Estrogen release from metallic stent surface for the prevention of restenosis

• Published in: Journal of controlled release Vol. 92; no. 1; pp. 83 - 91
• Main Authors: Joung, Yoon Ki, Kim, Hyun Il, Kim, Sung Soo, Chung, Kwang Hoe, Jang, Yang Soo, Park, Ki Dong
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 19.09.2003; Elsevier
• Subjects: 17^b-estradiol; Biological and medical sciences; Delayed-Action Preparations - administration & dosage; Delayed-Action Preparations - pharmacokinetics; Estrogen immobilization; Estrogen-releasing stent; estrogens; Estrogens - administration & dosage; Estrogens - chemistry; Estrogens - pharmacokinetics; General pharmacology; Graft Occlusion, Vascular - prevention & control; In vitro release; Medical sciences; Metallic stent; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Restenosis; stainless steel; Stainless Steel - chemistry; Stainless Steel - pharmacokinetics; Stents - adverse effects; Surface Properties - drug effects; Restenosis; In vitro release; Estrogen immobilization; Estrogen-releasing stent; Metallic stent; Stability; Pharmaceutical technology; Controlled release form; Estrogen; Immobilization; Cardiovascular disease; In vitro; Stent; Prevention; Vascular disease; Stainless steel; Dosage form; Active ingredient; Release
• ISSN: 0168-3659; 1873-4995
• DOI: 10.1016/S0168-3659(03)00305-5

For the prevention of coronary restenosis, estrogen was coupled onto a metallic stent and in vitro release of estrogen was investigated. Estrogen was introduced to the metal surface using a hydrolysable covalent bond for local sustained delivery of drug as follows: (i) the stainless steel (SS) surface was activated with silane by plasma polymerization, (ii) the activated surface (SS–Si surface) was treated with acrylic acid by plasma polymerization (SS–Si–AAc surface), and (iii) 17β-estradiol (E 2) was covalently linked to the carboxyl group on that surface (SS–Si–AAc–E 2 surface). The modified surfaces were characterized by X-ray photoelectron spectroscopy (XPS), Fourier transform infrared (FT-IR) spectroscopy, and water contact angle measurement. The amount of E 2 was measured by UV–visible spectrophotometry and high performance liquid chromatography (HPLC). The in vitro release profile of E 2 demonstrated sustained release of E 2 in aqueous buffer. In summary, a novel method of immobilizing estrogen onto a metallic stent surface using plasma polymerization has been developed. The obtained results attest to the usefulness of the estrogen-releasing stent for preventing restenosis.