Abstract
Glycyrrhetic acid (GA)-modified pullulan nanoparticles (GAP NPs) were synthesized as a novel carrier of curcumin (CUR) with a degree of substitution (DS) of GA moieties within the range of 1.2–6.2 groups per hundred glucose units. In the present study, we investigated the physicochemical characteristics, release behavior, in vitro cytotoxicity and cellular uptake of the particles. Self-assembled GAP NPs with spherical shapes could readily improve the water solubility and stability of CUR. The CUR release was sustained and pH-dependent. The cellular uptake of CUR-GAP NPs was confirmed by green fluorescence in the cells. An MTT study showed CUR-GAP NPs with higher cytotoxicity in HepG2 cells than free CUR, but GAP NPs had no significant cytotoxicity. GAP is thus an excellent carrier for the solubilization, stabilization, and controlled delivery of CUR.
Highlights
Curcumin (CUR), a low-molecular-weight and hydrophobic polyphenol with fluorescence, obtained from the turmeric Curcuma rhizome, has low intrinsic toxicity but a wide range of pharamacological activities, including antioxidant, anti-inflammatory, antimicrobial, antiamyloid, and antitumor properties [1,2]
The 1H nuclear magnetic resonance (1H-NMR) spectra for GA-modified pullulan (GAP) showed the characteristic peaks of pullulan and new peaks assigned to the CH3, CH2, and CH protons of the Glycyrrhetic acid (GA) moiety at 0.63–2.0 ppm, which indicated the successful conjugation of GA to pullulan
When the ratio of CUR to GAP weight was increased from 5%–20%, CUR loading capacity and diameter of CUR-GAP NPs increased from 4.97%–10.29% and 97.1 nm–123.6 nm respectively, while encapsulation efficiency decreased from 78.3%–68.9%
Summary
Curcumin (CUR), a low-molecular-weight and hydrophobic polyphenol with fluorescence, obtained from the turmeric Curcuma rhizome, has low intrinsic toxicity but a wide range of pharamacological activities, including antioxidant, anti-inflammatory, antimicrobial, antiamyloid, and antitumor properties [1,2]. Pullulan-based NPs have been extensively used for nanoparticulate drug delivery because of their outstanding biocompatibility, high water-solubility, non-toxicity, and multiple hydroxyl groups that can be chemically modified; in addition, they lack immunogenicity, so are useful as a plasma expanders [16,17]. We evaluated the use of GAP NPs as a drug carrier of CUR and investigated release behavior, cellular uptake and cytotoxicity
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