scholarly journals PEGylated Doxorubicin Prodrug-Forming Reduction-Sensitive Micelles With High Drug Loading and Improved Anticancer Therapy

2021 ◽  
Vol 9 ◽  
Author(s):  
Dongdong Wang ◽  
Xiaoyi Zhang ◽  
Bingbing Xu
Keyword(s):  
Drug Delivery Systems ◽  
Drug Loading ◽  
Tumor Therapy ◽  
Anticancer Therapy ◽  
Release Behavior ◽  
Two Phase ◽  
Extracellular Milieu ◽  
Drug Release Behavior ◽  
Reduction Potentials ◽  
High Drug Loading

Significant efforts on the design and development of advanced drug delivery systems for targeted cancer chemotherapy continue to be a major challenge. Here, we reported a kind of reduction-responsive PEGylated doxorubicin (DOX) prodrug via the simple esterification and amidation reactions, which self-assembled into the biodegradable micelles in solutions. Since there was an obvious difference in the reduction potentials between the oxidizing extracellular milieu and the reducing intracellular fluids, these PEG–disulfide–DOX micelles were localized intracellularly and degraded rapidly by the stimulus to release the drugs once reaching the targeted tumors, which obviously enhanced the therapeutic efficacy with low side effects. Moreover, these reduction-sensitive micelles could also physically encapsulate the free DOX drug into the polymeric cargo, exhibiting a two-phase programmed drug release behavior. Consequently, it showed a potential to develop an intelligent and multifunctional chemotherapeutic payload transporter for the effective tumor therapy.

scholarly journals Synthesis and compatibility evaluation of versatile mesoporous silica nanoparticles with red blood cells: an overview

RSC Advances ◽  
2019 ◽  
Vol 9 (61) ◽  
pp. 35566-35578 ◽  
Author(s):  
Subhankar Mukhopadhyay ◽  
Hanitrarimalala Veroniaina ◽  
Tadious Chimombe ◽  
Lidong Han ◽  
Wu Zhenghong ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Mesoporous Silica ◽  
Silica Nanoparticles ◽  
Blood Cells ◽  
Drug Delivery Systems ◽  
Mesoporous Silica Nanoparticles ◽  
Drug Loading ◽  
Loading Capacity ◽  
High Drug ◽  
High Drug Loading

Protean mesoporous silica nanoparticles are propitious candidates over decades for nanoscale drug delivery systems due to their unique characteristics, including changeable pore size, mesoporosity, high drug loading capacity and biodegradability.

Dialysis-derived urchin-like supramolecular assembly of tannic acid and paclitaxel with high porosity

Nanoscale ◽  
2021 ◽  
Author(s):  
Jiyeon Kim ◽  
Chanuk Choi ◽  
Seonki Hong
Keyword(s):  
Drug Delivery ◽  
Tannic Acid ◽  
Drug Delivery Systems ◽  
Drug Loading ◽  
Supramolecular Assembly ◽  
High Porosity ◽  
Active Pharmaceutical Ingredients ◽  
High Drug ◽  
Pharmaceutical Ingredients ◽  
High Drug Loading

Co-crystallization of active pharmaceutical ingredients (APIs) with pharmaceutically acceptable additives has emerged as an alternative to current drug delivery systems for hydrophobic drugs, due to the high drug loading efficiency....

Application of Carbon Nanotubes as Drug Delivery System for Anticancer Therapy

2020 ◽  
pp. 29-36
Author(s):  
Sabita Shrestha
Keyword(s):  
Carbon Nanotubes ◽  
Drug Delivery ◽  
Drug Loading ◽  
High Surface ◽  
High Surface Area ◽  
Anticancer Therapy ◽  
Loading Capacity ◽  
One Dimensional ◽  
Nano Medicine ◽  
High Drug Loading

Carbon nanotubes are one-dimensional allotrope of carbon having high aspect ratio, high surface area, and excellent material properties. It has applications in many fields such as catalyst, nano-electronics, field emission, nano medicine, solar cells, energy storage etc. Drug delivery is one of the important applications of carbon nanotubes because of its unique properties such as high drug loading capacity, thermal ablation, ease of cellular uptake. This article briefly overviews the different steps in drug delivery and anticancer therapy such as mechanism of drug loading, transportation, distribution, metabolism and finally excretion of drug.

scholarly journals Schiff-Linked PEGylated Doxorubicin Prodrug Forming pH-Responsive Nanoparticles With High Drug Loading and Effective Anticancer Therapy

2021 ◽  
Vol 11 ◽  
Author(s):  
Jian Song ◽  
Bingbing Xu ◽  
Hui Yao ◽  
Xiaofang Lu ◽  
Yang Tan ◽  
...  
Keyword(s):  
Drug Release ◽  
Tumor Cells ◽  
Drug Loading ◽  
Drug Carriers ◽  
Anticancer Therapy ◽  
Therapeutic Effects ◽  
Ph Responsive ◽  
High Drug ◽  
High Drug Loading ◽  
Mcf 7

