The use of pH-sensitive functional selenium nanoparticles shows enhanced in vivo VEGF-siRNA silencing and fluorescence imaging

Nanoscale ◽  
2014 ◽  
Vol 6 (15) ◽  
pp. 9279-9292 ◽  
Author(s):  
Qianqian Yu ◽  
Yanan Liu ◽  
Chengwen Cao ◽  
Fangling Le ◽  
Xiuying Qin ◽  
...  
Keyword(s):  
Side Effects ◽  
Gene Silencing ◽  
Fluorescence Imaging ◽  
Delivery System ◽  
Ph Sensitive ◽  
Selenium Nanoparticles ◽  
Vegf Gene ◽  
Sirna Silencing

The pH-sensitive delivery system G2/PAH-Cit/SeNPs@siRNA enhances anti-tumor effects through VEGF gene silencing and reduces angiogenesis, with no side effects in organs.

scholarly journals Carboxymethyl cellulose-grafted graphene oxide for efficient antitumor drug delivery

2018 ◽  
Vol 7 (4) ◽  
pp. 291-301 ◽  
Author(s):  
Zepeng Jiao ◽  
Bin Zhang ◽  
Chunya Li ◽  
Weicong Kuang ◽  
Jingxian Zhang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Graphene Oxide ◽  
Drug Delivery System ◽  
Delivery System ◽  
Carboxymethyl Cellulose ◽  
Drug Carrier ◽  
Controlled Drug Release ◽  
Ph Sensitive ◽  
Tumor Growth Inhibition

Abstract A drug delivery system based on carboxymethyl cellulose-grafted graphene oxide loaded by methotrexate (MTX/CMC-GO) with pH-sensitive and controlled drug-release properties was developed in this work. CMC was grafted on graphene oxide by ethylenediamine through hydrothermal treatment. CMC serves as a pH-sensitive trigger, while CMC-GO serves as a drug-carrying vehicle due to the curved layer and large plain surface. Different amounts of drugs could be loaded into CMC-GO nanocarriers by control of the original amount of drug/carrier ratios. Additionally, low cytotoxicity against NIH-3T3 cells and low in vivo toxicity was observed. In vivo tumor growth inhibition assays showed that MTX/CMC-GO demonstrated superior antitumor activity than free MTX against HT-29 cells. Moreover, prolonged survival time of mice was observed after MTX/CMC-GO administration. The MTX/CMC-GO drug delivery system has a great potential in colon cancer therapy.

In vitro and in vivo chemo-phototherapy of magnetic TiO2 drug delivery system formed by pH-sensitive coordination bond

2016 ◽  
Vol 31 (4) ◽  
pp. 568-581 ◽  
Author(s):  
Huijuan Zhang ◽  
Yandan Ji ◽  
Qianqian Chen ◽  
Xing Zhu ◽  
Xiaoge Zhang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ph Sensitive ◽  
Coordination Bond

A pH-sensitive fusogenic peptide facilitates endosomal escape and greatly enhances the gene silencing of siRNA-containing nanoparticles in vitro and in vivo

2009 ◽  
Vol 139 (2) ◽  
pp. 127-132 ◽  
Author(s):  
Hiroto Hatakeyama ◽  
Erika Ito ◽  
Hidetaka Akita ◽  
Motoi Oishi ◽  
Yukio Nagasaki ◽  
...  
Keyword(s):  
Gene Silencing ◽  
Ph Sensitive ◽  
Endosomal Escape

scholarly journals Improved Safety and Anti-Glioblastoma Efficacy of CAT3-Encapsulated SMEDDS through Metabolism Modification

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 484
Author(s):  
Hongliang Wang ◽  
Lin Li ◽  
Jun Ye ◽  
Wujun Dong ◽  
Xing Zhang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Gastrointestinal Tract ◽  
Side Effects ◽  
Drug Delivery System ◽  
Delivery System ◽  
Lymphatic Transport ◽  
Pharmacokinetic Parameters ◽  
Gastrointestinal Side Effects ◽  
The Brain

13a-(S)-3-pivaloyloxyl-6,7-dimethoxyphenanthro(9,10-b)-indolizidine (CAT3) is a novel oral anti-glioma pro-drug with a potent anti-tumor effect against temozolomide-resistant glioma. 13a(S)-3-hydroxyl-6,7-dimethoxyphenanthro(9,10-b)-indolizidine (PF403) is the active in vivo lipase degradation metabolite of CAT3. Both CAT3 and PF403 can penetrate the blood–brain barrier to cause an anti-glioma effect. However, PF403, which is produced in the gastrointestinal tract and plasma, causes significant gastrointestinal side effects, limiting the clinical application of CAT3. The objective of this paper was to propose a metabolism modification for CAT3 using a self-microemulsifying drug delivery system (SMEDDS), in order to reduce the generation of PF403 in the gastrointestinal tract and plasma, as well as increase the bioavailability of CAT3 in vivo and the amount of anti-tumor substances in the brain. Thus, a CAT3-loaded self-microemulsifying drug delivery system (CAT3-SMEDDS) was prepared, and its physicochemical characterization was systematically carried out. Next, the pharmacokinetic parameters of CAT3 and its metabolite in the rats’ plasma and brain were measured. Furthermore, the in vivo anti-glioma effects and safety of CAT3-SMEDDS were evaluated. Finally, Caco-2 cell uptake, MDCK monolayer cellular transfer, and the intestinal lymphatic transport mechanisms of SMEDDS were investigated in vitro and in vivo. Results show that CAT3-SMEDDS was able to form nanoemulsion droplets in artificial gastrointestinal fluid within 1 min, displaying an ideal particle size (15–30 nm), positive charge (5–9 mV), and controlled release behavior. CAT3-SMEDDS increased the membrane permeability of CAT3 by 3.9-fold and promoted intestinal lymphatic transport. Hence, the bioavailability of CAT3 was increased 79% and the level of its metabolite, PF403, was decreased to 49%. Moreover, the concentrations of CAT3 and PF403 were increased 2–6-fold and 1.3–7.2-fold, respectively, in the brain. Therefore, the anti-glioma effect in the orthotopic models was improved with CAT3-SMEDDS compared with CAT3 in 21 days. Additionally, CAT3-SMEDDS reduced the gastrointestinal side effects of CAT3, such as severe diarrhea, necrosis, and edema, and observed less inflammatory cell infiltration in the gastrointestinal tract, compared with the bare CAT3. Our work reveals that, through the metabolism modification effect, SMEDDS can improve the bioavailability of CAT3 and reduce the generation of PF403 in the gastrointestinal tract and plasma. Therefore, it has the potential to increase the anti-glioma effect and reduce the gastrointestinal side effects of CAT3 simultaneously.

