72 results match your criteria peptide sirna-carrier


A Nanomule Peptide Carrier Delivers siRNA Across the Intact Blood-Brain Barrier to Attenuate Ischemic Stroke.

Front Mol Biosci 2021 26;8:611367. Epub 2021 Mar 26.

Michael Smith Laboratories, University of British Columbia, Vancouver, BC, Canada.

The blood-brain barrier (BBB) hinders the distribution of therapeutics intended for treatment of neuroinflammation (NI) of the central nervous system. A twelve-amino acid peptide that transcytoses the BBB, termed MTfp, was chemically conjugated to siRNA to create a novel peptide-oligonucleotide conjugate (POC), directed to downregulate NOX4, a gene thought responsible for oxidative stress in ischemic stroke. The MTfp-NOX4 POC has the ability to cross the intact BBB and knockdown NOX4 expression in the brain. Read More

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Advancing peptide siRNA-carrier designs through L/D-amino acid stereochemical modifications to enhance gene silencing.

Mol Ther Nucleic Acids 2021 Jun 19;24:462-476. Epub 2021 Mar 19.

Department of Oral Health Sciences, James B. Edwards College of Dental Medicine, Medical University of South Carolina (MUSC), Charleston, SC 29425, USA.

The 599 peptide has been previously shown to effectively deliver small interfering RNAs (siRNAs) to cancer cells, inducing targeted-oncogene silencing, with a consequent inhibition of tumor growth. Although effective, this study was undertaken to advance the 599 peptide siRNA-carrier design through L/D-amino acid stereochemical modifications. Consequently, 599 was modified to generate eight different peptide variants, incorporating either different stereochemical patterns of L/D-amino acids or a specific D-amino acid substitution. Read More

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Calcium-siRNA Nanocomplexes Optimized by Bovine Serum Albumin Coating Can Achieve Convenient and Efficient siRNA Delivery for Periodontitis Therapy.

Int J Nanomedicine 2020 20;15:9241-9253. Epub 2020 Nov 20.

State Key Laboratory of Military Stomatology, Department of Periodontology, School of Stomatology, Air Force Medical University, Xi'an, People's Republic of China.

Purpose: Reducing toxicity, immunogenicity, and costs of small interfering RNAs (siRNA) carrier materials are key goals for RNA interference (RNAi) technology transition from bench to bed. Recently, calcium ions (Ca) have garnered attention as a novel, alternative material for delivering siRNA to cells. However, the tolerance for Ca concentration varies in different cell types, which has limited its applications in vivo. Read More

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December 2020

Silencing KLK12 expression via RGDfC-decorated selenium nanoparticles for the treatment of colorectal cancer in vitro and in vivo.

Mater Sci Eng C Mater Biol Appl 2020 May 24;110:110594. Epub 2020 Jan 24.

Department of General Surgery, Guangzhou Digestive Disease Center, Guangzhou First People's Hospital, School of Medicine, South China University of Technology, Guangzhou 510180, China. Electronic address:

Short interfering RNA (siRNA) has been investigated as a promising modality of cancer treatment due to its capability to target specific target genes for downregulation. However, the successful application of this strategy depends on producing a safe and effective carrier system for delivering siRNA to the tumor. Thus, investigation of siRNA delivery carriers is a fundamental step in the field of siRNA-based therapeutics. Read More

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Anti-Metastatic Effects on Melanoma via Intravenous Administration of Anti-NF-κB siRNA Complexed with Functional Peptide-Modified Nano-Micelles.

Pharmaceutics 2020 Jan 15;12(1). Epub 2020 Jan 15.

School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.

Controlling metastasis is an important strategy in cancer treatment. Nanotechnology and nucleic acids with novel modalities are promising regulators of cancer metastasis. We aimed to develop a small interfering RNA (siRNA) systemic delivery and anti-metastasis system using nanotechnology. Read More

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January 2020

Design and anti-tumor activity of self-loaded nanocarriers of siRNA.

Colloids Surf B Biointerfaces 2019 Nov 24;183:110385. Epub 2019 Jul 24.

