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[1]Stone GW, Moses JW, Ellis SG, Schofer J, Dawkins KD, Morice MC, Colombo A, Schampaert E, Grube E, Kirtane AJ, Cutlip DE, Fahy M, Pocock SJ, Mehran R, Leon MB. Safety and efficacy of sirolimus-and paclitaxel-eluting coronary stents. N Engl J Med 356, 998–1008 (2007)
[2]Lemos PA, Serruys PW, Sousa JE. Drug-eluting stents: cost versus clinical benefit. Circulation 107, 3003–3007 (2003)
[3]Morice MC, Serruys PW, Sousa JE, Fajadet J, Ban Hayashi E, Perin M, Colombo A, Schuler G, Barragan P, Guagliumi G, Molnàr F, Falotico R. A randomized comparison of a sirolimus-eluting stent with a standard stent for coronary revascularization. N Engl J Med 346, 1773–1780 (2002)
[4]Grube E, Silber S, Hauptmann KE, Mueller R, Buellesfeld L, Gerckens U, Russell ME. TAXUS I: six-and twelve-month results from a randomized, double-blind trial on a slow release paclitaxel-eluting stent for de novo coronary lesions. Circulation 107, 38–42 (2003)
[5]Stone GW, Ellis SG, Cox DA, Hermiller J, O’Shaughnessy C, Mann JT, Turco M, Caputo R, Bergin P, Greenberg J, Popma JJ, Russell ME. A polymer-based, paclitaxel-eluting stent in patients with coronary artery disease. N Engl J Med 350, 221–231 (2004)
[6]Camendiz E, Steg PG, Wijns W. Stent thrombosis late after implantation of first-generation drug-eluting stents: cause for concern. Circulation 115, 1440–1455 (2007)
[7]Grube E, Buellesfeld L. BioMatrix Biolimus A9-eluting coronary stent: a next-generation drug-eluting stent for coronary artery disease. Exp Rev Med Dev 3, 731–741 (2006)
[8]Grundeken MJD, Wykrzykowska JJ. Biolimus-eluting stent with biodegradable polymer: one step forward in the fight against stent thrombosis vulnerability? Interv Cardiol 4, 11–25 (2012)
[9]Pendyala LK, Matsumoto D, Shinke T, Iwasaki T, Sugimoto R, Hou D, Chen JP, Singh J, King SB 3rd, Chronos N, Li J. Nobori stent shows less vascular inflammation and early recovery of endothelial function compared with cypher stent. JACC Cardiovasc Intv 5, 436–444 (2012)
[10]Cai Q, Bei JZ, Wang SG. Study on the Biocompatibility and Degradation Behavior of Poly-(l-lactide-co-glycolide) in vitro and in vivo. J Funct Polym 13, 249–254(2000)
[11]Cai Q, Bei JZ, Luo AQ, Wang SG. Biodegradation Behavior of Poly (lactide-co-glycolide) Agitated by Microorganism. Polym Degrad Stabil 71, 243–251 (2001)
[12]Cai Q, Shi GX, Bei JZ, Wang SG. Enzymatic degradation behavior and mechanism of Poly (lactide-co-glycolide) foams by Trypsin. Biomaterials 24, 629–638 (2003)
[13]Muthu MS. Nanoparticles based on PLGA and its co-polymer: An overview. Asian J Pharm 3, 266–273 (2009)
[14]de Scheerder I, Gershlick A, Chevalier B, Camenzind E, Vrints C, Reifart N, Missault L, Goy JJ, Urban P, Heldman A. The Elutes Clinical Study: 12-month clinical follow-up. Circulation 106, II–394. Abstract. (2002)
[15]Park SJ, Shim WH, Ho D, Raizner AE, Park SW, Hong MK, Lee CW, Choi D, Jang Y, Lam R, Weissman NJ, Mintz GS. A paclitaxel-eluting stent for the prevention of coronary restenosis. N Engl J Med 348, 1537–1545 (2003)
[16]Leon MB, Moses JW, Popma JJ, Fishell T, Wong SC, Midel M, Douglas J, Lambert C, Mooney M, Teirstein P. A multicenter randomized clinical study of the sirolimus-eluting stent in native coronary lesions: angiographic results. Circulation 106, II–393. Abstract. (2002)
[17]Sousa JE, Serruys PW, Costa MA. New frontiers in cardiology: drug eluting stents: part II. Circulation 107, 2383–2389 (2003)
[18]Sehgal SN. Rapamune (RAPA, rapamycin, sirolimus): mechanism of action immunosuppressive effect results from blockade of signal transduction and inhibition of cell cycle progression. Clin Biomech 31, 335–340 (1998)
[19]Sehgal SN. Rapamune (Sirolimus, rapamycin): an overview and mechanism of action. Ther Drug Monit 17, 660–665 (1995)
