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 Folic Acid-Functionalized Black Phosphorus Quantum Dots for Targeted Chemo-Photothermal Combination Cancer Therapy

Pharmaceutics ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 242 ◽  
Author(s):  
Miaomiao Luo ◽  
Wei Cheng ◽  
Xiaowei Zeng ◽  
Lin Mei ◽  
Gan Liu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Quantum Dots ◽  
Folic Acid ◽  
Drug Delivery System ◽  
Delivery System ◽  
Black Phosphorus ◽  
Model Drug ◽  
Black Phosphorus Quantum Dots

Due to the inherent limitations, single chemo or photothermal therapies (PTT) are always inefficient. The combination of chemotherapy and PTT for the treatment of cancers has attracted a great interest during the past few years. As a photothermal agent, black phosphorus quantum dots (BPQDs) possess an excellent extinction coefficient, high photothermal conversion efficacy, and good biocompatibility. Herein, we developed a photo- and pH-sensitive nanoparticle based on BPQDs for targeted chemo-photothermal therapy. Doxorubicin (DOX) was employed as a model drug. This nanosystem displayed outstanding photothermal performance both in vitro and in vivo. Folic acid conjugation onto the surface endowed this system an excellent tumor-targeting effect, which was demonstrated by the cellular targeting assay. The BPQDs-based drug delivery system exhibited pH- and photo-responsive release properties, which could reduce the potential damage to normal cells. The in vitro cell viability study showed a synergistic effect in suppressing cancer cell proliferation. Therefore, this BPQDs-based drug delivery system has substantial potential for future clinical applications.

scholarly journals Degradable Spirocyclic Polyacetal-Based Core-Amphiphilic Assemblies for Encapsulation and Release of Hydrophobic Cargo

Nanomaterials ◽  
2021 ◽  
Vol 11 (1) ◽  
pp. 161
Author(s):  
Brandon Andrade-Gagnon ◽  
Marilyne Bélanger-Bouliga ◽  
Phuong Trang Nguyen ◽  
Thi Hong Diep Nguyen ◽  
Steve Bourgault ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Cancer Therapy ◽  
Nile Red ◽  
Shell Structures ◽  
Acid Sensitivity ◽  
Cellular Assays ◽  
Click Polymerization ◽  
Intracellular Drug Delivery ◽  
Model Drug

Polymeric nanomaterials that degrade in acidic environments have gained considerable attention in nanomedicine for intracellular drug delivery and cancer therapy. Among various acid-degradable linkages, spirocyclic acetals have rarely been used to fabricate such vehicles. In addition to acid sensitivity, they benefit from conformational rigidity that is otherwise not attainable by their non-spirocyclic analogs. Herein, amphiphilic spirocyclic polyacetals are synthesized by Cu-catalyzed alkyne–azide “click” polymerization. Unlike conventional block copolymers, which often form core–shell structures, these polymers self-assemble to form core amphiphilic assemblies capable of encapsulating Nile red as a hydrophobic model drug. In vitro experiments show that while release from these materials can occur at neutral pH with preservation of their integrity, acidic pH accelerates efficient cargo release and leads to the complete degradation of assemblies. Moreover, cellular assays reveal that these materials are fully cytocompatible, interact with the plasma membrane, and can be internalized by cells, rendering them as potential candidates for cancer therapy and/or drug delivery.

Chitosan oligosaccharide copolymer micelles with double disulphide linkage in the backbone associated by H-bonding duplexes for targeted intracellular drug delivery

2015 ◽  
Vol 6 (9) ◽  
pp. 1454-1464 ◽  
Author(s):  
Qinglai Yang ◽  
Changyu He ◽  
Yuhong Xu ◽  
Bingya Liu ◽  
Zhifeng Shao ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Folic Acid ◽  
Block Copolymer ◽  
Chitosan Oligosaccharide ◽  
Intracellular Drug Delivery ◽  
Block Copolymer Micelles ◽  
Copolymer Micelles

Folic acid conjugated block copolymer micelles with H-bonding associated double disulphide linkage in the backbone were developed.