School of Life Sciences, Jilin University, Changchun 130012, PR China; Engineering Laboratory for AIDS Vaccine, Jilin University, Changchun 130012, PR China; Key Laboratory for Molecular Enzymology and Engineering, Ministry of Education, Jilin Universtiy, Changchun 130012, PR China. Electronic address:

Polypeptide carriers have a good cell compatibility, rich functionality, and facile synthesis and modification, make them promising materials as siRNA vectors. Phenylalanine dipeptide (FF) has been previously assessed as an siRNA vector and showed to have two major drawbacks, namely poor water solubility and poor serum stability. Herein, the FF backbone was modified by ligating a PEG-Arg-Ala (PEG-RA) sequence at the N-terminus to increase its hydrophilicity and serum stability. Read More

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November 2019

Targeting KRAS Mutant Lung Cancer Cells with siRNA-Loaded Bovine Serum Albumin Nanoparticles.

Pharm Res 2019 Jul 9;36(9):133. Epub 2019 Jul 9.

Department of Pharmacy, Pharmaceutical Technology and Biopharmaceutics, Ludwig-Maximilian University of Munich, Butenandtstr. 5-13, 81377, Munich, Germany.

Purpose: KRAS is the most frequently mutated gene in human cancers. Despite its direct involvement in malignancy and intensive effort, direct inhibition of KRAS via pharmacological inhibitors has been challenging. RNAi induced knockdown using siRNAs against mutant KRAS alleles offers a promising tool for selective therapeutic silencing in KRAS-mutant lung cancers. Read More

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Preparation and characterization of novel albumin-sericin nanoparticles as siRNA delivery vehicle for laryngeal cancer treatment.

Prep Biochem Biotechnol 2019 8;49(7):659-670. Epub 2019 May 8.

b Department of Chemistry, Biochemistry Division , Hacettepe University , Ankara , Turkey.

Small interfering RNA (siRNA)-based gene silencing strategy has high potential on suppressing specific molecular targets, involved in cancer progression. However, the lack of an effective nanocarrier system that safely delivers siRNA to its target still limits the clinical applications of siRNA. This study aimed to develop albumin-sericin nanoparticles (Alb-Ser NPs) as a novel siRNA delivery system for laryngeal cancer treatment. Read More

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Preparation and Characterization of Functionalized Graphene Oxide Carrier for siRNA Delivery.

Int J Mol Sci 2018 Oct 17;19(10). Epub 2018 Oct 17.

Department of Pharmaceutics, School of Pharmaceutical Sciences, Capital Medical University, Beijing 100069, China.

A successful siRNA delivery system is dependent on the development of a good siRNA carrier. Graphene oxide (GO) has gained great attention as a promising nanocarrier in recent years. It has been reported that GO could be used to deliver a series of drugs including synthetic compounds, proteins, antibodies, and genes. Read More

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October 2018

Anti-angiogenic treatment of endometriosis via anti-VEGFA siRNA delivery by means of peptide-based carrier in a rat subcutaneous model.

Gene Ther 2018 12 25;25(8):548-555. Epub 2018 Sep 25.

D.O. Ott Research Institute of Obstetrics, Gynecology and Reproductology, Mendeleevskaya line, 3, Saint-Petersburg, 199034, Russia.

Development of gene therapy for endometriosis requires inhibition of vascularization in endometrial lesions. We have previously developed CXCR4 receptor-targeted siRNA carrier L1 and observed efficient RNAi-mediated down-regulation of VEGFA gene expression in endothelial cells followed by decrease in VEGFA protein production and inhibition of cell migration. In this study we evaluated L1 carrier as non-viral vector for anti-VEGFA siRNA delivery into endometrial implants in rat subcutaneous endometriosis model created by subcutaneous auto-transplantation of uterus horn's fragments. Read More

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December 2018

Nanoscale polysaccharide derivative as an AEG-1 siRNA carrier for effective osteosarcoma therapy.

Int J Nanomedicine 2018 8;13:857-875. Epub 2018 Feb 8.

PCFM Lab and GDHPPC Lab, School of Materials Science and Engineering, Sun Yat-sen University, Guangzhou.

