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Current Development of siRNA Bioconjugates: From Research to the Clinic
In this study, it was shown that the main factor determining the nature of the biodistribution of conjugates is their lipophilicity. Conjugates of siRNA with lower lipophilicity; i.e., derivatives of retinoic acid, lithocholic acid, and docosahexanoic acid with greater efficiency than cholesterol conjugates accumulated in the kidneys, bladder, and lungs of the mouse after subcutaneous injection (Biscans et al., 2018). This fact is consistent with previous data that showed that more lipophilic conjugates bind more efficiently to serum components, and thus are not excreted by the kidneys (Wolfrum et al., 2007; Osborn et al.,...
Source: Frontiers in Pharmacology - April 25, 2019 Category: Drugs & Pharmacology Source Type: research
Design and Invitro Characterization of Green Synthesized Magnetic Nanoparticles Conjugated with Multitargeted Poly Lactic Acid Copolymers for Co-delivery of siRNA and Paclitaxel
CONCLUSION: Conjugation of both folic acid and T7-peptide on the surface of micelles compared to separate conjugation of one of these ligands, increased the efficiency of drug and siRNA delivery to breast cancer cells.PMID:34520835 | DOI:10.1016/j.ejps.2021.106007
Source: European Journal of Pharmaceutical Sciences - September 14, 2021 Category: Drugs & Pharmacology Authors: Amin Amani Mohammad Dustparast Mehran Noruzpour Rasool Asghari Zakaria Hossein Ali Ebrahimi Source Type: research
Combination of Nanovectorized siRNA Directed against Survivin with Doxorubicin for Efficient Anti-Cancer Activity in HER2+ Breast Cancer Cells
In conclusion, a combination of anti-Survivin siRNA and DOX would be a good alternative in HER2+ breast cancer therapy.PMID:36432729 | DOI:10.3390/pharmaceutics14112537
Source: Cancer Control - November 26, 2022 Category: Cancer & Oncology Authors: Sahar Eljack Emilie Allard-Vannier Yoann Misericordia Katel Herv é-Aubert Nicolas Aubrey Igor Chourpa Areeg Faggad Stephanie David Source Type: research
Exosomes-delivered PD-L1 siRNA and CTLA-4 siRNA protect against growth and tumor immune escape in colorectal cancer
CONCLUSION: Exosomes containing PD-L1 siRNA and CTLA-4 siRNA suppressed CRC progression and enhanced tumor immune responses.PMID:37217085 | DOI:10.1016/j.ygeno.2023.110646
Source: Genomics - May 22, 2023 Category: Genetics & Stem Cells Authors: Jian Li Yuxiang Chen Mingmei Liao Shuyi Yu Binwen Yuan Zeming Jia Lin Zhou Yaping Tang Source Type: research
Effect of the combination of cationic lipid and phospholipid on gene-knockdown using siRNA lipoplexes in breast tumor cells and mouse lungs
Mol Med Rep. 2023 Oct;28(4):180. doi: 10.3892/mmr.2023.13067. Epub 2023 Aug 18.ABSTRACTPreviously, using three types of cationic lipids, the effect of phospholipids in liposomal formulations on gene-knockdown efficacy was determined after in vitro and in vivo transfection with small interfering RNA (siRNA)/cationic liposome complexes (siRNA lipoplexes) containing various cationic lipids and phospholipids. In the present study, six other types of cationic lipids, namely N,N-dimethyl-N-tetradecyltetradecan-1-aminium bromide, N-hexadecyl-N,N-dimethylhexadecan-1-aminium bromide (DC-1-16), 2-[bis{2-(tetradecanoyloxy)ethyl}amino...
Source: Molecular Medicine - August 18, 2023 Category: Molecular Biology Authors: Yoshiyuki Hattori Min Tang Aya Aoki Momoka Ezaki Hana Sakai Kei-Ichi Ozaki Source Type: research
A new liposomal nanocarrier for co-delivery of gedunin and p-glycoprotein siRNA to target breast cancer stem cells
Nat Prod Res. 2022 Jan 27:1-4. doi: 10.1080/14786419.2022.2032048. Online ahead of print.ABSTRACTGedunin is a secondary metabolite found in neem tree. Since the first discovery of this compound, its bio-active properties have been continuously evaluated. However, the low hydrophobicity of gedunin decreases its bioavailability and pharmacokinetic profile. In the present investigation, a new liposomal nanocarrier for co-delivery of gedunin and P-glycoprotein (P-gp) siRNA [siRNA coated liposomal gedunin (Lipo-Ged-siRNA)] was developed to improve the anti-proliferative activity of gedunin. Characteristics of prepared Lipo-Ged-...
Source: Natural Product Research - January 27, 2022 Category: Biochemistry Authors: Mohan Singh Rana Meran Keshawa Ediriweera Umapriyatharshini Rajagopalan Desiree Nedra Karunaratne Kamani Hemamala Tennekoon Sameera Ranganath Samarakoon Source Type: research
SiRNA-phospholipid conjugates for gene and drug delivery in cancer treatment.
In this study, the thiol-modified sense and antisense siRNA are chemically conjugated with phospholipids to form sense and antisense siRNA-phospholipid, and then these sense or antisense siRNA-phospholipids with equal amounts are annealed to generate siRNA-phospholipids. The siRNA-phospholipids can serve dual functions as agents that can silence gene expression and as a component of nanoparticles to embed hydrophobic anticancer drugs to cure tumor. siRNA-phospholipids together with cationic lipids and DSPE-PEG2000 fuse around PLGA to form siRNA-phospholipids enveloped nanoparticles (siRNA-PCNPs), which can deliver siRNAs a...
Source: Biomaterials - May 2, 2014 Category: Materials Science Authors: Liu H, Li Y, Mozhi A, Zhang L, Liu Y, Xu X, Xing J, Liang X, Ma G, Yang J, Zhang X Tags: Biomaterials Source Type: research
Co-delivery of Doxorubicin and Bmi1 siRNA by Folate Receptor Targeted Liposomes Exhibits Enhanced Anti-Tumor Effects in vitro and in vivo
Bmi1 gene overexpression is found in various human tumors and has been shown as a potential target for gene treatment. However, siRNA-based treatments targeting Bmi1 gene have been restricted to limited delivery, low bioavailability and hence relatively reduced efficacy. To overcome these barriers, we developed a folate receptor targeted co-delivery system folate-doxorubicin/Bmi1 siRNA liposome (FA-DOX/siRNA-L). The FA-DOX/siRNA-L was prepared through electrostatic interaction between folate doxorubicin liposome (FA-DOX-L) and Bmi1 siRNA. In vitro and in vivo studies showed that FA-DOX/siRNA-L inhibited tumor growth by com...
Source: Theranostics - November 15, 2014 Category: Molecular Biology Authors: Tan Yang, Bin Li, Shibo Qi, Yong Liu, Yongkang Gai, Peng Ye, Guang Yang, Wendian Zhang, Peng Zhang, Xingxing He, Weijie Li, Zhiping Zhang, Guangya Xiang, Chuanrui Xu Tags: Research Paper Source Type: research