Developing efficacious drug delivery systems for targeted cancer chemotherapy remains a major challenge. Here we demonstrated a kind of pH-responsive PEGylated doxorubicin (DOX) prodrug via the effective esterification and Schiff base reactions, which could self-assemble into the biodegradable micelles in aqueous solutions. Owing to low pH values inside the tumor cells, these PEG-Schiff-DOX nanoparticles exhibited high drug loading ability and pH-responsive drug release behavior within the tumor cells or tissues upon changes in physical and chemical environments, but they displayed good stability at physiological conditions for a long period. CCK-8 assay showed that these PEGylated DOX prodrugs had a similar cytotoxicity to the MCF-7 tumor cells as the free DOX drug. Moreover, this kind of nanoparticle could also encapsulate small DOX drugs with high drug loading, sufficient drug release and enhanced therapeutic effects toward MCF-7 cells, which will be benefited for developing more drug carriers with desirable functions for clinical anticancer therapy.

scholarly journals Formulation, characterization and evaluation of morusin loaded niosomes for potentiation of anticancer therapy

RSC Advances ◽  
2018 ◽  
Vol 8 (57) ◽  
pp. 32621-32636 ◽  
Author(s):  
Srishti Agarwal ◽  
M. Sheikh Mohamed ◽  
Sreejith Raveendran ◽  
Ankit K. Rochani ◽  
Toru Maekawa ◽  
...  
Keyword(s):  
Sustained Release ◽  
Cell Lines ◽  
Cancer Cell ◽  
Therapeutic Efficacy ◽  
Drug Loading ◽  
Anticancer Therapy ◽  
Cancer Cell Lines ◽  
High Drug ◽  
High Drug Loading

Highly cytocompatible morusin-loaded niosomes were synthesized showing high drug loading and encapsulation efficiencies with sustained release of the drug. Enhanced therapeutic efficacy was observed against 4 different cancer cell lines.

scholarly journals Design of Non-Haemolytic Nanoemulsions for Intravenous Administration of Hydrophobic APIs

Pharmaceutics ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 1141
Author(s):  
Line Séguy ◽  
Anne-Claire Groo ◽  
Didier Goux ◽  
Didier Hennequin ◽  
Aurélie Malzert-Fréon
Keyword(s):  
Intravenous Administration ◽  
Drug Delivery Systems ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Medium Chain Triglyceride ◽  
Storage Conditions ◽  
Ternary Diagram ◽  
Preclinical Development ◽  
High Drug Loading

Among advanced formulation strategies, nanoemulsions are considered useful drug-delivery systems allowing to improve the solubility and the bioavailability of lipophilic drugs. To select safe excipients for nanoemulsion formulation and to discard any haemolytic potential, an in vitro miniaturized test was performed on human whole blood. From haemolysis results obtained on eighteen of the most commonly used excipients, a medium chain triglyceride, a surfactant, and a solubilizer were selected for formulation assays. Based on a design of experiments and a ternary diagram, the feasibility of nanoemulsions was determined. The composition was defined to produce monodisperse nanodroplets with a diameter of either 50 or 120 nm, and their physicochemical properties were optimized to be suitable for intravenous administration. These nanoemulsions, stable over 21 days in storage conditions, were shown to be able to encapsulate with high encapsulation efficiency and high drug loading, up to 16% (w/w), two water practically insoluble drug models: ibuprofen and fenofibrate. Both drugs may be released according to a modulable profile in sink conditions. Such nanoemulsions appear as a very promising and attractive strategy for the efficient early preclinical development of hydrophobic drugs.

scholarly journals Galactose Oxidase Enables Modular Assembly of Conjugates from Native Antibodies with High Drug-to-Antibody Ratios

2021 ◽  
Author(s):  
Antonio Angelastro ◽  
Alexey Barkhanskiy ◽  
Ashley P. Mattey ◽  
Edward G. Pallister ◽  
Reynard Spiess ◽  
...  
Keyword(s):  
Drug Loading ◽  
Anticancer Therapy ◽  
Galactose Oxidase ◽  
Reaction Conditions ◽  
Modular Assembly ◽  
High Drug ◽  
Drug Conjugates ◽  
Antibody Conjugates ◽  
High Drug Loading ◽  
Antibody Drug

The potential of antibody conjugates with high drug loading in anticancer therapy has recently been highlighted by the approval of Trastuzumab deruxtecan and Sacituzumab govitecan. These biopharmaceutical approaches have spurred interest in bioconjugation strategies with high and defined degrees antibody-to-drug (DAR) ratios, in particular on native antibodies. Here we report a glycoengineering methodology to generate antibody drug conjugates with DAR of up to eight, by combining highly selective enzymatic galactosylation and oxidation with biorthogonal tandem Knoevenagel-Michael addition chemistry. This three step approach offers a selective route to conjugates from native antibodies with high drug loading, and thus illustrates how biocatalysis can be used for the generation of biopharmaceuticals using mild reaction conditions.

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