Abstract：
:Oridonin (ORI), a diterpenoid compound with promising antitumor activity, was proved to possess potent antileukemia efficacies in vitro and in vivo recently. However, the development and application of ORI was limited by its poor solubility and rapid plasma clearance. The purpose of this study was to solve these problems. PEGylated oridonin linked with succinic acid (SA) as spacer moiety (PEG-SA-ORI conjugate) was synthesized. mPEG amines with four specifications of molecular weight (MW) were utilized. All polymeric conjugates showed satisfactory aqueous solubility and in vitro studies implied that the drug solubility and release features of conjugates were relevant to PEGs. The drug solubility increased more when the MW of PEG was lower, while more significant sustained-release effect was shown with higher PEG MW. Moreover, the release behaviors of conjugates showed a pH-sensitive property. In vivo pharmacokinetic studies demonstrated that the elimination half-life was prolonged in comparison with ORI solution. PEGylation could be a promising method to obtain better efficacy in the field of drug delivery system.
journal_name
Int J Pharmjournal_title
International journal of pharmaceuticsauthors
Shen J,Zhang D,Zhao Z,Jia L,Zheng D,Liu G,Hao L,Zhang Q,Tian X,Li C,Guo Hdoi
10.1016/j.ijpharm.2013.08.014subject
Has Abstractpub_date
2013-11-01 00:00:00pages
80-6issue
1eissn
0378-5173issn
1873-3476pii
S0378-5173(13)00736-9journal_volume
456pub_type
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