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High drug payload curcumin nanosuspensions stabilized by mPEG-DSPE and SPC: in vitro and in vivo evaluation.
- Source :
- Drug Delivery; 2017, Vol. 24 Issue 1, p109-120, 12p
- Publication Year :
- 2017
-
Abstract
- Context: Curcumin (CUR) is a promising drug candidate based on its broad bioactivities and good antitumor effect, but the application of CUR is potentially restricted because of its poor solubility and bioavailability. Objective: This study aims at developing a simple and effective drug delivery system for CUR to enhance its solubility and bioavailability thus to improve its antitumor efficacy. Materials and methods:Curcumin nanosuspensions (CUR-NSps) were prepared by precipitation-ultrasonication method using mPEG2000-DSPE and soybean lecithin as a combined stabilizer. Results: CUR-NSps with a high drug payload of 67.07% were successfully prepared. The resultant CUR-NSps had a mean particle size of 186.33 ± 2.73 nm with a zeta potential of −19.00 ± 1.31 mV.In vitrocytotoxicity assay showed that CUR-NSps exhibited enhanced cytotoxicity compared to CUR solution. The pharmacokinetics results demonstrated that CUR-NSps exhibited a significantly greater AUC0–24and prolonged MRT compared to CUR injections after intravenous administration. In the biodistribution study, CUR-NSps demonstrated enhanced biodistribution compared with CUR injections in liver, spleen, kidney, brain, and tumor. The CUR-NSps also showed improved antitumor therapeutic efficacy over the injections (70.34% versus 40.03%,p < 0.01). Conclusions: These results suggest that CUR-NSps might represent a promising drug formulation for intravenous administration of CUR for the treatment of cancer. [ABSTRACT FROM AUTHOR]
- Subjects :
- CURCUMIN
DRUG efficacy
BIOAVAILABILITY
IN vitro studies
PHARMACOKINETICS
Subjects
Details
- Language :
- English
- ISSN :
- 10717544
- Volume :
- 24
- Issue :
- 1
- Database :
- Complementary Index
- Journal :
- Drug Delivery
- Publication Type :
- Academic Journal
- Accession number :
- 126591017
- Full Text :
- https://doi.org/10.1080/10717544.2016.1233589