Polyether polyurethane delivery systems. I. Evaluation of monolithic systems for N6-(Δ2-isopentenyl)adenosine

Autor: Bhaskar Chaudhuri, Adel H. Karara, Yunik Chang
Rok vydání: 1988
Předmět:
Zdroj: International Journal of Pharmaceutics. 42:117-122
ISSN: 0378-5173
DOI: 10.1016/0378-5173(88)90167-6
Popis: The nucleoside, N6-(Δ2-isopentenyl)adenosine (IPA) is reported to have inhibitory and cytotoxic properties against several types of cancer cells. The efficacy of this potent antileukemic agent is diminished by rapid enzymatic degradation in the body. In an effort to optimize the release properties of IPA, the drug was incorporated in polymeric delivery systems. Polyether-polyurethane was the polymer of choice because of its hydrophilic-hydrophobic character. Release studies from monolithic devices revealed linear relationships when the cumulative amount of IPA was plotted against the square root of time. IPA release from devices (1.12 mm thick) showed presence of lag time. In vitro L1210 cell culture studies showed that the IPA-polyether polyurethane devices maintained effective drug concentrations for ca. 100 h. Compared to conventional solutions, the polymeric system was more effective in controlling cell proliferation. Almost total cell death occurred when IPA was released at controlled rates due to increased contact time. Results of this study indicate that effective in-vitro antileukemic activity was obtained by the prepared polymeric system.
Databáze: OpenAIRE