Brij78

It has been demonstrated that various polymeric surfactants including D-alpha-tocopheryl poly (ethylene glycol) succinate 1000 (commonly known as TPGS), polysorbates (commonly known as Tween) as well as alkyl-PEO (commonly known as Brij) are capable of inhibiting efflux pumps. Brij78 (polyoxyethylene 20 stearylether) had been shown to inhibit the efflux pumps. Scientists have prepared doxorubicin and paclitaxel-loaded nanoparticles using Brij78 as an emulsifying agent to overcome MDR by inhibiting P-gp. Since curcumin had been reported to be a substrate of P-gp and active efflux by P-gp, Brij78 and TPGS, which are commonly used in pharmaceutical formulations as surfactants, provide a good opportunity for enhancing oral bioavailability of curcumin.

Curcumin-loaded Solid Lipid Nanoparticles With Brij78 and TPGS Improved In Vivo Oral Bioavailability and In Situ Intestinal Absorption of Curcumin

In order to improve the solubility and bioavailability of curcumin, scientists have developed a formulation of curcumin solid lipid nanoparticles (Cur-SLNs) containing P-gp modulator excipients, TPGS and Brij78. Cur-SLNs were prepared by emulsification and low-temperature curing. Then the physicochemical properties, entrapment efficiency, and in vitro release of Cur-SLNs were characterized. The effects of Cur-SLNs on curcumin bioavailability and intestinal absorption were studied. The optimized formulation had a mean particle size of about 135.3±1.5 nm and a zeta potential value of 24.7±2.1mV. In vitro release study indicated that Cur-SLNs exhibited a sustained release in SGF and SIF. 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%. The effect in improving the oral bioavailability of curcumin may result from improving the water solubility, enhancing the absorption by improving the intestinal permeability, inhibiting P-gp-mediated efflux by surfactants, Brij78 and TPGS. Thus, encapsulating drugs on SLNs containing Brij78 and TPGS will be a promising method to improve the bioavailability of the hydrophobic drug, such as curcumin.

Fig.1 Effective permeability coefficient (P_eff) of different perfusion solutions. (Ji, 2016)

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Reference

1. Ji, H.; et al. Curcumin-loaded solid lipid nanoparticles with Brij78 and TPGS improved in vivo oral bioavailability and in situ intestinal absorption of curcumin. Drug delivery. 2016, 23(2): 459-470.