Transferrin and cell-penetrating peptide dual-functioned liposome for targeted drug delivery to glioma.
A brain drug delivery system for glioma chemotherapy based on transferrin and cell-penetrating peptide dual-functioned liposome, Tf/TAT-lip, was made and evaluated with doxorubicin (DOX) as a model drug. TAT conjugated liposome (TAT-lip) loaded with doxorubicin (DOX) were prepared by the thin film hydration methods (lip-DOX) and then conjugated with transferrin (Tf) to yield Tf/TAT-lip-DOX which was characterized for their various physicochemical and pharmaceutical properties. Cellular uptakes were explored in both brain capillary endothelial cells (BCECs) of rats and U87 cells. The blood brain barrier model in vitro was established to evaluate the trans-endothelial ability crossing the BBB. The biodistribution of each formulation was further identified. The Tf/TAT-lip-DOX presents the best anti-proliferative activity against U87 cells. The orthotropic glioma model was established for the evaluation of anti-glioma effect. In conclusion, the experimental data in vitro and in vivo indicated that the Tf/TAT-lip was a promising brain drug delivery system due to its high delivery efficiency across the BBB.
Affiliated Bayi Brain Hospital, Beijing Military Hospital, PLA and PhD Student Program of Southern Medical University Beijing, China ; Department of Neurosurgery, The Affiliated Hospital of Hainan Medical College Haikou, Hainan Province, China.
Chuanyi
C
Zheng
Department of Neurosurgery, The Affiliated Hospital of Hainan Medical College Haikou, Hainan Province, China.
Chunyang
C
Ma
Department of Neurosurgery, The Affiliated Hospital of Hainan Medical College Haikou, Hainan Province, China.
Enqi
E
Bai
Department of Neurosurgery, The Affiliated Hospital of Hainan Medical College Haikou, Hainan Province, China.
Kun
K
Yang
Affiliated Bayi Brain Hospital, Beijing Military Hospital, PLA and PhD Student Program of Southern Medical University Beijing, China.
Ruxiang
R
Xu
Dual-ligand; blood-brain barrier; cell penetrating peptide; liposome; transferrin receptor