scholarly journals Bottlebrush-architectured poly(ethylene glycol) as an efficient vector for RNA interference in vivo

2019 ◽  
Vol 5 (2) ◽  
pp. eaav9322 ◽  
Author(s):  
Dali Wang ◽  
Jiaqi Lin ◽  
Fei Jia ◽  
Xuyu Tan ◽  
Yuyan Wang ◽  
...  
Keyword(s):  
Rna Interference ◽  
Ethylene Glycol ◽  
Target Genes ◽  
Area Under The Curve ◽  
Fold Increase ◽  
Small Interfering Rnas ◽  
Poly Ethylene Glycol ◽  
Linear Poly ◽  
Poly Ethylene

Nonhepatic delivery of small interfering RNAs (siRNAs) remains a challenge for development of RNA interference–based therapeutics. We report a noncationic vector wherein linear poly(ethylene glycol) (PEG), a polymer generally considered as inert and safe biologically but ineffective as a vector, is transformed into a bottlebrush architecture. This topology provides covalently embedded siRNA with augmented nuclease stability and cellular uptake. Consisting almost entirely of PEG and siRNA, the conjugates exhibit a ~25-fold increase in blood elimination half-life and a ~19-fold increase in the area under the curve compared with unmodified siRNA. The improved pharmacokinetics results in greater tumor uptake and diminished liver capture. Despite the structural simplicity these conjugates efficiently knock down target genes in vivo without apparent toxic and immunogenic reactions. Given the benign biological nature of PEG and its widespread precedence in biopharmaceuticals, we anticipate the brush polymer–based technology to have a significant impact on siRNA therapeutics.

scholarly journals Poly(ethylene glycol)-b-poly(1,3-trimethylene carbonate) Amphiphilic Copolymers for Long-Acting Injectables: Synthesis, Non-Acylating Performance and In Vivo Degradation

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1438
Author(s):  
Silvio Curia ◽  
Feifei Ng ◽  
Marie-Emérentienne Cagnon ◽  
Victor Nicoulin ◽  
Adolfo Lopez-Noriega
Keyword(s):  
Ethylene Glycol ◽  
Ring Opening ◽  
Gel Chromatography ◽  
Amphiphilic Copolymers ◽  
Trimethylene Carbonate ◽  
Poly Ethylene Glycol ◽  
Poly Ethylene ◽  
Long Acting ◽  
In Vivo Degradation

This article presents the evaluation of diblock and triblock poly(ethylene glycol)-b-poly(1,3-trimethylene carbonate) amphiphilic copolymers (PEG-PTMCs) as excipients for the formulation of long-acting injectables (LAIs). Copolymers were successfully synthesised through bulk ring-opening polymerisation. The concomitant formation of PTMC homopolymer could not be avoided irrespective of the catalyst amount, but the by-product could easily be removed by gel chromatography. Pure PEG-PTMCs undergo faster erosion in vivo than their corresponding homopolymer. Furthermore, these copolymers show outstanding stability compared to their polyester analogues when formulated with amine-containing reactive drugs, which makes them particularly suitable as LAIs for the sustained release of drugs susceptible to acylation.

scholarly journals Local Toxicity of Topically Administrated Thermoresponsive Systems: In Vitro Studies with In Vivo Correlation

2018 ◽  
Vol 47 (3) ◽  
pp. 426-432 ◽  
Author(s):  
Sivan Yogev ◽  
Ayelet Shabtay-Orbach ◽  
Abraham Nyska ◽  
Boaz Mizrahi
Keyword(s):  
Block Copolymer ◽  
Ethylene Glycol ◽  
Medical Devices ◽  
Poly Lactic Acid ◽  
Poly Ethylene Glycol ◽  
Thermoresponsive Polymers ◽  
Wide Range ◽  
Poly Ethylene

Thermoresponsive materials have the ability to respond to a small change in temperature—a property that makes them useful in a wide range of applications and medical devices. Although very promising, there is only little conclusive data about the cytotoxicity and tissue toxicity of these materials. This work studied the biocompatibility of three Food and Drug Administration approved thermoresponsive polymers: poly( N-isopropyl acrylamide), poly(ethylene glycol)-poly(propylene glycol)-poly(ethylene glycol) tri-block copolymer, and poly(lactic acid-co-glycolic acid) and poly(ethylene glycol) tri-block copolymer. Fibroblast NIH 3T3 and HaCaT keratinocyte cells were used for the cytotoxicity testing and a mouse model for the in vivo evaluation. In vivo results generally showed similar trends as the results seen in vitro, with all tested materials presenting a satisfactory biocompatibility in vivo. pNIPAM, however, showed the highest toxicity both in vitro and in vivo, which was explained by the release of harmful monomers and impurities. More data focusing on the biocompatibility of novel thermoresponsive biomaterials will facilitate the use of existing and future medical devices.

