Self-Assembled Nanomicelles to Enhance Solubility and Anticancer Activity of Etoposide

Alsalhi, Abdullah; Ayon, Navid J.; Sikder, Sadia; Youan, Bi‐Botti C.

doi:10.1089/adt.2021.089

Cited by 4 publications

(2 citation statements)

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“…Weak signal for hydroxylic protons of PEG (δ = 4.2 ppm, d) and aromatic protons of VIT E TPGS (δ = 7.3 ppm, e) were also observed. Extremely weak signal for the hydroxylic and the aromatic protons are due to significantly outnumbered alkyl protons present in both the VIT E TPGS [24] and HCO-40 [37], which also aligns with published literature [38][39][40][41]. Comparison to spectra for blank nanomicelles and DTX nanomicelles in D 2 O revealed these similar set of peaks confirming the presence of the stable polymers in the nanomicelles.…”

Section: Characterization Of the Synthesized Nanomicelles Loaded With...supporting

confidence: 86%

“…New generation and novel drug delivery systems, such as liposomes, solid lipid nanoparticles (SLNs), and nanomicelles, have been recently used to improve the therapeutic index and to reduce the adverse effects of DTX [19][20][21]. Increasing the aqueous solubility and ultimately bioavailability are the most critical features of the oral formulation of DTX and other similar hydrophobic drugs [22], which can be achieved by using P-gp inhibitors, selfassembled emulsifiers, and nanocarriers, including nanomicelles [23,24]. Nanomicelles are synthesized from both ionic and nonionic surfactants, and they are developed by the supramolecular assembly of hydrophobic heads and hydrophilic tails, in which a colloidal dispersion is formed [25].…”

Section: Introductionmentioning

confidence: 99%

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Self-Assembled Nanomicellar Formulation of Docetaxel as a Potential Breast Cancer Chemotherapeutic System

Alshamrani

Ayon

Alsalhi

et al. 2022

Life

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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.

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