Bivalirudin and sirolimus co-eluting coronary stent: Potential strategy for the prevention of stent thrombosis and restenosis
Basic science / drug development published in Int J Pharm (2021)
Abstract
Localized drug delivery with sustained elution characteristics from nanocarrier coated stents represents a viable therapeutic approach to circumvent concerns related to coronary stent therapy. We fabricated a Sirolimus (SRL) and Bivalirudin (BIV) releasing nanoparticles (NPs) coated stent for concurrent mitigation of vascular restenosis and acute stent thrombosis. SRL NPs were prepared by nanoprecipitation method whereas the BIV vesicles were generated using hydrophobic ion pair approach followed by micellization phenomenon. MTT assay and confocal microscopic analysis indicated superior anti-proliferative activity and higher cellular uptake of SRL NPs into human coronary artery smooth muscle cells, respectively. DSC and ATR-FTIR techniques confirmed the formation of complex between BIV and phosphatidylglycerol via some weak physical interactions. More than 2 fold rise in log P value was obtained for DSPG-BIV at 3:1 M ratio compared with native BIV solution. The SAXS analysis indicated formation of oligolamellar vesicles of DSPG-BIV complex which was preferentially entrapped into lipophilic lamellae of vesicles. APTT, PT, and TT tests revealed that the BIV vesicles caused significant prolongation of clotting time compared to native BIV solution. The SEM analysis showed uniform and defect free stent coating. In vitro release study demonstrated that SRL and BIV were eluted in a sustained manner from coated stents.
Abstract sourced from PubMed (NCBI) for the cited record. See the original publication for the authoritative version.
Summary
Bivalirudin and sirolimus dual-drug-eluting coronary stent using nanoprecipitation and hydrophobic-ion-pair vesicle formulations. Sustained release achieves anti-restenosis and antithrombotic activity from stent surface.
Why This Matters for Hirudotherapy
This study fabricated a coronary stent coated with sirolimus nanoparticles and bivalirudin vesicles for concurrent prevention of restenosis and acute stent thrombosis. Bivalirudin was complexed with phosphatidylglycerol via hydrophobic ion pairing, producing oligolamellar vesicles with enhanced lipophilicity and sustained clotting-time prolongation (APTT, PT, TT) compared to native bivalirudin solution. Sirolimus nanoparticles showed anti-proliferative activity and cellular uptake in human coronary artery smooth muscle cells, and both drugs eluted in a sustained manner from the coated stent. For ASH's domain, the connection to leech therapy or the leech secretome is indirect at best: the abstract itself makes no mention of leeches, hirudin, or hirudotherapy, though bivalirudin is indexed under the MeSH term 'Hirudins.' The honest caveat is that this is an in vitro materials and formulation study with no in vivo or clinical data, and the abstract provides no basis for leech-product or hirudotherapy claims.
Citation
Bivalirudin and sirolimus co-eluting coronary stent: Potential strategy for the prevention of stent thrombosis and restenosis.
Sane M et al. · International journal of pharmaceutics, 2021
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