Engineering fast dissolving sodium acetate mediated crystalline solid dispersion of docetaxel

Ngo, Albert Nguessan; Thomas, D. I.; Murowchick, James B.; Ayon, Navid J.; Jaiswal, Ankit; Youan, Bi‐Botti C.

doi:10.1016/j.ijpharm.2018.04.045

Cited by 19 publications

(6 citation statements)

References 72 publications

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“…LC-MS/MS analysis of (a) native docetaxel (11.29 min) and (b) docetaxel-loaded nanomicelles (11.19 min) exhibited similar retention time (difference = 0.10 min), m/z, and fragmentation profile (Figure 9), which indicates that the nanomicelles, as a delivery system, maintain the chemical stability of DTX. The result is, indeed, expected because docetaxel is stable inside the hydrophobic core of the nanomicelles which upon release when detected by LC-MS/MS had the same retention time, m/z and fragmentation pattern which is consistent with the data we have published before on docetaxel stability in solid dispersion formulation [36].…”

Section: Lc-ms/ms Analysis For Chemical Stabilitysupporting

confidence: 90%

“…The control (10 µM of native DTX) was dissolved in an aliquot of the same organic solvent spiked with blank nanomicelles to account for the interaction of polymers with the drug and hence its effect on the stability of drug. LC-MS/MS analysis was performed using a method we previously developed to analyze docetaxel in solid-dispersion dosage form [36]. The LC-MS/MS analysis was carried out on an AB Sciex 3200 QTrap mass spectrometer (Foster City, CA, USA) coupled to a Shimadzu UFLC system (Columbia, MD, USA) using electrospray ionization (ESI) and run with Analyst version 1.4.2 software.…”

Section: In Vitro Cytotoxicity: Mts Assaymentioning

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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Section: Lc-ms/ms Analysis For Chemical Stabilitysupporting

confidence: 90%

Section: In Vitro Cytotoxicity: Mts Assaymentioning

confidence: 99%

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

Alshamrani

Ayon

Alsalhi

et al. 2022

Life

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“…The physical mixture of meloxicam and PVP showed a reduction in the intensity of Braggs peaks due to the dilution effect of the polymer (Ngo et al 2018). However, the DC increased to 40.01.…”

Section: Xrpdmentioning

confidence: 98%

Binary or ternary mixture of solid dispersion: Meloxicam case

Hameed¹,

Mohamed²,

Sahib³

2022

PHAR

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The present work was carried out to assess the value of adding water insoluble polymer to meloxicam amorphous solid formulation (ASD). Meloxicam was mixed with polyvinylpyrrolidone (PVP) (1:1 ratio) as a binary mixture and with PVP and ethyl cellulose (1:1:1 ratio) as a ternary mixture. Solvent evaporation method was used to prepare ASD formulations. The differential scanning calorimetry, powder X-Ray diffraction, Cambridge Structural Database and in-vitro dissolution were performed to assess the formulas. The results showed that the addition of insoluble polymer could prevent the recrystallization process during ASD formation. However, the binary mixture showed higher drug release percentage than the ternary mixture. Therefore, a rational amount of insoluble polymer could be considered to control recrystallization and manipulate drug release from ASD formulations.

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“…Among the various formulations developed to enhance the solubility, dissolution, and oral bioavailability of poorly water‐soluble drugs, solid dispersions show promising results and have been successfully applied in commercial dosage forms . Solid dispersions consist of at least two different components, namely, a polymer and drug; the drug can be molecularly dispersed in the polymer matrix or can be dispersed as amorphous or crystalline particles that are formed by solvent evaporation or cooling from the melted state.…”

Section: Dissolution Data For Pure Cilostazol and Solid Dispersions Omentioning

confidence: 99%

“…[9][10][11] Solid dispersions consist of at least two different components, namely, a polymer and drug; the drug can be molecularly dispersed in the polymer matrix or can be dispersed as amorphous or crystalline particles that are formed by solvent evaporation or cooling from the melted state. [9][10][11] Solid dispersions consist of at least two different components, namely, a polymer and drug; the drug can be molecularly dispersed in the polymer matrix or can be dispersed as amorphous or crystalline particles that are formed by solvent evaporation or cooling from the melted state.…”

mentioning

confidence: 99%

Effect of Polymer Type on the Dissolution Profile of a Solid Dispersion of Cilostazol

Lee

et al. 2019

Bulletin Korean Chem Soc

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Engineering fast dissolving sodium acetate mediated crystalline solid dispersion of docetaxel

Cited by 19 publications

References 72 publications

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

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

Binary or ternary mixture of solid dispersion: Meloxicam case

Effect of Polymer Type on the Dissolution Profile of a Solid Dispersion of Cilostazol

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Engineering fast dissolving sodium acetate mediated crystalline solid dispersion of docetaxel

Cited by 19 publications

References 72 publications

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

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

﻿Binary or ternary mixture of solid dispersion: Meloxicam case

Effect of Polymer Type on the Dissolution Profile of a Solid Dispersion of Cilostazol

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Binary or ternary mixture of solid dispersion: Meloxicam case