1. Curcumin-loaded solid lipid nanoparticles with Brij78 and TPGS improved in vivo oral bioavailability and in situ intestinal absorption of curcumin
- Author
-
Jingling Tang, Li Mengting, Linhua Wu, Nannan Zheng, Jinmei Ren, and Hongyu Ji
- Subjects
Male ,Materials science ,Curcumin ,Metabolic Clearance Rate ,Drug Compounding ,Pharmaceutical Science ,Administration, Oral ,Biological Availability ,02 engineering and technology ,Pharmacology ,030226 pharmacology & pharmacy ,Intestinal absorption ,Polyethylene Glycols ,03 medical and health sciences ,chemistry.chemical_compound ,Surface-Active Agents ,0302 clinical medicine ,Pharmacokinetics ,In vivo ,Solid lipid nanoparticle ,Intestine, Small ,Zeta potential ,Animals ,Nanotechnology ,Technology, Pharmaceutical ,Vitamin E ,ATP Binding Cassette Transporter, Subfamily B, Member 1 ,Solubility ,Particle Size ,Rats, Wistar ,Drug Carriers ,Chromatography ,Models, Statistical ,General Medicine ,021001 nanoscience & nanotechnology ,Lipids ,Bioavailability ,body regions ,chemistry ,Intestinal Absorption ,Models, Chemical ,Area Under Curve ,Nanoparticles ,0210 nano-technology ,Half-Life - Abstract
The present study was to formulate curcumin solid lipid nanoparticles (Cur-SLNs) with P-gp modulator excipients, TPGS and Brij78, to enhance the solubility and bioavailability of curcumin.The formulation was optimized by Plackett-Burman screening design and Box-Behnken experiment design. Then physiochemical properties, entrapment efficiency and in vitro release of Cur-SLNs were characterized. In vivo pharmacokinetics study and in situ single-pass intestinal perfusion were performed to investigate the effects of Cur-SLNs on the bioavailability and intestinal absorption of curcumin.The optimized formulations showed an average size of 135.3 ± 1.5 nm with a zeta potential value of -24.7 ± 2.1 mV and 91.09% ± 1.23% drug entrapment efficiency, meanwhile displayed a sustained release profile. In vivo pharmacokinetic study showed AUC0→t for Cur-SLNs was 12.27-folds greater than curcumin suspension and the relative bioavailability of Cur-SLNs was 942.53%. Meanwhile, Tmax and t(1/2) of curcumin for Cur-SLNs were both delayed comparing to the suspensions (p 0.01). The in situ intestinal absorption study revealed that the effective permeability (Peff) value of curcumin for SLNs was significantly improved (p 0.01) comparing to curcumin solution.Cur-SLNs with TPGS and Brij78 could improve the oral bioavailability and intestinal absorption of curcumin effectively.
- Published
- 2014