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Published on: August 31, 2019
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Optimization of RGD-modified Nano-liposomes Encapsulating Eptifibatide
Hassan Bardania1, Seyed Abbas Shojaosadati2, Farzad Kobarfard3
1Department of Nanobiotechnology, Faculty of Biological Sciences, Tarbiat Modares University, Tehran, Iran.
Iranian Journal of Biotechnology
|September 30, 2017
Summary
Optimizing nano-liposome delivery of eptifibatide, a peptide drug, enhanced its encapsulation efficiency. Sodium lauryl sulfate increased drug release but not encapsulation in RGD-modified nano-liposomes.
Area of Science:
- Nanotechnology
- Pharmaceutical Sciences
- Biochemistry
Background:
- Eptifibatide is an effective intravenous peptide drug targeting platelet GP IIb/IIIa receptors.
- Its short half-life necessitates improved delivery systems, like nano-liposomes, for targeted thrombus treatment.
Purpose of the Study:
- To optimize the encapsulation efficiency of eptifibatide into Arg-Gly-Asp (RGD)-modified nano-liposomes (RMNL).
- To evaluate the impact of sodium lauryl sulfate (SLS) on eptifibatide release from RMNL.
Main Methods:
- Response surface methodology (RSM) was used to optimize five variables affecting drug entrapment efficiency (DEE).
- The influence of varying SLS concentrations on encapsulation and drug release was assessed.
- Nano-liposome size and morphology were characterized by transmission electron microscopy (TEM).
Main Results:
- Maximum DEE of 38% was achieved with specific concentrations of eptifibatide, DSPC, cholesterol, and dipalmitoyl-GRGDSPA peptide, along with 7 freeze/thaw cycles.
- Sodium lauryl sulfate significantly enhanced eptifibatide release from RMNL.
- SLS did not significantly affect the encapsulation efficiency.
Conclusions:
- Optimizing formulations for expensive peptide drugs is crucial for maximizing encapsulation efficiency.
- This approach minimizes experimental trials for valuable peptide drug formulations.