Synthesis and Drug Release from a PH/Temperature Sensitive Bead of Poly(N-Acryloylglycinate) and Alginate

2011 ◽  
Vol 117-119 ◽  
pp. 1227-1230
Author(s):  
Kui Lin Deng ◽  
Ting Gao ◽  
Yu Bo Gou ◽  
Wei Wang ◽  
Peng Fei Zhang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Temperature Sensitive ◽  
Polymer Content ◽  
In Vitro Drug Release ◽  
Buffer Solutions ◽  
Drug Delivery Carrier ◽  
Different Temperatures ◽  
Model Drug

In this paper, a new pH/temperature sensitive beads with core-shelled structure, composed of sodium alginate and poly(N-acryloylglycinate), were prepared using as drug delivery carrier. Selecting indomethacin as a model drug, in vitro drug release behaviors were investigated at different temperatures, phosphate buffer solutions (PBS) and polymer content. At pH=2.1, the release amount of indomethacin loaded in the beads was only 2.46% while this value approached to 95.23% in pH=7.4 PBS. In addition, the release rate of indomethacin at 37°C is much higher than at 18°C.

scholarly journals Folic Acid-Chitosan Conjugated Nanoparticles for Improving Tumor-Targeted Drug Delivery

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Huijuan Song ◽  
Chang Su ◽  
Wenyu Cui ◽  
Bingya Zhu ◽  
Liwei Liu ◽  
...  
Keyword(s):  
Folic Acid ◽  
Drug Release ◽  
Targeted Drug Delivery ◽  
Folate Receptor ◽  
Release Pattern ◽  
Monodisperse Nanoparticles ◽  
Targeting Delivery ◽  
Model Drug ◽  
Average Size

Objective. To prepare folic acid-chitosan conjugated nanoparticles (FA-CS NPs) and evaluate their targeting specificity on tumor cells.Methods. Chitosan (CS) NPs were prepared by ionic cross linking method, and folic acid (FA) was conjugated with CS NPs by electrostatic interaction. The properties of NPs were investigated, and doxorubicin hydrochloride (Dox) as a model drug was encapsulated for investigating drug release patternin vitro. The cytotoxicity and cellular uptake of FA-CS NPs were also investigated.Results. The results reveal that the obtained FA-CS NPs were monodisperse nanoparticles with suitable average size and positive surface charge. Dox was easily loaded into FA-CS NPs, and the release pattern showed a long and biphasic drug release. Noticeable phagocytosis effect was observed in the presence of rhodamine B-labeled FA-CSNPs when incubating with the folate receptor-positive SMMC-7221 cells.Conclusion. Compared with the unmodified CS NPs, FA-CS NPs showed much higher cell uptaking ability due to the known folate-receptor mediated endocytosis. FA-CS NPs provide a potential way to enhance the using efficiency of antitumor drug by folate receptor mediated targeting delivery.

scholarly journals Single Domain Antibodies as Carriers for Intracellular Drug Delivery: A Proof of Principle Study

Biomolecules ◽  
2021 ◽  
Vol 11 (7) ◽  
pp. 927
Author(s):  
Sebas D. Pronk ◽  
Erik Schooten ◽  
Jurgen Heinen ◽  
Esra Helfrich ◽  
Sabrina Oliveira ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Targeted Delivery ◽  
Single Domain ◽  
Drug Conjugates ◽  
Intracellular Drug Delivery ◽  
Internalization Rate ◽  
Single Domain Antibodies ◽  
Different Characteristics

Antibody-drug conjugates (ADCs) are currently used for the targeted delivery of drugs to diseased cells, but intracellular drug delivery and therefore efficacy may be suboptimal because of the large size, slow internalization and ineffective intracellular trafficking of the antibody. Using a phage display method selecting internalizing phages only, we developed internalizing single domain antibodies (sdAbs) with high binding affinity to rat PDGFRβ, a receptor involved in different types of diseases. We demonstrate that these constructs have different characteristics with respect to internalization rates but all traffic to lysosomes. To compare their efficacy in targeted drug delivery, we conjugated the sdAbs to a cytotoxic drug. The conjugates showed improved cytotoxicity correlating to their internalization speed. The efficacy of the conjugates was inhibited in the presence of vacuolin-1, an inhibitor of lysosomal maturation, suggesting lysosomal trafficking is needed for efficient drug release. In conclusion, sdAb constructs with different internalization rates can be designed against the same target, and sdAbs with a high internalization rate induce more cell killing than sdAbs with a lower internalization rate in vitro. Even though the overall efficacy should also be tested in vivo, sdAbs are particularly interesting formats to be explored to obtain different internalization rates.

