RGD-MODIFIED SUNITINIB LIPOSOME TO IMPROVE THE THERAPEUTIC EFFICIENCY OF RENAL CARCINOMA

Huibing Li^1,2* Shimiao Zhu¹, Qi Li¹, Zongsu Zhang, Changyi Quan^1,*

¹Department of Urology, Tianjin Institute of Urology, The Secondary Hospital of Tianjin Medical University. No.23 Pingjiang road, Hexi district, Tianjin, 300211, China - ²Department of Urology, The First Affiliated Hospital, and College of Clinical Medicine of Henan University of Science and Technology, Luoyang 471003, China

Objective: Renal carcinoma is a very high degree of malignancy with a very high incidence and mortality. Angiogenesis of renal carcinoma is very important for tumor metastasis and prognosis. Inhibition of this process can be more effective against renal carcinoma. To overcome the limitations of sunitinib for treating renal carcinoma, in this study, we developed a RGD-modified liposomal drug delivery system.

Methods: The liposomes were prepared and characterized for particle size, zeta potential, encapsulation efficiency, release profile, stability, and hemolysis. The enhanced target and anti-angiogenesis effects were also studied in vitro and in vivo.

Results: The results suggested that the RGD-modified liposome (S/RGDL) obviously suppressed the proliferation capacity both in vitro and in vivo compared to naked sunitinib and non-coated liposome (S/L), which might be due to the dual-antiangiogenesis of both sunitinib and RGD peptide.

Conclusion: This work presented a way that S/RGDL may be used as potential means to improve the therapeutic efficiency of renal carcinoma via enhancing target and anti-angiogenesis ability.