title: Cisplatin-conjugated porous gelatin particles: assessment of optimal conditions for binding and release.
abstract: This study was designed to evaluate the optimal conditions for binding cisplatin and porous gelatin particles (PGPs) and to establish in vivo drug release pharmacokinetics. PGPs were immersed in cisplatin solutions under different conditions: concentration, immersion time, and temperature. Thereafter, PGPs were washed in distilled water to remove uncombined cisplatin and were then freeze-dried. The platinum concentration (PC) in the PGPs was then measured. For the in vivo release test, 50 mg/kg of the cisplatin-conjugated PGPs was implanted subcutaneously in the abdominal region of two rabbits. PCs in the blood were measured at different time intervals. PCs significantly increased in direct proportion to the concentration and immersion time (p < 0.01). Although PC increased at higher solution temperature, it was not a linear progression. For the in vivo release test, platinum was released from cisplatin-conjugated PGPs after 1 day, and the peak PC was confirmed 2 days after implantation. Platinum in the blood was detected until 7 days after implantation in one rabbit and 15 days after administration in the other rabbit. Platinum binding with PGPs increased with a higher concentration of cisplatin solution at a higher temperature over a longer duration of time. Release of cisplatin from cisplatin-conjugated PGPs was confirmed in vivo.
authors.affiliation: Department of Radiology, Shiga University of Medical Science, Seta Tsukinowa-cho, Otsu City, 520-2192 Shiga, Japan. junryuhei@yahoo.co.jp
authors.forename: Shinichi
authors.initials: S
authors.lastname: Ohta
authors.forename: Norihisa
authors.initials: N
authors.lastname: Nitta
authors.forename: Akinaga
authors.initials: A
authors.lastname: Sonoda
authors.forename: Ayumi
authors.initials: A
authors.lastname: Nitta-Seko
authors.forename: Toyohiko
authors.initials: T
authors.lastname: Tanaka
authors.forename: Masashi
authors.initials: M
authors.lastname: Takahashi
authors.forename: Kiyoshi
authors.initials: K
authors.lastname: Murata
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D002945:Cisplatin / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D004337:Drug Carriers; D005260:Female; D005780:Gelatin; D008863:Microspheres; D010984:Platinum / Q000032:analysis / Q000097:blood; D011817:Rabbits; D013696:Temperature; D013997:Time Factors
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D010984:Platinum; D005780:Gelatin; D002945:Cisplatin