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The Synthesis of RGD-functionalized Hydrogels as a Tool for Therapeutic Applications
Published on: October 7, 2016
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Cyclic RGD functionalized liposomes encapsulating urokinase for thrombolysis
Nengpan Zhang1, Chunlin Li2, Dayong Zhou3
1School of Nano Technology and Nano Bionics, University of Science and Technology of China, Hefei 230026, China; CAS Key Laboratory of Nano-Bio Interface, Suzhou Institute of Nano-Tech and Nano-Bionics, Chinese Academy of Sciences, Suzhou 215123, China.
Acta Biomaterialia
|February 8, 2018
Summary
Targeted thrombolysis using cyclic RGD (cRGD) functionalized liposomes improved urokinase efficacy. These liposomes bind activated platelets, enhancing drug delivery and reducing dosage by 75% for effective thrombosis treatment.
Area of Science:
- Biomedical Engineering
- Nanotechnology
- Pharmacology
Background:
- Thrombosis is a major cause of morbidity and mortality, often treated with thrombolytic drugs.
- Current thrombolytic therapies have limitations including short plasma half-life and systemic side effects.
- Urokinase is a widely used thrombolytic agent, but its clinical efficacy can be improved.
Purpose of the Study:
- To develop and evaluate cyclic RGD (cRGD) functionalized liposomes for targeted delivery of urokinase.
- To enhance thrombolytic efficacy and reduce systemic side effects of urokinase.
- To investigate the binding specificity and drug release characteristics of cRGD-urokinase liposomes.
Main Methods:
- Preparation of cRGD functionalized liposomes encapsulating urokinase.
- Flow cytometry to assess binding of cRGD liposomes to activated platelets.
- In vitro release studies to determine urokinase release kinetics.
- In vitro and in vivo thrombolysis experiments using a mouse mesenteric thrombosis model.
Main Results:
- cRGD liposomes specifically bind to activated platelets, not resting platelets.
- Urokinase release from liposomes reached a plateau around 5 hours with 60% release.
- In vitro experiments showed good thrombolysis potential for cRGD-urokinase liposomes.
- In vivo studies demonstrated a 75% dose reduction of urokinase with equivalent thrombolytic effect compared to free urokinase.
- cRGD liposomes improved thrombolytic efficacy by approximately 4-fold over free urokinase.
Conclusions:
- cRGD functionalized liposomes offer a promising strategy for targeted thrombolysis.
- Encapsulating urokinase in cRGD liposomes enhances its therapeutic efficacy and reduces required dosage.
- This targeted drug delivery system holds significant potential for clinical application in treating thrombosis.
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