Liposomes Combined an Integrin αvβ3-Specific Vector with pH-Responsible Cell-Penetrating Property for Highly Effective Antiglioma Therapy through the Blood–Brain Barrier

• DOI: 10.1021/acsami.5b06429
• Publication Date: 2015-09-15T14:53:35Z
• Authors: Kairong Shi; Yang Long; Chaoqun Xu; Yang Wang; Yue Qiu; Qianwen Yu; Yayuan Liu; Qianyu Zhang; Huile Gao; Zhirong Zhang; Qin He
• Keywords: Nanocarriers; Vasculogenic mimicry; Cell-penetrating peptide; Brain tumor

Glioma, one of the most common aggressive malignancies, has highest mortality in present world. Delivery nanocarriers from systemic circulation to glioma sites would encounter multiple physiological and biological barriers, such as blood–brain barrier (BBB) poor penetration into tumor. To circumvent these hurdles, paclitaxel-loaded liposomes were developed by conjugating with a TR peptide (PTX-TR-Lip), integrin αvβ3-specific vector pH-responsible cell-penetrating property, for transporting drug across BBB then delivering glioma. Surface plasmon resonance (SPR) studies confirmed very high affinity TR-Lip αvβ3. In vitro results showed that exhibited strong transport ability BBB, killed cells brain cancer stem (CSCs), destroyed vasculogenic mimicry (VM) channels. vivo demonstrated could better target glioma, eliminated CSCs VM channels tumor tissues. The median survival time tumor-bearing mice after administering PTX-TR-Lip (45 days) was significantly longer than giving free PTX (25.5 days, p < 0.001) or other controls. conclusion, improve therapeutic efficacy vivo.