{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"omics_type":["Unknown"],"volume":["33"],"submitter":["Ling C"],"pubmed_abstract":["Extremely low actual biological effect of insoluble small molecule drugs in ischemia region is a pain point and aporia in Ischemia Stroke (IS) therapy, Although there are studies on single, double-ligands modified liposomes or biomimetic exogenous carriers for directly targeting IS so far, but they often have off-target effects due to they were swallowed, degraded directly (instability) and sabotaged without the help of endogenous cell in the systemic circulation. DSPE-PEG<sub>3400</sub>-PGP (PGP) and DSPE-PEG<sub>3400</sub>-cRGD (cRGD) were synthesized via michael addition reaction of maleimide (-Mal) with sulfhydryl (-SH), succinimidyl ester (-NHS) with active primary amine group (-NH<sub>2</sub>) respectively. The cRGD and PGP were modified on liposomes by thin film hydration method. Optimal modified ratio of cRGD and PGP were achieved by cellular uptake of HL-60 cells and THP-1 cells <i>in vitro</i>. The precise targeting effects of cRGD/PGP-Lips were examined in a nude MCAO model by an in a vivo imaging system. Puerarin (Pue) was cleverly encapsulated using a calcium acetate gradient to construct cRGD/PGP-Pue-Lips, and its therapeutic efficiency were assessed by rat MCAO model of IS. Optimal modification ratio for both cRGD and PGP were 3 %. The cRGD/PGP-Lips had significant synergetic targeting efficiency <i>in vitro</i> and <i>in vivo</i>, and the encapsulation efficiency of Pue were greater than 80 % through calcium acetate gradient. The cRGD/PGP-Pue-Lips could effectively penetrate BBB and enhance Pue retention on the brain ischemia region <i>in vivo</i>, resulting in a nearly two-fold reduction significantly in cerebral infarction area and edema in rats. In addition, cRGD/PGP-Pue-Lips didn't cause systemic toxicity in major organ tissues. Precise dual-ligands modified nanocarrier targeting endogenous cells is highly competitive as a novel anti-stroke and perspective for treatment of IS."],"journal":["Materials today. Bio"],"pagination":["102077"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC12281153"],"repository":["biostudies-literature"],"pubmed_title":["Neutrophil/monocyte-targeted dual-ligands modified liposomes delivering puerarin for ischemia stroke treatment."],"pmcid":["PMC12281153"],"pubmed_authors":["Li X","Ling C","Yu C","Chen L","Liang J","Wei H","Wang J"],"additional_accession":[]},"is_claimable":false,"name":"Neutrophil/monocyte-targeted dual-ligands modified liposomes delivering puerarin for ischemia stroke treatment.","description":"Extremely low actual biological effect of insoluble small molecule drugs in ischemia region is a pain point and aporia in Ischemia Stroke (IS) therapy, Although there are studies on single, double-ligands modified liposomes or biomimetic exogenous carriers for directly targeting IS so far, but they often have off-target effects due to they were swallowed, degraded directly (instability) and sabotaged without the help of endogenous cell in the systemic circulation. DSPE-PEG<sub>3400</sub>-PGP (PGP) and DSPE-PEG<sub>3400</sub>-cRGD (cRGD) were synthesized via michael addition reaction of maleimide (-Mal) with sulfhydryl (-SH), succinimidyl ester (-NHS) with active primary amine group (-NH<sub>2</sub>) respectively. The cRGD and PGP were modified on liposomes by thin film hydration method. Optimal modified ratio of cRGD and PGP were achieved by cellular uptake of HL-60 cells and THP-1 cells <i>in vitro</i>. The precise targeting effects of cRGD/PGP-Lips were examined in a nude MCAO model by an in a vivo imaging system. Puerarin (Pue) was cleverly encapsulated using a calcium acetate gradient to construct cRGD/PGP-Pue-Lips, and its therapeutic efficiency were assessed by rat MCAO model of IS. Optimal modification ratio for both cRGD and PGP were 3 %. The cRGD/PGP-Lips had significant synergetic targeting efficiency <i>in vitro</i> and <i>in vivo</i>, and the encapsulation efficiency of Pue were greater than 80 % through calcium acetate gradient. The cRGD/PGP-Pue-Lips could effectively penetrate BBB and enhance Pue retention on the brain ischemia region <i>in vivo</i>, resulting in a nearly two-fold reduction significantly in cerebral infarction area and edema in rats. In addition, cRGD/PGP-Pue-Lips didn't cause systemic toxicity in major organ tissues. Precise dual-ligands modified nanocarrier targeting endogenous cells is highly competitive as a novel anti-stroke and perspective for treatment of IS.","dates":{"release":"2025-01-01T00:00:00Z","publication":"2025 Aug","modification":"2026-03-27T15:14:21.272Z","creation":"2025-08-23T03:09:04.791Z"},"accession":"S-EPMC12281153","cross_references":{"pubmed":["40697323"],"doi":["10.1016/j.mtbio.2025.102077"]}}