Synthesis of a high functionality and quality lipid with gp130 binding hydrophobic peptide for the preparation of human glioma cell-targeted PEGylated liposomes

Suga, Tadaharu; Watanabe, Masanori; Sugimoto, Yuri; Masuda, Tomonari; Kuroda, Naotaka; Hagimori, Masayori; Kawakami, Shigeru

doi:10.1016/j.jddst.2018.12.037

Cited by 15 publications

(7 citation statements)

References 19 publications

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“…We have previously reported that ligand-peptide-modified liposomes can be prepared by bulk mixing for 1 h using HFQ lipids with (SG) 5 as spacer. 5 , 6 , 8 , 9 Our HFQ lipids might form unstable micelles compared to those observed with conventional PEG lipids. Therefore, we hypothesized that HFQ lipids would be rapidly inserted into PEGylated liposomes without any additional destabilization of the liposomal membrane.…”

Section: Discussionmentioning

confidence: 81%

“…In addition, HFQ lipids were designed to meet the criteria for dispersibility in water (0.2 mM and above to enable ligand modification using the post-insertion method (bulk mixing)). [7][8][9] In the bulk mixing method, lipid composition of the nanoparticles, mixing temperature, and duration may affect the physicochemical properties. 10,11 For the large-scale preparation of targeted liposomes, it is necessary to change the preparation conditions, including the conditions mentioned above, and change the volume.…”

Section: Introductionmentioning

confidence: 99%

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Microfluidic Post-Insertion Method for the Efficient Preparation of PEGylated Liposomes Using High Functionality and Quality Lipids

Sugimoto

Suga

Kato

et al. 2022

IJN

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Targeted liposomes using ligand peptides have been applied to deliver therapeutic agents to the target sites. The postinsertion method is commonly used because targeted liposomes can be prepared by simple mixing of ligand peptide-lipid and liposomes. A large-scale preparation method is required for the clinical application of ligand-peptide-modified liposomes. Largescale preparation involves an increase in volume and a change in the preparation conditions. Therefore, the physicochemical properties of liposomes may change owing to large alterations in the preparation conditions. To address this issue, we focused on a microfluidic device and developed a novel ligand peptide modification method, the microfluidic post-insertion method. Methods: We used integrin αvβ3-targeted GRGDS (RGD) and cyclic RGDfK (cRGD)-modified high functionality and quality (HFQ) lipids, which we had previously developed. First, the preparation conditions of the total flow rate in the microfluidic device for modifying HFQ lipids to polyethylene glycol (PEG)-modified (PEGylated) liposomes were optimized by evaluating the physicochemical properties of the liposomes. The targeting ability of integrin αvβ3-expressing colon 26 murine colorectal carcinoma cells was evaluated by comparing the cellular association properties of the liposomes prepared by the conventional post-insertion method. Results: When the RGD-HFQ lipid was modified into PEGylated liposomes by varying the total flow rate (1, 6, and 12 mL/min) of the microfluidic device, as the total flow rate increased, the polydispersity index also increased, whereas the particle size did not change. Furthermore, the RGD-and cRGD-modified PEGylated liposomes prepared at a total flow rate of 1 mL/min showed high cellular association properties equivalent to those prepared by the conventional post-insertion method. Conclusion: Microfluidic post-insertion method of HFQ lipids might be useful for clinical application and large-scale preparation of targeted liposomes.

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Section: Discussionmentioning

confidence: 81%

Section: Introductionmentioning

confidence: 99%

Microfluidic Post-Insertion Method for the Efficient Preparation of PEGylated Liposomes Using High Functionality and Quality Lipids

Sugimoto

Suga

Kato

et al. 2022

IJN

Self Cite

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“…108 Suga et al used this sequence to functionalize PEGylated liposomes with the previously described (SG) n linker to enhance targeting of glioma cells. 84 Their results demonstrated a selective association of VTW-K 3 -(SG) 5 /PEGylated liposomes with U251MG glioma cells for enhanced uptake compared to other control ligand sequences.…”

Section: Receptor-targeting Peptide Ligandsmentioning

confidence: 94%

Peptide functionalized liposomes for receptor targeted cancer therapy

2021

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Most clinically approved cancer therapies are potent and toxic small molecules that are limited by severe off-target toxicities and poor tumor-specific localization. Over the past few decades, attempts have been made to load chemotherapies into liposomes, which act to deliver the therapeutic agent directly to the tumor. Although liposomal encapsulation has been shown to decrease toxicity in human patients, reliance on passive targeting via the enhanced permeability and retention (EPR) effect has left some of these issues unresolved. Recently, investigations into modifying the surface of liposomes via covalent and/or electrostatic functionalization have offered mechanisms for tumor homing and subsequently controlled chemotherapeutic delivery. A wide variety of biomolecules can be utilized to functionalize liposomes such as proteins, carbohydrates, and nucleic acids, which enable multiple directions for cancer cell localization. Importantly, when nanoparticles are modified with such molecules, care must be taken as not to inactivate or denature the ligand. Peptides, which are small proteins with <30 amino acids, have demonstrated the exceptional ability to act as ligands for transmembrane protein receptors overexpressed in many tumor phenotypes. Exploring this strategy offers a method in tumor targeting for cancers such as glioblastoma multiforme, pancreatic, lung, and breast based on the manifold of receptors overexpressed on various tumor cell populations. In this review, we offer a comprehensive summary of peptide-functionalized liposomes for receptor-targeted cancer therapy.

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“…To identify novel peptides targeting malignant gliomas, Wang et al used a 12-mer peptide phage display library and obtained the peptide (VTWTPQAWFQWV) bound to U87MG cells. In addition, the VTW phage is bound strongly to other human glioma cell lines, including H4, SW1088, and SW1783 (85)(86)(87).…”

Section: In Vitro Panningmentioning

confidence: 99%

Filamentous Bacteriophage—A Powerful Carrier for Glioma Therapy

et al. 2021

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Glioma is a life-threatening malignant tumor. Resistance to traditional treatments and tumor recurrence present major challenges in treating and managing this disease, consequently, new therapeutic strategies must be developed. Crossing the blood-brain barrier (BBB) is another challenge for most drug vectors and therapy medications. Filamentous bacteriophage can enter the brain across the BBB. Compared to traditional drug vectors, phage-based drugs offer thermodynamic stability, biocompatibility, homogeneity, high carrying capacity, self-assembly, scalability, and low toxicity. Tumor-targeting peptides from phage library and phages displaying targeting peptides are ideal drug delivery agents. This review summarized recent studies on phage-based glioma therapy and shed light on the developing therapeutics phage in the personalized treatment of glioma.

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Synthesis of a high functionality and quality lipid with gp130 binding hydrophobic peptide for the preparation of human glioma cell-targeted PEGylated liposomes

Cited by 15 publications

References 19 publications

Microfluidic Post-Insertion Method for the Efficient Preparation of PEGylated Liposomes Using High Functionality and Quality Lipids

Microfluidic Post-Insertion Method for the Efficient Preparation of PEGylated Liposomes Using High Functionality and Quality Lipids

Peptide functionalized liposomes for receptor targeted cancer therapy

Filamentous Bacteriophage—A Powerful Carrier for Glioma Therapy

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