In vitro and in vivo assessment of novel pH-sensitive interpenetrating polymer networks of a graft copolymer for gastro-protective delivery of ketoprofen

RSC Advances ◽  
2016 ◽  
Vol 6 (69) ◽  
pp. 64344-64356 ◽  
Author(s):  
Rashmi Boppana ◽  
Raghavendra V. Kulkarni ◽  
G. Krishna Mohan ◽  
Srinivas Mutalik ◽  
Tejraj M. Aminabhavi
Keyword(s):  
Side Effects ◽  
Drug Release ◽  
Graft Copolymer ◽  
Polymer Networks ◽  
Ph Sensitive ◽  
Interpenetrating Polymer Networks ◽  
In Vivo Assessment

Novel pH-sensitive IPN microbeads exhibited drug release in response to changing pH and reduced side effects of ketoprofenin vivo.

scholarly journals Anti-Inflammatory Effect of Very High Dose Local Vessel Wall Statin Administration: Poly(L,L-Lactide) Biodegradable Microspheres with Simvastatin for Drug Delivery System (DDS)

2021 ◽  
Vol 22 (14) ◽  
pp. 7486
Author(s):  
Piotr Wacinski ◽  
Mariusz Gadzinowski ◽  
Wojciech Dabrowski ◽  
Justyna Szumilo ◽  
Jakub Wacinski ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Side Effects ◽  
Drug Delivery System ◽  
Delivery System ◽  
Vessel Wall ◽  
Systemic Side Effects ◽  
Anti Inflammatory ◽  
Inflammatory Effect

Atherosclerosis involves an ongoing inflammatory response of the vascular endothelium and vessel wall of the aorta and vein. The pleiotropic effects of statins have been well described in many in vitro and in vivo studies, but these effects are difficult to achieve in clinical practice due to the low bioavailability of statins and their first-pass metabolism in the liver. The aim of this study was to test a vessel wall local drug delivery system (DDS) using PLA microstructures loaded with simvastatin. Wistar rats were fed high cholesterol chow as a model. The rat vessels were chemically injured by repeated injections of perivascular paclitaxel and 5-fluorouracil. The vessels were then cultured and treated by the injection of several concentrations of poly(L,L-lactide) microparticles loaded with the high local HMG-CoA inhibitor simvastatin (0.58 mg/kg) concentration (SVPLA). Histopathological examinations of the harvested vessels and vital organs after 24 h, 7 days and 4 weeks were performed. Microcirculation in mice as an additional test was performed to demonstrate the safety of this approach. A single dose of SVPLA microspheres with an average diameter of 6.4 μm and a drug concentration equal to 8.1% of particles limited the inflammatory reaction of the endothelium and vessel wall and had no influence on microcirculation in vivo or in vitro. A potent pleiotropic (anti-inflammatory) effect of simvastatin after local SVPLA administration was observed. Moreover, significant concentrations of free simvastatin were observed in the vessel wall (compared to the maximum serum level). In addition, it appeared that simvastatin, once locally administered as SVPLA particles, exerted potent pleiotropic effects on chemically injured vessels and presented anti-inflammatory action. Presumably, this effect was due to the high local concentrations of simvastatin. No local or systemic side effects were observed. This approach could be useful for local simvastatin DDSs when high, local drug concentrations are difficult to obtain, or systemic side effects are present.

scholarly journals Phthalocyanine incorporated alginate hydrogel with near infrared fluorescence for non-invasive imaging monitoring in vivo

RSC Advances ◽  
2017 ◽  
Vol 7 (11) ◽  
pp. 6501-6510 ◽  
Author(s):  
Jie Liang ◽  
Xia Dong ◽  
Chang Wei ◽  
Deling Kong ◽  
Tianjun Liu ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Fluorescence Imaging ◽  
Drug Delivery System ◽  
Delivery System ◽  
Near Infrared ◽  
Alginate Hydrogel ◽  
Near Infrared Fluorescence ◽  
Non Invasive ◽  
System P

A phthalocyanine incorporated alginate hydrogel with rhodamine was monitored by fluorescence imaging as a dual fluorescent drug delivery system.

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