Background: Nanomedicine, which is the application of nanotechnology in medicine to make medical diagnosis and treatment more accurate, has great potential for precision medicine. Despite some improvements in nanomedicine, the lack of efficient and low-toxic vectors remains a major obstacle.

Objective: The aim of this study was to prepare an efficient and low-toxic vector which could deliver astrocyte elevated gene-1 () small interfering RNA (siRNA; siAEG-1) into osteosarcoma cells effectively and silence the targeted gene both in vitro and in vivo. Read More

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Synthesis, characterization, and in vitro cytotoxicity of fatty acyl-CGKRK-chitosan oligosaccharides conjugates for siRNA delivery.

Int J Biol Macromol 2018 Jun 2;112:694-702. Epub 2018 Feb 2.

Department of Biomedical and Pharmaceutical Sciences, Chapman University School of Pharmacy, Harry and Diane Rinker Health Science Campus, Irvine, CA 92618, United States. Electronic address:

In this studies, three fatty acyl derivatives of CGKRK homing peptides were coupled successfully to chitosan oligosaccharides (COS) using sulfosuccinimidyl-4-(N-maleimidomethyl)cyclohexane-1-carboxylate sodium salt (sulfo-SMCC). The COS-SMCC was prepared by direct coupling between COS and sulfo-SMCC in PBS (pH7.5) at RT for 48h. Read More

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From Pulmonary Surfactant, Synthetic KL4 Peptide as Effective siRNA Delivery Vector for Pulmonary Delivery.

Mol Pharm 2017 12 17;14(12):4606-4617. Epub 2017 Nov 17.

Department of Pharmacology & Pharmacy, Li Ka Shing Faculty of Medicine, The University of Hong Kong , 21 Sassoon Road, Pokfulam, Hong Kong.

Pulmonary delivery of small interfering RNA (siRNA) has huge potential for the treatment of a wide range of respiratory diseases. The ability of naked siRNA to transfect cells in the lungs without a delivery vector has prompted the investigation of whether an endogenous component is at least partially responsible for the cellular uptake of siRNA, and whether a safe and efficient delivery system could be developed from this component to further improve the transfection efficiency. Surfactant protein B (SP-B), a positively charged protein molecule found in lung surfactant, is one of the possible candidates. Read More

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December 2017

Targeting neuronal nitric oxide synthase by a cell penetrating peptide Tat-LK15/siRNA bioconjugate.

Neurosci Lett 2017 05 24;650:153-160. Epub 2017 Apr 24.

Department of Anesthesiology, Guangzhou General Hospital of Guangzhou Military Command, Guangzhou, 510010, Guangdong Province, China.

We developed a cell penetrating peptide (CPP) Tat-LK15, as a siRNA carrier to target nNOS. The feasibility, stability, efficiency and selectivity of this peptide-siRNA complex were evaluated in rat neuronal cells. We also compared the new method with conventional siRNA carrier Lipofectamine™. Read More

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Efficiency and Safety of β-CD-(D) as siRNA Carrier for Decreasing Matrix Metalloproteinase-9 Expression and Improving Wound Healing in Diabetic Rats.

ACS Appl Mater Interfaces 2017 May 5;9(20):17417-17426. Epub 2017 May 5.

Department of Endocrinology, Sun Yat-sen Memorial Hospital, Guangdong Provincal Key Laboratory of Malignant Tumor Epigenetics and Gene Reguatioǹ Medical Research Center, Sun Yat-sen University , Guangzhou 510120, China.

Overexpression of matrix metalloproteinase-9 (MMP-9) is critical for diabetic chronic wounds involved in the refractory wound healing process. We aimed to develop a strategy through RNAi to decrease MMP-9 expression and improve diabetic wound healing. We had explored β-CD-(D) as a gene carrier to take siRNA and effectively interfere with MMP-9 expression. Read More

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PEGylation rate influences peptide-based nanoparticles mediated siRNA delivery in vitro and in vivo.

J Control Release 2017 06 12;256:79-91. Epub 2017 Apr 12.