[20]Burke SE, Lubbers NL, Chen YW, Hsieh GC, Mollison KW, Luly JR, Wegner CD. Neointimal formation after balloon-induced vascular injury in Yucatan minipigs is reduced by oral rapamycin. J Cardiovasc Pharmacol 33, 829–835 (1999)
[21]MacDonald A, Scarola J, Burke JT, Zimmerman JJ. Clinical pharmacokinetics and therapeutic drug monitoring of sirolimus. Clin Ther 22, B101–121 (2000)
[22]Groth CG, Backman L, Morales JM, Calne R, Kreis H, Lang P, Touraine JL, Claesson K, Campistol JM, Durand D, Wramner L, Brattstrom C, Charpentier B. Sirolimus (rapamycin)-based therapy in human renal transplantation: similar efficacy and different toxicity compared with cyclosporine. Sirolimus European Renal Transplant Study Group. Transplantation 67, 1036–1042 (1999)
[23]Zhang H, Deng W, Wang X, Wang S, Ge J, Toft E. Solely abluminal drug release from coronary stents could possibly improve reendothelialization. Catheter Cardiovasc Interv (2013)
[24]Langer R, Brown L, Edelman E. Controlled release and magnetically modulated release systems for macromolecules. Methods Enzymol 112, 399–422 (1985)
[25]Parker T, Dave V, Falotico R. Polymers for drug eluting stents. Curr Pharm Des 16, 3978–3988 (2010)
[26]Otsuka Y, Saito S, Nakamura M, Shuto H, Mitsudo K. Comparison of pharmacokinetics of the limus-eluting stents in Japanese patients. Catheter Cardiovasc Interv 78, 1078–1085 (2011)
[27]Minami Y, Kaneda H, Inoue M, Ikutomi M, Morita T, Nakajima T. Endothelial dysfunction following drug-eluting stent implantation: a systematic review of the literature. Int J Cardiol 165, 222–228 (2012)
[28]Schwartz RS, Murphy JG, Edwards WD, Camrud AR, Vliestra RE, Holmes DR. Restenosis after balloon angioplasty. A practical proliferative model in porcine coronary arteries. Circulation 82(6), 2190–2200 (1990)
[29]Schwartz RS, Chu A, Edwards WD, Srivatsa SS, Simari RD, Isner JM, Holmes DR Jr. A proliferation analysis of arterial neointimal hyperplasia: lessons for antiproliferative restenosis therapies. Int J Cardiol 53, 71–80(1996)
[30]Rodriguez-Granillo A, Rubilar B, Rodriguez-Granillo G, Rodriguez AE. Advantages and disadvantages of biodegradable platforms in drug eluting stents. World J Cardiol 3, 84–92 (2011)
[31]Kastrati A, Mehilli J, Dirschinger J, Dotzer F, Schuhlen H, Neumann F-J, Fleckenstein M, Pfafferott C, Seyfarth M, Schomig A. Intracoronary stenting and angiographic results: strut thickness effect on restenosis outcome (ISAR-STEREO) trial. Circulation 103, 2816–2821 (2001)
[32]Pache J, Kastrati A, Mehilli J, Schuhlen H, Dotzer F, Hausleiter J, Fleckenstein M, Neumann FJ, Sattelberger U, Schmitt C, Muller M, Dirschinger J, Schomig A. Intracoronary stenting and angiographic results: strut thickness effect on restenosis outcome (ISAR-STEREO-2) trial. J Am Coll Cardiol 41, 1283–1288 (2003)
[33]Iijima R, Ikari Y, Miyazawa A, Nakajima H, Hara K. Predictors of restenosis after implantation of 2.5. mm stents in small coronary arteries. Circ J 68, 236–240 (2004)
[34]Schofer J, Schlüter M, Gershlick AH, Wijns W, García E, Schampaert E, Breithardt G. Sirolimus eluting stents for treatment of patients with long atherosclerotic lesions in small coronary arteries: double-blind, randomised controlled trial (E-SIRIUS). Lancet 362, 1093–1099 (2003)
[35]Muramatsu T, Tsukahara R, Ho M, Ito Y, Ishimori H, Hirano K, Nakano M, Matsushita M, Leung W. Clinical outcome of stent implantation in small coronary arteries using different type of coronary stents. J Invasive Cardiol 13, 634–639(2001)
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Frontiers in Bioscience-Landmark (FBL) is published by IMR Press from Volume 26 Issue 5 (2021). Previous articles were published by another publisher on a subscription basis, and they are hosted by IMR Press on imrpress.com as a courtesy and upon agreement with Frontiers in Bioscience.
