
Anticancer Efficacy ◽  
Tumor Accumulation

Polymer–lipid hybrid micelles co-delivered hydrophilic mitomycin C and hydrophobic 10-hydroxycamptothecin showed improved cellular uptake and cytotoxicity in vitro and enhanced tumor accumulation and antitumor activity in vivo.

scholarly journals Nanoformulations of α-Mangostin for Cancer Drug Delivery System

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 1993
Author(s):  
Lisna Meylina ◽  
Muchtaridi Muchtaridi ◽  
I Made Joni ◽  
Ahmed Fouad Abdelwahab Mohammed ◽  
Nasrul Wathoni
Keyword(s):  
Drug Delivery ◽  
Cellular Uptake ◽  
Polymeric Nanoparticles ◽  
Cancer Drug ◽  
Garcinia Mangostana ◽  
Active Constituent ◽  
Anticancer Efficacy ◽  
Anticancer Properties ◽  
Cancer Drug Delivery

Natural compounds are emerging as effective agents for the treatment of malignant diseases. The active constituent of α-mangostin from the pericarp of Garcinia mangostana L. has earned significant interest as a plant base compound with anticancer properties. Despite α-mangostin’s superior properties as an anticancer agent, its applications are limited due to its poor solubility and physicochemical stability, rapid systemic clearance, and low cellular uptake. Our review aimed to summarize and discuss the nanoparticle formulations of α-mangostin for cancer drug delivery systems from published papers recorded in Scopus, PubMed, and Google Scholar. We investigated various types of α-mangostin nanoformulations to improve its anticancer efficacy by improving bioavailability, cellular uptake, and localization to specific areas These nanoformulations include nanofibers, lipid carrier nanostructures, solid lipid nanoparticles, polymeric nanoparticles, nanomicelles, liposomes, and gold nanoparticles. Notably, polymeric nanoparticles and nanomicelles can increase the accumulation of α-mangostin into tumors and inhibit tumor growth in vivo. In addition, polymeric nanoparticles with the addition of target ligands can increase the cellular uptake of α-mangostin. In conclusion, nanoformulations of α-mangostin are a promising tool to enhance the cellular uptake, accumulation in cancer cells, and the efficacy of α-mangostin as a candidate for anticancer drugs.

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