Centre de Recherche de Biologie cellulaire de Montpellier, CNRS UMR 5237, 1919 Route de Mende, 34293 Montpellier Cedex 5, France. Electronic address:

Small interfering RNAs (siRNAs) present a strong therapeutic potential because of their ability to inhibit the expression of any desired protein. Recently, we developed the retro-inverso amphipathic RICK peptide as novel non-covalent siRNA carrier. This peptide is able to form nanoparticles (NPs) by self-assembling with the siRNA resulting in the fully siRNA protection based on its protease resistant peptide sequence. Read More

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Aerosol Delivery of siRNA to the Lungs. Part 2: Nanocarrier-based Delivery Systems.

Kona 2017 30;34:44-69. Epub 2016 Apr 30.

Translational Drug Delivery Research (TransDDR) Laboratory, Department of Pharmaceutical Sciences, The Daniel K. Inouye College of Pharmacy, University of Hawaii at Hilo, 200 West Kawili Street, Hilo, Hawaii 96720, USA; Natural Products and Experimental Therapeutics Program, The Cancer Research Center, University of Hawaii at Manoa, Honolulu, Hawaii 96813, USA.

In this article, applications of engineered nanoparticles containing siRNA for inhalation delivery are reviewed and discussed. Diseases with identified protein malfunctions may be mitigated through the use of well-designed siRNA therapeutics. The inhalation route of administration provides local delivery of siRNA therapeutics to the lungs for various pulmonary diseases. Read More

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Gene-silencing effects of anti-survivin siRNA delivered by RGDV-functionalized nanodiamond carrier in the breast carcinoma cell line MCF-7.

Int J Nanomedicine 2016;11:5771-5787. Epub 2016 Nov 4.

School of Chemical Biology and Pharmaceutical Sciences, Capital Medical University, Beijing, People's Republic of China.

Nanodiamond (ND) is a renowned material in nonviral small interfering RNA (siRNA) carrier field due to its unique physical, chemical, and biological properties. In our previous work, it was proven that ND could deliver siRNA into cells efficiently and downregulate the expression of desired protein. However, synthesizing a high-efficient tumor-targeting carrier using ND is still a challenge. Read More

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February 2017

Multifunctional WS @Poly(ethylene imine) Nanoplatforms for Imaging Guided Gene-Photothermal Synergistic Therapy of Cancer.

Adv Healthc Mater 2016 11 26;5(21):2776-2787. Epub 2016 Sep 26.

College of Materials Science and Opto-electronic Technology, University of Chinese Academy of Sciences, Beijing, 100049, P. R. China.

The combination of photothermal therapy (PTT) with gene therapy (GT) to improve PTT efficiency and thus eliminate cancer cells under mild hyperthermia is highly needed. Herein, multifunctional WS @poly(ethylene imine) (WS @PEI) nanoplatform has been designed and constructed for gene-photothermal synergistic therapy of tumors at mild condition. After a surface modification of WS with a positively charged PEI, the as-prepared WS @PEI nanoplatform can not only act as an efficient survivin-siRNA carrier for GT but also exhibit remarkable near-infrared (NIR) photothermal effects for PTT. Read More

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November 2016

Development of an Innovative Intradermal siRNA Delivery System Using a Combination of a Functional Stearylated Cytoplasm-Responsive Peptide and a Tight Junction-Opening Peptide.

Molecules 2016 Sep 24;21(10). Epub 2016 Sep 24.

Laboratory of Pharmaceutics and Drug Delivery, Department of Pharmaceutical Science, School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.

As a new category of therapeutics for skin diseases including atopic dermatitis (AD), nucleic acids are gaining importance in the clinical setting. Intradermal administration is noninvasive and improves patients' quality of life. However, intradermal small interfering RNA (siRNA) delivery is difficult because of two barriers encountered in the skin: intercellular lipids in the stratum corneum and tight junctions in the stratum granulosum. Read More

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September 2016

Aerosol Delivery of siRNA to the Lungs. Part 1: Rationale for Gene Delivery Systems.

Kona 2016 Feb 30;33:63-85. Epub 2015 Sep 30.

Department of Pharmaceutical Sciences, The Daniel K. Inouye College of Pharmacy, University of Hawaii at Hilo, 200 West Kawili Street, Hilo, Hawaii 96720, USA; Natural Products and Experimental Therapeutics Program, University of Hawaii Cancer Center, University of Hawaii at Manoa, Honolulu, Hawaii 96813, USA.

