Improvement of the bioavailability of curcumin by a supersaturatable self nanoemulsifying drug delivery system with incorporation of a hydrophilic polymer: in vitro and in vivo characterisation

Abstract

Objectives The current study was focused on preparing curcumin (CUR) supersaturated self-nano-emulsion (PI-CUR-SNEDDS) using hydrophilic polymer and to study the influence of polymer precipitation inhibitor on the physicochemical and biopharmaceutical properties of the PI-CUR-SNEDDS. Methods PI-CUR-SNEDDS were prepared using hydrophilic polymer in order to maintain the supersaturation of CUR in nano-emulsion solution, artificial gastrointestinal fluid (AGF), and the precipitates formed, and characterised by in vitro dispersion tests, in vitro intestinal absorption and in vivo pharmacokinetic and compared with CUR-SNEDDS. Key findings PI-CUR-SNEDDS prepared with 2% hydroxypropyl methylcellulose 55–60 (HPMC55-60) as precipitation inhibitor (PI) significantly improved the viscosity, physical stability and CUR’s equilibrium solubility of nanoemulsion. HPMC55-60 and CUR interact in AGF through intermolecular interactions, form hydrogen bonds, and produce amorphous precipitates. Compared with CUR-SNEDDS, the proportion of CUR in the hydrophilic phase increased by about 3-fold, and apparent permeability coefficient (Papp) in duodenum, jejunum, ileum, and colon increased by 2.30, 3.65, 1.54 and 2.08-fold, respectively, and the area under the plasma concentration-time curve0-12h of PI-CUR-SNEDDS also increased by 3.50-fold. Conclusions Our results suggested that HPMC55-60 maintained the CUR supersaturation state by forming hydrogen bonds with CUR, increasing the solution’s viscosity and drug solubilisation, thus improving the absorption and bioavailability of CUR.

Susceptibility of periodontal pathogens to a novel target-specific drug delivery system containing self-nanoemulsifying curcumin: An in vitro study

“… 8 , 9 , 10 , 35 , 36 Another independent study that characterized in vitro, a formulation containing SNEC in HPMC concluded that HPMC maintained the supersaturation state of curcumin by developing hydrogen bonds with the latter and thus improving the drug solubilization and viscosity of the system, thereby enhancing the absorption and bioavailability of curcumin. 37 It was observed in an in vitro study that the presence of 10% w/w of HPMC in the tested formulations resulted in almost 100-fold greater concentrations of curcumin compared to the formulation without the polymer. This high drug concentration was further found to be sustained for 3 hours in comparison to the formulation without the polymer.…”

Curcumin-Loaded RH60/F127 Mixed Micelles: Characterization, Biopharmaceutical Characters and Anti-Inflammatory Modulation of Airway Inflammation

“…Approximately, 100 μL of the supernatant was placed into another clean tube and filtered with a 0.22 μm filter. Samples were analyzed using LC-MS/MS [ 24 , 25 ].…”

Development of Linagliptin Ultra Fine Solid Supersaturated Bio-SNEDDS Using Triangular Mixture Design for Enhancement of Oral Bioavailability: Impact of P-gp Inhibition

“…8 e, f). The strength and broadening of the N-H peak for both Ss-F4 and Ss-F8 may be due to formation of hydrogen bonding between HPBCD as PI and LIN [48].…”