10-Hydroxycamptothecin (HCPT) nanosuspensions stabilized by mPEG₁₀₀₀-HCPT conjugate: high stabilizing efficiency and improved antitumor efficacy.

ABSTRACT: In this study, polyethylene glycol (PEG)ylated 10-hydroxycamptothecin (mPEG₁₀₀₀-HCPT) was synthesized and used as a stabilizer to prepare 10-hydroxycamptothecin (HCPT) nanosuspensions for their in vitro and in vivo antitumor investigation. The resultant HCPT nanosuspensions (HCPT-NSps) had a very high drug payload of 94.90% (w/w) and a mean particle size of 92.90±0.20 nm with narrow size distribution (polydispersity index of 0.16±0.01). HCPT-NSps could be lyophilized without the need of the addition of any cryoprotectant and then be reconstituted into nanosuspensions of a similar size by direct resuspension in water. HCPT was in crystalline form in HCPT-NSps. Using mPEG₁₀₀₀-HCPT as stabilizer, insoluble camptothecin and 7-ethyl-10-hydroxycamptothecin could also be eas

SUBMITTER: Yang L 

PROVIDER: S-EPMC5439984 | biostudies-literature | 2017

REPOSITORIES: biostudies-literature