This article reviews the pulmonary route of administration, aerosol delivery devices, characterization of pulmonary drug delivery systems, and discusses the rationale for inhaled delivery of siRNA. Diseases with known protein malfunctions may be mitigated through the use of siRNA therapeutics. The inhalation route of administration provides local delivery of siRNA therapeutics for the treatment of various pulmonary diseases, however barriers to pulmonary delivery and intracellular delivery of siRNA exists. Read More

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February 2016

Comparing exosome-like vesicles with liposomes for the functional cellular delivery of small RNAs.

J Control Release 2016 06 9;232:51-61. Epub 2016 Apr 9.

Laboratory of General Biochemistry and Physical Pharmacy, Faculty of Pharmaceutical Sciences, Ghent University, Ottergemsesteenweg 460, 9000 Ghent, Belgium.

Exosome-like vesicles (ELVs) play an important role in intercellular communication by acting as natural carriers for biomolecule transfer between cells. This unique feature rationalizes their exploitation as bio-inspired drug delivery systems. However, the therapeutic application of ELVs is hampered by the lack of efficient and reproducible drug loading methods, in particular for therapeutic macromolecules. Read More

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Antibody-coupled siRNA as an efficient method for in vivo mRNA knockdown.

Nat Protoc 2016 Jan 3;11(1):22-36. Epub 2015 Dec 3.

Department of Medicine A, Hematology and Oncology, University Hospital Muenster, Muenster, Germany.

Knockdown of genes by RNA interference (RNAi) in vitro requires methods of transfection or transduction, both of which have limited impact in vivo. As a virus-free approach, we chemically coupled cell surface receptors internalizing antibodies to the short interfering RNA (siRNA) carrier peptide protamine using the bispecific cross-linker sulfo-SMCC (sulfosuccinimidyl 4-(N-maleimidomethyl)cyclohexane-1-carboxylate). First, protamine was conjugated amino-terminally to sulfo-SMCC, and then this conjugate was coupled via cysteine residues to the IgG backbone to carry siRNA. Read More

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January 2016

Dual antitumoral potency of EG5 siRNA nanoplexes armed with cytotoxic bifunctional glutamyl-methotrexate targeting ligand.

Biomaterials 2016 Jan 5;77:98-110. Epub 2015 Nov 5.

Department of Pharmacy and Center for NanoScience, Ludwig-Maximilians-Universität München, Munich, Germany; Nanosystems Initiative Munich, Germany. Electronic address:

Synthetic small interfering RNA (siRNA) is a class of therapeutic entities that allow for specific silencing of target genes via RNA interference (RNAi) and comprise an enormous clinical potential for a variety of diseases, including cancer. However, efficient tissue-specific delivery of siRNA remains the major limitation in the development of RNAi-based cancer therapeutics. To achieve this, we have synthesized a series of sequence-defined oligomers, which include a cationic (oligoethanamino)amide core (for nanoparticle formation with siRNA), cysteines (as bioreversible disulfide units), and a polyethylene glycol chain (for shielding of surface charges) coupled to a terminal targeting ligand. Read More

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January 2016

siRNA delivered by EGFR-specific scFv sensitizes EGFR-TKI-resistant human lung cancer cells.

Biomaterials 2016 Jan 23;76:196-207. Epub 2015 Oct 23.

Department of Respiratory Medicine, Xijing Hospital, Fourth Military Medical University, 127 Changle West Road, Xi'an 710032, China. Electronic address:

The overexpression of epidermal growth factor receptor (EGFR) is closely associated with a poor outcome in non-small cell lung cancer (NSCLC), and EGFR is an ideal biomarker for the targeted therapy of NSCLC. Although patients with EGFR-activating mutations respond to EGFR tyrosine kinase inhibitors (EGFR-TKIs), they eventually acquire resistance, which typically results from a secondary EGFR mutation or the activation of other signaling pathways. Novel approaches to overcome or prevent EGFR-TKI resistance are clinically important. Read More

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January 2016

Non-covalent Nanocomplexes of Folic Acid and Reducible Polyethylenimine for Survivin siRNA Delivery.