Excipient effects on in vitro cytotoxicity of a novel paclitaxel self‐emulsifying drug delivery system

2003 ◽  
Vol 92 (12) ◽  
pp. 2411-2418 ◽  
Author(s):  
Neslihan Gursoy ◽  
Jean‐Sebastien Garrigue ◽  
Alain Razafindratsita ◽  
Gregory Lambert ◽  
Simon Benita ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
In Vitro Cytotoxicity

Polymeric/Inorganic Multifunctional Nanoparticles for Simultaneous Drug Delivery and Visualization

2010 ◽  
Vol 1257 ◽  
Author(s):  
Andrea Fornara ◽  
Alberto Recalenda ◽  
Jian Qin ◽  
Abhilash Sugunan ◽  
Fei Ye ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Fluorescence Microscopy ◽  
Contrast Agents ◽  
Gold Nanorods ◽  
In Vitro Cytotoxicity ◽  
In Vivo Studies ◽  
Multifunctional Nanoparticles ◽  
Cytotoxicity Studies

AbstractNanoparticles consisting of different biocompatible materials are attracting a lot of interest in the biomedical area as useful tools for drug delivery, photo-therapy and contrast enhancement agents in MRI, fluorescence and confocal microscopy. This work mainly focuses on the synthesis of polymeric/inorganic multifunctional nanoparticles (PIMN) based on biocompatible di-block copolymer poly(L,L-lactide-co-ethylene glycol) (PLLA-PEG) via an emulsion-evaporation method. Besides containing a hydrophobic drug (Indomethacin), these polymeric nanoparticles incorporate different visualization agents such as superparamagnetic iron oxide nanoparticles (SPION) and fluorescent Quantum Dots (QDs) that are used as contrast agents for Magnetic Resonance Imaging (MRI) and fluorescence microscopy together. Gold Nanorods are also incorporated in such nanostructures to allow simultaneous visualization and photodynamic therapy. MRI studies are performed with different loading of SPION into PIMN, showing an enhancement in T2 contrast superior to commercial contrast agents. Core-shell QDs absorption and emission spectra are recorded before and after their loading into PIMN. With these polymeric/inorganic multifunctional nanoparticles, both MRI visualization and confocal fluorescence microscopy studies can be performed. Gold nanorods are also synthesized and incorporated into PIMN without changing their longitudinal absorption peak usable for lased excitation and phototherapy. In-vitro cytotoxicity studies have also been performed to confirm the low cytotoxicity of PIMN for further in-vivo studies.

The Study of Albumin Release from Silica/Albumin as a Potential Drug Delivery Carrier

2014 ◽  
Vol 69 (5) ◽  
Author(s):  
Shafiyah Pondi ◽  
Jon Efendi ◽  
Ho Chin Siong ◽  
Lai Sin Yuan ◽  
Sheela Chandren ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Fumed Silica ◽  
In Vitro Release ◽  
Phosphate Buffer Solution ◽  
Buffer Solution ◽  
Solution Ph ◽  
Drug Delivery Carrier ◽  
High Interaction ◽  
Uv Visible

The drug-delivery field has been an attractive as well as challenging area for research. With the emerging of new formulated drugs and pharmaceutical compounds, development of good drug-delivery system (DDS) is crucially required. This study aims to utilize albumin as the drug template in silica/albumin/drug (S/A/D) system. Prior to designing this system, the interaction between silica and albumin was investigated. It is hypothesized that high interaction between silica and albumin may result in slower drug release over time, which is preferred for a good DDS. Silica and albumin (S/A) materials were prepared by using fumed silica and tetraethyl orthosilicate (TEOS) as the silica precursors. Three different S/A samples were prepared; fumed silica with albumin (FS/A), fumed silica with pre-treated albumin by sodium borohydrate (FS/A-N), and silica sol (TEOS) with albumin (SS/A). In-vitro release of albumin in phosphate buffer solution (pH 7) was carried out to examine the interaction between albumin and silica. The concentration of albumin was detected at 280 nm by UV-visible spectrophotometer. All samples were characterized by diffuse reflectance-UV-visible spectrophotometer (DR-UV), Fourier transform infrared spectrophotometer (FTIR) dan thermogravimetric-differential thermal analysis (TG-DTA). DR-UV results show that SS/A exhibited the lowest absorption intensity at 280 nm, which indicates better interaction between silica and albumin. This result was supported by the presence of Si-O stretching band of silanol at 952 cm-1 from the FTIR spectrum. Release study of albumin demonstrated that the release of albumin from SS/A was slowest compared to those of FS/A and FS/A-N. 

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