In vivo and in vitro degradation of poly(ether ester) block copolymers based on poly(ethylene glycol) and poly(butylene terephthalate)

Biomaterials ◽  
2004 ◽  
Vol 25 (2) ◽  
pp. 247-258 ◽  
Author(s):  
A.A. Deschamps ◽  
A.A. van Apeldoorn ◽  
H. Hayen ◽  
J.D. de Bruijn ◽  
U. Karst ◽  
...  
Keyword(s):  
Block Copolymers ◽  
Ethylene Glycol ◽  
Poly Ethylene Glycol ◽  
In Vitro Degradation ◽  
Butylene Terephthalate ◽  
Poly Ethylene ◽  
Ether Ester

In vitro and in vivo study of poly(ethylene glycol) conjugated ketoprofen to extend the duration of action

2007 ◽  
Vol 341 (1-2) ◽  
pp. 50-57 ◽  
Author(s):  
Hoo-Kyun Choi ◽  
Myung-Kwan Chun ◽  
Se Hee Lee ◽  
Mee Hee Jang ◽  
Hee Doo Kim ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
In Vivo Study ◽  
Poly Ethylene Glycol ◽  
Duration Of Action ◽  
Poly Ethylene

Stabilization of L-Asparaginase Modified with Comb-Shaped Poly(ethylene glycol) Derivatives, in vivo and in vitro

1994 ◽  
Vol 5 (4) ◽  
pp. 283-286 ◽  
Author(s):  
Yoh Kodera ◽  
Taichi Sekine ◽  
Tohru Yasukohchi ◽  
Yoshihiro Kiriu ◽  
Misao Hiroto ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Poly Ethylene Glycol ◽  
Poly Ethylene ◽  
Ethylene Glycol Derivatives

Furry nanoparticles: synthesis and characterization of nanoemulsion-mediated core crosslinked nanoparticles and their robust stability in vivo

2020 ◽  
Vol 11 (27) ◽  
pp. 4408-4416
Author(s):  
Rena Tanaka ◽  
Koichi Arai ◽  
Jun Matsuno ◽  
Miyo Soejima ◽  
Ji Ha Lee ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Structural Stability ◽  
Robust Stability ◽  
Synthesis And Characterization ◽  
Poly Ethylene Glycol ◽  
Nanoparticles Synthesis ◽  
High Structural Stability ◽  
Poly Ethylene

Core crosslinked nanoparticles were prepared via nanoemulsion stabilized by a poly(ethylene glycol)-bearing surfactant, which show high structural stability in vivo.

A smart drug-delivery nanosystem based on carboxylated graphene quantum dots for tumor-targeted chemotherapy

Nanomedicine ◽  
2019 ◽  
Vol 14 (15) ◽  
pp. 2011-2025 ◽  
Author(s):  
Zhen Li ◽  
Jialong Fan ◽  
Chunyi Tong ◽  
Hongyan Zhou ◽  
Wenmiao Wang ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Quantum Dots ◽  
Folic Acid ◽  
Ethylene Glycol ◽  
Drug Delivery System ◽  
Delivery System ◽  
Graphene Quantum Dots ◽  
Poly Ethylene Glycol ◽  
Poly Ethylene

Aim: Constructing a new drug-delivery system using carboxylated graphene quantum dots (cGQDs) for tumor chemotherapy in vivo. Materials & methods: A drug-delivery system was synthesized through a crosslink reaction of cGQDs, NH2-poly(ethylene glycol)-NH2 and folic acid. Results: A drug delivery system of folic acid-poly(ethylene glycol)-cGQDs was successfully constructed with ideal entrapment efficiency (97.5%) and drug-loading capacity (40.1%). Cell image indicated that the nanosystem entered into human cervical cancer cells mainly through macropinocytosis-dependent pathway. In vivo experiments showed the outstanding antitumor ability and low systemic toxicity of this nanodrug-delivery system. Conclusion: The newly developed drug-delivery system provides an important alternative for tumor therapy without causing systemic adverse effects.

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