Increasing Cellular Uptake and Permeation of Curcumin Using a Novel Polymer-Surfactant Formulation

Abstract

Several therapeutically active molecules are poorly water-soluble, thereby creating a challenge for pharmaceutical scientists to develop an active solution for their oral drug delivery. This study aimed to investigate the potential for novel polymer-surfactant-based formulations (designated A and B) to improve the solubility and permeability of curcumin. A solubility study and characterization studies (FTIR, DSC and XRD) were conducted for the various formulations. The cytotoxicity of formulations and commercial comparators was tested via MTT and LDH assays, and their permeability by in vitro drug transport and cellular drug uptake was established using the Caco-2 cell model. The apparent permeability coefficients (Papp) are considered a good indicator of drug permeation. However, it can be argued that the magnitude of Papp, when used to reflect the permeability of the cells to the drug, can be influenced by the initial drug concentration (C0) in the donor chamber. Therefore, Papp (suspension) and Papp (solution) were calculated based on the different values of C0. It was clear that Papp (solution) can more accurately reflect drug permeation than Papp (suspension). Formulation A, containing Soluplus® and vitamin E TPGs, significantly increased the permeation and cellular uptake of curcumin compared to other samples, which is believed to be related to the increased aqueous solubility of the drug in this formulation.

Toxicity Evaluation and Controlled-Release of Curcumin-Loaded Amphiphilic Poly-N-vinylpyrrolidone Nanoparticles: In Vitro and In Vivo Models

“…Sixty minute after treating cells with free curcumin and PVP-Cur NPs, it was shown that the relative fluorescence intensity of curcumin loaded into the nanoparticles was 1.5 times higher than that of the free curcumin ( Figure 4 ). This difference in the absorption is due to the presence of an amphiphilic poly(N-vinylpyrrolidone) shell and correlates with other studies related to curcumin encapsulation [ 53 , 54 ].…”

Electrosprayed Core (Cellulose Acetate)–Shell (Polyvinylpyrrolidone) Nanoparticles for Smart Acetaminophen Delivery

“…The amorphous state is a high-energy state over the crystalline state, and, thus, the long time period of stable existence needs fine compatibility between the co-existence components to prevent possible solid-phase separation [ 78 , 79 , 80 ]. FTIR spectra can be exploited to disclose the possible secondary interactions between the components, which include hydrogen bonding, electrostatic interactions, hydrophobic interactions, and Van Der Waals forces and are favorable to high stability [ 81 , 82 , 83 ]. The ATR-FTIR spectra of the raw materials (ATP, PVP, and CA) and their electrosprayed products (P1, P2, and P3) are included in Figure 7 .…”

Tween–80 Coating in Enhancing Physicochemical Stability, Kinetics and Release Mechanism of Layered Double Hydroxide-Ferulate

“…Despite the amazing properties offered by LDHs, their low solubilization in water, agglomeration, and unsatisfactory targeted delivery have limited the potential of LDHs in CRF [5]. To deal with the aforementioned limitations, LDHs were attempted to be incorporated with a wide range of new materials, including polymeric surfactants [6][7][8]. Owing to the ability of polymeric surfactants to manipulate the nature of LDHs, predominantly in terms of size distribution, size of the particle, morphology, surface interaction, and zeta potential, this ability has therefore assisted in making LDHs more favorable for drug encapsulation [2,[7][8].…”