DSPE-PEG2000-Maleimide, a functional phosphatide-polyethylene glycol derivative, is an ideal candidate for the development of biocompatible biomaterials and drug delivery systems[1]. DSPE-PEG2000-Maleimide can be used to prepare liposome-polycation-oligonucleotides complexes by film hydration for systemic small interfering RNA (siRNA) delivery[2]. The novel nanoparticle based on DSPE-PEG2000-Maleimide showed significantly enhanced binding affinity and luciferase gene silencing activity against EGFR-overexpressing MDA-MB-231 breast cancer cells in vitro[2]. A novel maleimide bubble consisting of 90mol% DSPC, 7mol% DSPE-PEG2000, and 3mol% DSPE-PEG2000-Maleimide was used to simulate adhesion of the target bubble, the in vitro model of adherent bubbles based on DSPE-PEG2000-Maleimide can be used to study ultrasound targeted imaging[3]. DSPE–PEG2000–iRGD was synthesized by coupling iRGD peptides to DSPE–PEG2000–maleimide, whose fabrication of the iRGD-carrying αvβ3 integrin-targeted microbubbles, this DSPE–PEG2000–maleimide-based ultrasound contrast agent is widely used for molecular imaging of tumor angiogenesis[4]. The maleimide-thiol Michael addition, Aizde-DBCO (Dibenzocyclooctyne), and TCO (trans-cycloctene)-Tetrazine click chemistry were employed to conjugate three different proteins, subunit keyhole limpet hemocyanin (sKLH), Ovalbumin (OVA), and cross-reactive material 197 (CRM197), to the surface of PLGA/lipid hybrid nanoparticles (hNPs), which are useful for developing multivalent vaccines against different pathogens. Three proteins including subunit keyhole limpet hemocyanin (sKLH), Ovalbumin (OVA) and cross-reactive material 197 (CRM197) were attached to the DSPE-PEG2000-Maleimide-based PLGA/lipid hybrid nanoparticles (hNPs) through maleimide-thiol Michael addition, Aizde-DBCO (Dibenzocyclooctyne), and TCO (trans-cycloctene)-Tetrazine click chemistry to create multivalent vaccines against various pathogens[5].
References:
[1] Kang S T, Yeh C K. A maleimide-based in-vitro model for ultrasound targeted imaging[J]. Ultrasonics sonochemistry, 2011, 18(1): 327-333.
[2] Gao J, Liu W, Xia Y, et al. The promotion of siRNA delivery to breast cancer overexpressing epidermal growth factor receptor through anti-EGFR antibody conjugation by immunoliposomes[J]. Biomaterials, 2011, 32(13): 3459-3470.
[3] Kang S T, Yeh C K. A maleimide-based in-vitro model for ultrasound targeted imaging[J]. Ultrasonics sonochemistry, 2011, 18(1): 327-333.
[4] Yan F, Xu X, Chen Y, et al. A lipopeptide-based αvβ3 integrin-targeted ultrasound contrast agent for molecular imaging of tumor angiogenesis[J]. Ultrasound in medicine & biology, 2015, 41(10): 2765-2773.
[5] Hu H, Zhang C. Conjugation of Multiple Proteins Onto the Surface of PLGA/Lipid Hybrid Nanoparticles[J]. Journal of Biomedical Materials Research Part A, 2025, 113(1): e37807.