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.
Resumen
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.
Por qué esto importa para la hirudoterapia
Este estudio fabricó un stent coronario recubierto con nanopartículas de sirolimus y vesículas de bivalirudina para la prevención concurrente de reestenosis y trombosis aguda del stent. La bivalirudina se complejó con fosfatidilglicerol mediante apareamiento iónico hidrofóbico, produciendo vesículas oligolamelares con mayor lipofilicidad y prolongación sostenida del tiempo de coagulación (TTPa, TP, TT) en comparación con la solución nativa de bivalirudina. Las nanopartículas de sirolimus mostraron actividad antiproliferativa y captación celular en células de músculo liso de arteria coronaria humana, y ambos fármacos se eluyeron de forma sostenida desde el stent recubierto. Para el dominio de la ASH, la conexión con la terapia con sanguijuelas o el secretoma de la sanguijuela es indirecta en el mejor de los casos: el resumen en sí no menciona sanguijuelas, hirudina ni hirudoterapia, aunque la bivalirudina está indexada bajo el término MeSH 'Hirudins'. La advertencia honesta es que se trata de un estudio in vitro de materiales y formulación sin datos in vivo ni clínicos, y el resumen no aporta base para afirmaciones sobre productos de sanguijuela o hirudoterapia.
Citación
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
Contexto clínico relacionado
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Añadido a la biblioteca ASH: May 27, 2026 · Última actualización del sitio: 18 de junio de 2026