Anticancer Res 2015 Oct;35(10):5433-41

College of Life Science, Jilin University, Changchun, P.R. China College of Pharmacy, The Ohio State University, Columbus, OH, U.S.A.

Background/aim: Efficient delivery of siRNA is critical for its therapeutic applications. This study was aimed at the design, synthesis and evaluation of a novel delivery system based on non-covalent complexes of folic acid (FA) and a reducible polyethylenimine (PEI) derivative, PEI-SS.

Materials And Methods: PEI-SS was synthesized by crosslinking low-molecular weight PEI using a reducible crosslinking agent. Read More

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October 2015

Optimization of a siRNA Carrier Modified with a pH-Sensitive Cationic Lipid and a Cyclic RGD Peptide for Efficiently Targeting Tumor Endothelial Cells.

Pharmaceutics 2015 Sep 14;7(3):320-33. Epub 2015 Sep 14.

Laboratory for Innovative Nanomedicine, Faculty of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-ku, Sapporo 060-0812, Japan.

In recent years, anti-angiogenic therapy has attracted much interest because it is a versatile approach to treating most types of tumors, and therefore would be expected to be applicable for various cancers. Severe adverse events in patients treated with currently available anti-angiogenic therapeutics have, however, been reported, and these are caused by their inhibitory effects in normal tissue. To achieve an efficient anti-angiogenic therapy with minimal toxicity, a drug delivery system (DDS) specific to tumor endothelial cells (TECs) is needed. Read More

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September 2015

Potential application of injectable chitosan hydrogel treated with siRNA in chronic rhinosinusitis therapy.

Mol Med Rep 2015 Nov 21;12(5):6688-94. Epub 2015 Aug 21.

Department of Otorhinolaryngology, Yinzhou Hospital Affiliated to the Medical School of Ningbo University, Ningbo, Zhejiang 315000, P.R. China.

Chronic rhinosinusitis is a condition with severe clinical symptoms and limited therapeutic solutions. It has been reported that vascular endothelial growth factor (VEGF) can promote nasal epithelial cell growth and result in hyperplasia of the sinuses. Therefore, the downregulation of VEGF may inhibit the process of hyperplasia. Read More

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November 2015

Peptide-like Polymers Exerting Effective Glioma-Targeted siRNA Delivery and Release for Therapeutic Application.

Small 2015 Oct 28;11(38):5142-50. Epub 2015 Jul 28.

Department of Pharmaceutics, School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai, 201203, China.

Lipopolymer 49, a solid-phase synthesized T-shaped peptide-like oligoamide containing two central oleic acids, 20 aminoethane, and two terminal cysteine units, is identified as very potent and biocompatible small interfering RNA (siRNA) carrier for gene silencing in glioma cells. This carrier is combined with a novel targeting polymer 727, containing a precise sequence of Angiopep 2 targeting peptide, linked with 28 monomer units of ethylene glycol, 40 aminoethane, and two terminal cysteines in siRNA complex formation. Angiopep-polyethylene glycol (PEG)/siRNA polyplexes exhibit good nanoparticle features, effective glioma-targeting siRNA delivery, and intracellular siRNA release, resulting in an outstanding gene downregulation both in glioma cells and upon intravenous delivery in glioma model nude mice without significant biotoxicity. Read More

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October 2015

Light-activated RNA interference in human embryonic stem cells.

Biomaterials 2015 Sep 10;63:70-9. Epub 2015 Jun 10.

Department of Chemistry and Biochemistry, University of California, Santa Barbara, CA 93106, United States. Electronic address:

We describe a near infrared (NIR) light-activated gene silencing method in undifferentiated human embryonic stem cell (hESC) using a plasmonic hollow gold nanoshell (HGN) as the siRNA carrier. Our modular biotin-streptavidin coupling strategy enables positively charged TAT-peptide to coat oligonucleotides-saturated nanoparticles as a stable colloid formation. TAT-peptide coated nanoparticles with dense siRNA loading show efficient penetration into a wide variety of hESC cell lines. Read More

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September 2015