These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Controlled release of a protein kinase inhibitor UCN-01 from liposomes influenced by the particle size.
    Author: Yamauchi M, Kusano H, Saito E, Abe M, Tsutsumi K, Uosaki Y, Nakakura M, Kato Y, Aoki N.
    Journal: Int J Pharm; 2008 Mar 03; 351(1-2):250-8. PubMed ID: 17904317.
    Abstract:
    A protein kinase inhibitor UCN-01 binds with high affinity to human alpha 1-acid glycoprotein (hAGP) which may compromise the drugs therapeutic effectiveness. Liposomal formulations of UCN-01 have been evaluated as a means of reducing the impact of binding to hAGP. However, in an initial study, UCN-01 was released rapidly from liposomes added to rat plasma containing hAGP. The purpose of this study was to develop a liposomal formulation of UCN-01 that only slowly released drug. Liposomes composed of lipids with a high phase transition temperature and having an average particle size of 120 nm and above reduced leaking of UCN-01 when the formulations were evaluated by adding to rat plasma containing hAGP. Furthermore, formulations composed of larger liposomes were also more effective in vivo; in tests in which liposomal preparations were injected together with hAGP into rats, more UCN-01 was retained in liposomes for 24h after administration of 155 nm liposomes as compared to 112 nm liposomes.
    [Abstract] [Full Text] [Related] [New Search]