Curcumin-loaded solid lipid nanoparticles with Brij78 and TPGS improved in vivo oral bioavailability and in situ intestinal absorption of curcumin. (12th February 2016)

• Record Type: Journal Article
• Authors: Ji, Hongyu; Tang, Jingling; Li, Mengting; Ren, Jinmei; Zheng, Nannan; Wu, Linhua
• Is Part Of: Drug delivery. Volume 23:Number 2(2016:Feb.)
• Page Start: 459
• Page End: 470
• Publication Date: 2016-02-12
• Subjects: Curcumin -- in situ intestinal absorption -- oral bioavailability -- P-glycoprotein -- solid lipid nanoparticles; Drug delivery systems -- Periodicals; Drug targeting -- Periodicals; 615.05
• DOI: 10.3109/10717544.2014.918677
• Languages: English
• ISSNs: 1071-7544

Abstract

Abstract: Purpose : 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. Methods : 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. Results : 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 AUC 0→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. Conclusion : Cur-SLNs with TPGS and Brij78 could improve the oral bioavailability and intestinal absorption of curcumin effectively.