Improving curcumin solubility and bioavailability by encapsulation in saponin-coated curcumin nanoparticles prepared using a simple pH-driven loading method

Abstract

Curcumin is a bioactive phytochemical that can be utilized as a nutraceutical or pharmaceutical in functional foods, supplements, and medicines. However, the application of curcumin as a nutraceutical in commercial food and beverage products is currently limited by its low water-solubility, chemical instability, and poor oral bioavailability. In this study, all-natural colloidal delivery systems were developed to overcome these challenges, which consisted of saponin-coated curcumin nanoparticles formed using a pH-driven loading method. The physicochemical and structural properties of the curcumin nanoparticles formed using this process were characterized, including particle size distribution, surface potential, morphology, encapsulation efficiency, and loading capacity. Fourier transform infrared spectroscopy and X-ray diffraction indicated that curcumin was present in the nanoparticles in an amorphous form. The curcumin nanoparticles were unstable to aggregation at low pH values (<3) and high NaCl concentrations (>200 mM), which was attributed to a reduction in electrostatic repulsion between them. However, they were stable at higher pH values (3 to 8) and lower NaCl levels (0 to 200 mM), due to a stronger electrostatic repulsion between them. They also exhibited good stability during refrigerated storage (4 °C) or after conversion into a powdered form (lyophilized). A simulated gastrointestinal tract study demonstrated that the in vitro bioaccessibility was around 3.3-fold higher for curcumin nanoparticles than for free curcumin. Furthermore, oral administration to Sprague Dawley rats indicated that the in vivo bioavailability was around 8.9-fold higher for curcumin nanoparticles than for free curcumin. These results have important implications for the development of curcumin-enriched functional foods, supplements, and drugs.

Preparation of Poloxamer188-b-PCL and Study on in vitro Radioprotection Activity of Curcumin-Loaded Nanoparticles

“…However, in their clinical applications, CUR molecules show certain drawbacks, e.g., low solubility (Lim et al, 2018;Peng et al, 2018), poor stability (Kharat et al, 2017;Luo et al, 2017), low absorptivity (Gopi et al, 2017), and short half-life (Hussain et al, 2017). These weaknesses lead to the low bioavailability of CUR and limit its further applications.…”

The Role of Imidazolium-Based Surface-Active Ionic Liquid to Restrain the Excited-State Intramolecular H-Atom Transfer Dynamics of Medicinal Pigment Curcumin: A Theoretical and Experimental Approach

“… 19 Therefore, its poor aqueous solubility and low bioavailability need to be ameliorated to let curcumin act as a potential drug. To overcome these challenges, various drug delivery systems, such as vesicles, 20 proteins, 21 − 24 micelles, 25 hydrogels, 26 , 27 liposomes, 28 cyclodextrin, 29 polymer conjugates, 30 supra molecular assemblies, 31 and nanoparticles 32 , 33 have been used to encapsulate curcumin in order to improve its stability, bioavailability, and to enhance its aqueous solubility. However, utilization of micelle-based drug carrier systems has been generally preferred over the other particulate drug carrier system for the encapsulation of hydrophobic drugs due to their small size (∼10 to 50 nm) and comparatively increased bioavailability.…”

Determination and pharmacokinetic study of isothiouronium-modified pyrimidine-substituted curcumin analog (1G), a novel antitumor agent, in rat plasma by liquid chromatography–tandem mass spectrometry

“…Moreover, cell culture experiments have shown the antitumor activity of curcumin in various human cancer cell lines, such as leukemia [9], esophageal cancer [10], gastric cancer [11], liver cancer [12], lung cancer [13] and cervical cancer [14]. Despite the potential therapeutic effects of curcumin, clinical applications are restricted by its poor bioavailability, rapid metabolism, low solubility and extensive rapid excretion [15][16][17][18][19][20]. These inherent problems prompted us to synthesize novel isothiouronium-modified pyrimidinesubstituted curcumin analogs [21][22][23] with improved pharmacokinetic profiles.…”