Drug release kinetics from a drug-eluting stent with asymmetrical coat
1 Department of Health Science and Technology, Faculty of Medicine, Aalborg University, Niels Jernes Vej 109220 Aalborgo, Denmark
2 Shanghai Institute of Cardiovascular Diseases, Zhongshan Hospital, Fudan University, 180 Fenglin Road, 200032 Shanghai, China
3 Shengjing Hospital of China Medical University, 36 Sanhao Street, Heping District, 110004 Shenyang, China
4 Key Laboratory of Public Health Safety, Ministry of Education, School of Public Health, Fudan University, No.130, Dongan Road, 200032 Shanghai, China
5 Institute of Chemistry, Chinese Academy of Sciences, Zhongguancun North First Street 2, 100190 Beijing, China
6 Biomedical Research Center, College of Medicine, Qatar University, Shareh AIJamiaa, Postbox 2716, Doha, Qatar
Abstract
The aim of this study was to investigate the drug release profiles of biodegradable polymer sirolimus-or paclitaxel-eluting stents with asymmetrical coating (BPSES-A or BPPES-A) both in vitro and in vivo. In vitro, the drug release profile was characterized by measuring the drug concentration by HPLC over a time-course. In vivo, a porcine aorta stenting model was employed. The results showed that the drug release rates of BPSES-A and BPPES-A were slower, more stable and less burst releasing than those of conventionally coated stents (BPSES-C and BPPES-C respectively), both in vitro and in vivo. Based on the in vivo results, the sirolimus and paclitaxel content of the local coronary wall was maintained at a higher and more effective level with BPSES-A and BPPES-A than with BPSES-C and BPPES-C, respectively. The drug levels in peripheral tissue samples were below detection levels. These data demonstrated the effectiveness of both sirolimus and paclitaxel as stent coating agents, and revealed the favorable drug release kinetics and pharmacokinetics of asymmetrical coated stents compared with conventional coated stents.
