Docetaxel (DTX) is classified as a class IV drug that exhibits poor aqueous solubility (6–7 µg/mL in water) and permeability (P-glycoprotein substrate). The main objective of this study was to construct, characterize, and evaluate docetaxel loaded nanomicellar formulation in vitro for oral delivery to enhance the absorption and bioavailability of DTX, as well as to circumvent P-gp efflux inhibition. Formulations were prepared with two polymeric surfactants, hydrogenated castor oil-40 (HCO-40) and D-α-Tocopherol polyethylene glycol 1000 succinate (VIT E TPGS) with solvent evaporation technique, and the resulting DTX nanomicellar formulations were characterized by proton nuclear magnetic resonance spectroscopy (1H NMR), Fourier Transform Infrared Spectroscopy (FT–IR), X-ray powder diffraction (XRD), and transmission electron microscopy (TEM). Proton NMR, FT–IR, and XRD data indicated that DTX was completely encapsulated within the hydrophobic core of the nanomicelles in its amorphous state. TEM data revealed a smooth spherical shape of the nanomicellar formulation. The optimized formulation (F-2) possessed a mean diameter of 13.42 nm, a zeta potential of −0.19 mV, with a 99.3% entrapment efficiency. Dilution stability study indicated that nanomicelles were stable up to 100-fold dilution with minimal change in size, poly dispersity index (PDI), and zeta potential. In vitro cytotoxicity study revealed higher anticancer activity of DTX nanomicelles at 5 µM compared to the native drug against breast cancer cell line (MCF-7) cells. The LC–MS data confirmed the chemical stability of DTX within the nanomicelles. In vitro drug release study demonstrated faster dissolution of DTX from the nanomicelles compared to the naked drug. Our experimental results exhibit that nanomicelles could be a drug delivery system of choice to encapsulate drugs with low aqueous solubility and permeability that can preserve the stability of the active constituents to provide anticancer activity.
The objective of this study was to synthesize a novel choline hydroxide ionic liquid-based tooth bleaching gel. Ionic liquid-based gels were synthesized and characterized using FTIR along with pH testing. Tooth sample preparation was carried out in line with ISO 28399:2020. The effects of synthesized gels on tooth samples were tested. Tooth samples were stained and grouped into three experimental groups: EAI (22% choline hydroxide gel), EAII (44% choline hydroxide gel), and EB (choline citrate gel) and two control groups: CA (commercial at-home 16% carbamide peroxide gel) and CB (deionized water). The tooth color analysis, which included shade matching with the Vitapan shade guide (n = 2), and digital colorimetric analysis (n = 2) were evaluated. The surface characteristics and hardness were analyzed with 3D optical profilometry, Scanning Electron Microscopy (SEM), Energy Dispersive X-ray Spectroscopy (EDX), and Microhardness testing (n = 3), respectively. The tooth color analysis (Vitapan shade guide) revealed that all the tooth samples treated with synthesized choline citrate gel (EB) showed an A1 shade as compared to the other four groups, giving a range of shades. An analysis of the ΔE values from digital colorimetry; EAI, EAII, CA, and CB showed ΔE values in a range that was clinically perceptible at a glance. However, EB showed the highest value of ΔE. The mean microhardness values for the five groups showed that the effects of three experimental gels i.e., 44% choline hydroxide, 22% choline hydroxide, and choline citrate, on the microhardness of the tooth samples were similar to that of the positive control, which comprised commercial at-home 16% carbamide peroxide gel. SEM with EDX of three tested subgroups was closely related in surface profile, elemental composition, and Ca/P ratio. The roughness average values from optical profilometry of four tested subgroups lie within approximately a similar range, showing a statistically insignificant difference (p > 0.05) between the tested subgroups. The synthesized novel experimental tooth bleaching gels displayed similar tooth bleaching actions without any deleterious effects on the surface characteristics and microhardness of the treated tooth samples when compared with the commercial at-home tooth bleaching gel.
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