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In Vitro and In Vivo Evaluation of Targeted Sunitinib-Loaded Polymer Microbubbles Against Proliferation of Renal Cell
Jie Hu1, Yujin Zong1, Jun Li1
1Departments of Ultrasound (J.H., J.L., X.Z., J.Z., T.Z., H.S.) and Oral and Maxillofacial Surgery, School of Stomatology (B.B.), Xijing Hospital, Fourth Military Medical University, Xi'an, China; Department of Echocardiography, Affiliated Traditional Chinese Medicine Hospital, Xinjiang Medical University, Urumqi, China (J.H.); Key Laboratory of Biomedical Information Engineering of Ministry of Education, Department of Biomedical Engineering, School of Life Science and Technology, Xi'an Jiaotong University, Xi'an, China (Y.Z.); and Department of Biomedical Engineering, Urumqi General Hospital of Lanzhou Military Region, Urumqi, China (M.J.).
Objectives:
The poor safety profile of sunitinib capsules has encouraged the identification of targeted drug delivery systems against renal cell carcinoma. This study aimed to explore the effect of sunitinib-loaded microbubbles along with ultrasound (US) treatment on proliferation and apoptosis of human GRC-1 granulocyte renal carcinoma cells in vitro and in vivo (xenograft tumor growth in nude mice).
Methods:
Liposomes containing sunitinib were prepared by using the transmembrane ammonium sulfate gradient method and then absorbed into polymer microbubbles to generate sunitinib-loaded microbubbles. Entrapment of sunitinib was verified by 25-25-[N-[(7-nitro-2-1,3-benzoxadiazol-4-yl)methyl]amino]-27-norcholesterol staining. GRC-1 cells were treated with microbubbles alone, liposomes alone, sunitinib alone, sunitinib-loaded microbubbles without and with US, and no treatment (control). Cell survival and apoptosis were assessed at 12, 24, and 48 hours after treatment. Xenograft tumors were induced by implantation of GRC-1 cells in nude mice. The animals with tumors were then randomly assigned to sunitinib alone, sunitinib-loaded microbubbles - US, sunitinib-loaded microbubbles + US, and no treatment (control; n = 10 per group). The tumor volumes were analyzed on the 7th, 15th, and 21st days.
Results:
The sunitinib entrapment efficiency in the liposomes was approximately 78%. The effective sunitinib concentration in each group was 0.1 μg/mL. The sunitinib-loaded microbubble + US group showed a lower in vitro cell survival rate (P < .001) compared with the other groups. Greater in vivo inhibition of xenograft tumor growth was also observed in the sunitinib-loaded microbubble + US group compared with the other groups.
Conclusions:
Combined sunitinib-loaded microbubbles and US treatment significantly inhibits growth of renal carcinoma cells both in vitro and in vivo.
Insights
Sunitinib-loaded microbubbles combined with ultrasound treatment effectively inhibit renal cell carcinoma growth. This targeted approach reduces cancer cell survival and tumor progression in vitro and in vivo.
Area of Science:
- Oncology
- Biotechnology
- Nanomedicine
Background:
- Sunitinib, a targeted therapy for renal cell carcinoma (RCC), has a poor safety profile.
- Development of targeted drug delivery systems is crucial for improving RCC treatment efficacy and safety.
- Microbubbles offer a potential platform for localized drug delivery.
Purpose of the Study:
- To evaluate the efficacy of sunitinib-loaded microbubbles combined with ultrasound (US) treatment.
- To assess the impact on proliferation and apoptosis of GRC-1 renal carcinoma cells.
- To investigate the effects on in vitro and in vivo xenograft tumor growth.
Main Methods:
- Sunitinib was encapsulated in liposomes and then incorporated into polymer microbubbles.
- GRC-1 cells and nude mouse xenografts were treated with various combinations: microbubbles, liposomes, sunitinib, sunitinib-loaded microbubbles with/without US.
- Cell survival, apoptosis, and tumor volume were measured at specified time points.
Main Results:
- Sunitinib entrapment efficiency in liposomes was approximately 78%.
- The sunitinib-loaded microbubble + US group demonstrated significantly lower in vitro cell survival (P < .001).
- This combination therapy also showed significantly greater inhibition of in vivo xenograft tumor growth.
Conclusions:
- Sunitinib-loaded microbubbles combined with ultrasound represent a potent strategy for renal cell carcinoma treatment.
- This approach significantly inhibits renal carcinoma cell proliferation and induces apoptosis.
- The combined therapy shows promise for both in vitro and in vivo applications in oncology.