Keywords
- Biodegradable Polymer
- Drug-eluting Stent
- Drug Release Kinetics
- Sirolimus
- Paclitaxel
References
- [1] Stone GW, Moses JW, Ellis SG, Schofer J, Dawkins KD, Morice MC, Colombo A, Schampaert E, Grube E, Kirtane AJ, Cutlip DE, Fahy M, Pocock SJ, Mehran R, Leon MB. Safety and efficacy of sirolimus-and paclitaxel-eluting coronary stents. N Engl J Med 356, 998–1008 (2007)
- [2] Lemos PA, Serruys PW, Sousa JE. Drug-eluting stents: cost versus clinical benefit. Circulation 107, 3003–3007 (2003)
- [3] Morice MC, Serruys PW, Sousa JE, Fajadet J, Ban Hayashi E, Perin M, Colombo A, Schuler G, Barragan P, Guagliumi G, Molnàr F, Falotico R. A randomized comparison of a sirolimus-eluting stent with a standard stent for coronary revascularization. N Engl J Med 346, 1773–1780 (2002)
- [4] Grube E, Silber S, Hauptmann KE, Mueller R, Buellesfeld L, Gerckens U, Russell ME. TAXUS I: six-and twelve-month results from a randomized, double-blind trial on a slow release paclitaxel-eluting stent for de novo coronary lesions. Circulation 107, 38–42 (2003)
- [5] Stone GW, Ellis SG, Cox DA, Hermiller J, O’Shaughnessy C, Mann JT, Turco M, Caputo R, Bergin P, Greenberg J, Popma JJ, Russell ME. A polymer-based, paclitaxel-eluting stent in patients with coronary artery disease. N Engl J Med 350, 221–231 (2004)
- [6] Camendiz E, Steg PG, Wijns W. Stent thrombosis late after implantation of first-generation drug-eluting stents: cause for concern. Circulation 115, 1440–1455 (2007)
- [7] Grube E, Buellesfeld L. BioMatrix Biolimus A9-eluting coronary stent: a next-generation drug-eluting stent for coronary artery disease. Exp Rev Med Dev 3, 731–741 (2006)
- [8] Grundeken MJD, Wykrzykowska JJ. Biolimus-eluting stent with biodegradable polymer: one step forward in the fight against stent thrombosis vulnerability? Interv Cardiol 4, 11–25 (2012)
- [9] Pendyala LK, Matsumoto D, Shinke T, Iwasaki T, Sugimoto R, Hou D, Chen JP, Singh J, King SB 3rd, Chronos N, Li J. Nobori stent shows less vascular inflammation and early recovery of endothelial function compared with cypher stent. JACC Cardiovasc Intv 5, 436–444 (2012)
- [10] Cai Q, Bei JZ, Wang SG. Study on the Biocompatibility and Degradation Behavior of Poly-(l-lactide-co-glycolide) in vitro and in vivo. J Funct Polym 13, 249–254(2000)
- [11] Cai Q, Bei JZ, Luo AQ, Wang SG. Biodegradation Behavior of Poly (lactide-co-glycolide) Agitated by Microorganism. Polym Degrad Stabil 71, 243–251 (2001)
- [12] Cai Q, Shi GX, Bei JZ, Wang SG. Enzymatic degradation behavior and mechanism of Poly (lactide-co-glycolide) foams by Trypsin. Biomaterials 24, 629–638 (2003)
- [13] Muthu MS. Nanoparticles based on PLGA and its co-polymer: An overview. Asian J Pharm 3, 266–273 (2009)
- [14] de Scheerder I, Gershlick A, Chevalier B, Camenzind E, Vrints C, Reifart N, Missault L, Goy JJ, Urban P, Heldman A. The Elutes Clinical Study: 12-month clinical follow-up. Circulation 106, II–394. Abstract. (2002)
- [15] Park SJ, Shim WH, Ho D, Raizner AE, Park SW, Hong MK, Lee CW, Choi D, Jang Y, Lam R, Weissman NJ, Mintz GS. A paclitaxel-eluting stent for the prevention of coronary restenosis. N Engl J Med 348, 1537–1545 (2003)
- [16] Leon MB, Moses JW, Popma JJ, Fishell T, Wong SC, Midel M, Douglas J, Lambert C, Mooney M, Teirstein P. A multicenter randomized clinical study of the sirolimus-eluting stent in native coronary lesions: angiographic results. Circulation 106, II–393. Abstract. (2002)
- [17] Sousa JE, Serruys PW, Costa MA. New frontiers in cardiology: drug eluting stents: part II. Circulation 107, 2383–2389 (2003)
- [18] Sehgal SN. Rapamune (RAPA, rapamycin, sirolimus): mechanism of action immunosuppressive effect results from blockade of signal transduction and inhibition of cell cycle progression. Clin Biomech 31, 335–340 (1998)
