@article {YUAN237, author = {BO YUAN and YARONG ZHAO and SHIYAN DONG and YATING SUN and FEI HAO and JING XIE and LESHENG TENG and ROBERT J. LEE and YAOWEN FU and YE BI}, title = {Cell-penetrating Peptide-coated Liposomes for Drug Delivery Across the Blood{\textendash}Brain Barrier}, volume = {39}, number = {1}, pages = {237--243}, year = {2019}, doi = {10.21873/anticanres.13103}, publisher = {International Institute of Anticancer Research}, abstract = {Background/Aim: Glioma is a deadly form of brain cancer. Doxorubicin is cytotoxic against glioma cells. However, the blood-brain barrier (BBB) limits its ability to be delivered to the brain. Materials and Methods: Liposomes (R8PLP) formed from, 1,2-dioleoyl-3-trimethylammonium-propane chloride (DOTAP), 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy-(polyethylene glycol)-2000] (PEG-DSPE), cholesterol and egg phosphatidylcholine (ePC) were modified by cell-penetrating peptide R8 conjugated with oleic acid as a novel method for delivering doxorubicin. The antitumor effect of R8PLP was evaluated by uptake, cytotoxicity and brain accumulation. Results: The size of R8PLP was 95 nm. Doxorubicin was loaded into R8PLP by active loading with more than 95\% encapsulation efficiency. Cellular uptake of R8PLP by U87-MG cells was 8.6-fold higher than that of unmodified liposomes. R8PLP reduced cell viability by 16.18\% and 18.11\% compared to cholesterol-ePC-liposomes and free doxorubicin, respectively, at 3.6 μM after 24 h treatment. The biodistribution of doxorubicin in the brain was significantly improved by R8PLP. The area under the concentration-time curve (AUC0.5-12 h) of R8PLP was 2.4-times higher than that of cholesterol-ePC-PEG-DSPE-liposomes. Conclusion: These results suggest that R8-conjugated oleic acid-modified liposomes are effective delivery vehicles for glioma.}, issn = {0250-7005}, URL = {https://ar.iiarjournals.org/content/39/1/237}, eprint = {https://ar.iiarjournals.org/content/39/1/237.full.pdf}, journal = {Anticancer Research} }