- [19] Sehgal SN. Rapamune (Sirolimus, rapamycin): an overview and mechanism of action. Ther Drug Monit 17, 660–665 (1995)
- [20] Burke SE, Lubbers NL, Chen YW, Hsieh GC, Mollison KW, Luly JR, Wegner CD. Neointimal formation after balloon-induced vascular injury in Yucatan minipigs is reduced by oral rapamycin. J Cardiovasc Pharmacol 33, 829–835 (1999)
- [21] MacDonald A, Scarola J, Burke JT, Zimmerman JJ. Clinical pharmacokinetics and therapeutic drug monitoring of sirolimus. Clin Ther 22, B101–121 (2000)
- [22] Groth CG, Backman L, Morales JM, Calne R, Kreis H, Lang P, Touraine JL, Claesson K, Campistol JM, Durand D, Wramner L, Brattstrom C, Charpentier B. Sirolimus (rapamycin)-based therapy in human renal transplantation: similar efficacy and different toxicity compared with cyclosporine. Sirolimus European Renal Transplant Study Group. Transplantation 67, 1036–1042 (1999)
- [23] Zhang H, Deng W, Wang X, Wang S, Ge J, Toft E. Solely abluminal drug release from coronary stents could possibly improve reendothelialization. Catheter Cardiovasc Interv (2013)
- [24] Langer R, Brown L, Edelman E. Controlled release and magnetically modulated release systems for macromolecules. Methods Enzymol 112, 399–422 (1985)
- [25] Parker T, Dave V, Falotico R. Polymers for drug eluting stents. Curr Pharm Des 16, 3978–3988 (2010)
- [26] Otsuka Y, Saito S, Nakamura M, Shuto H, Mitsudo K. Comparison of pharmacokinetics of the limus-eluting stents in Japanese patients. Catheter Cardiovasc Interv 78, 1078–1085 (2011)
- [27] Minami Y, Kaneda H, Inoue M, Ikutomi M, Morita T, Nakajima T. Endothelial dysfunction following drug-eluting stent implantation: a systematic review of the literature. Int J Cardiol 165, 222–228 (2012)
- [28] Schwartz RS, Murphy JG, Edwards WD, Camrud AR, Vliestra RE, Holmes DR. Restenosis after balloon angioplasty. A practical proliferative model in porcine coronary arteries. Circulation 82(6), 2190–2200 (1990)
- [29] Schwartz RS, Chu A, Edwards WD, Srivatsa SS, Simari RD, Isner JM, Holmes DR Jr. A proliferation analysis of arterial neointimal hyperplasia: lessons for antiproliferative restenosis therapies. Int J Cardiol 53, 71–80(1996)
- [30] Rodriguez-Granillo A, Rubilar B, Rodriguez-Granillo G, Rodriguez AE. Advantages and disadvantages of biodegradable platforms in drug eluting stents. World J Cardiol 3, 84–92 (2011)
- [31] Kastrati A, Mehilli J, Dirschinger J, Dotzer F, Schuhlen H, Neumann F-J, Fleckenstein M, Pfafferott C, Seyfarth M, Schomig A. Intracoronary stenting and angiographic results: strut thickness effect on restenosis outcome (ISAR-STEREO) trial. Circulation 103, 2816–2821 (2001)
- [32] Pache J, Kastrati A, Mehilli J, Schuhlen H, Dotzer F, Hausleiter J, Fleckenstein M, Neumann FJ, Sattelberger U, Schmitt C, Muller M, Dirschinger J, Schomig A. Intracoronary stenting and angiographic results: strut thickness effect on restenosis outcome (ISAR-STEREO-2) trial. J Am Coll Cardiol 41, 1283–1288 (2003)
- [33] Iijima R, Ikari Y, Miyazawa A, Nakajima H, Hara K. Predictors of restenosis after implantation of 2.5. mm stents in small coronary arteries. Circ J 68, 236–240 (2004)
- [34] Schofer J, Schlüter M, Gershlick AH, Wijns W, García E, Schampaert E, Breithardt G. Sirolimus eluting stents for treatment of patients with long atherosclerotic lesions in small coronary arteries: double-blind, randomised controlled trial (E-SIRIUS). Lancet 362, 1093–1099 (2003)
- [35] Muramatsu T, Tsukahara R, Ho M, Ito Y, Ishimori H, Hirano K, Nakano M, Matsushita M, Leung W. Clinical outcome of stent implantation in small coronary arteries using different type of coronary stents. J Invasive Cardiol 13, 634–639(2001)
