Pharmaceutical Amorphous Nanoparticles

Jog, Rajan; Burgess, Diane J.

doi:10.1016/j.xphs.2016.09.014

Cited by 146 publications

(65 citation statements)

References 170 publications

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“…1,2) A number of strategies have been tried for enhancing the release rates and bioavailabilities of oral dosage forms of these antifungal drugs. [3][4][5][6][7] In injectable formulations, the use of cosolvents, such as ethanol, macrogol and propylene glycol, or surfactants, has been shown to successfully enhance the solubilization of the drugs. 8) Recently, in order to achieve sustained-release delivery, an approach using biodegradable microspheres (MS) containing antimicrobial agents or other types of drug has been tried.…”

Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of Itraconazole- or Miconazole-Loaded PLGA Microspheres

Matsuura

Kojima

Haraguchi

et al. 2019

CHEMICAL & PHARMACEUTICAL BULLETIN

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The purpose of this study was to prepare poly(lactide-co-glycolide) (PLGA) microspheres (MS) loaded with itraconazole (ITCZ) or miconazole (MCZ) under different evaporation temperatures (25 or 40°C) using an oil-in-water emulsion solvent evaporation method in order to evaluate the initial burst release of drug. Loading efficiencies were comparatively good and the diameters of prepared drug-loaded PLGA MS were around 20 µm in all formulations. The release rates of ITCZ-PLGA MS prepared at 40°C showed a significantly restricted release profile compared with the corresponding ITCZ-PLGA MS prepared at 25°C. This difference in release rate of ITCZ was thought to be caused by the self-healing effect of PLGA, as the glass transition temperature of PLGA is around 40°C. With respect to the MCZ-PLGA MS, the initial burst release was similar in formulations prepared at both 25 and 40°C. Scanning electron microscope results suggested that the initial burst release was due to the localization of MCZ on the surface of MCZ-PLGA MS at higher concentrations. Differential scanning calorimetry measurements suggested complete amorphization of MCZ in MCZ-PLGA MS, whereas crystalline ITCZ was detected in the ITCZ-PLGA MS. This complete amorphization of MCZ is considered to be one of the reasons for the initial burst release.

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Section: Introductionmentioning

confidence: 99%

Preparation and Characterization of Itraconazole- or Miconazole-Loaded PLGA Microspheres

Matsuura

Kojima

Haraguchi

et al. 2019

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Reducing the particle size, modifying the crystal habit, and designing the crystal form of APIs are common approaches to improve the bioavailability of APIs with poor water solubility and to enhance powder handling in the formulation design [2]. For example, Jog and Burgess reviewed the application of pharmaceutical amorphous nanoparticles in designing novel drug delivery systems and summarized the particle manufacturing techniques [3]. Modi et al investigated the effect of crystal habit on intrinsic dissolution behavior and demonstrated the effect of particle-level properties and the surface molecular environment on the intrinsic dissolution rate [4].…”

Section: Introductionmentioning

confidence: 99%

Recrystallization and Production of Spherical Submicron Particles of Sulfasalazine Using a Supercritical Antisolvent Process

2018

Crystals

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Abstract:In this study, the recrystallization and production of spherical submicron particles of sulfasalazine, an active pharmaceutical ingredient (API), were performed using the supercritical antisolvent (SAS) process, a nonconventional crystallization technique. Sulfasalazine was dissolved in tetrahydrofuran (THF), and supercritical carbon dioxide (CO 2 ) served as the antisolvent. The effects of operating parameters on the SAS process, including the operating pressure, solution concentration, solution flowrate, CO 2 flowrate, and spraying nozzle diameter, at two operating temperatures were examined. The solid-state characteristics of sulfasalazine before and after the SAS process, including particle size, crystal habit, and crystal form, were analyzed using a scanning electron microscope (SEM), powder X-ray diffractometer (PXRD), and differential scanning calorimeter (DSC). A higher operating temperature, intermediate operating pressure, higher CO 2 flowrate, and lower solution flowrate are recommended to obtain spherical particles of sulfasalazine. The effects of the solution concentration and spraying nozzle diameter on the SAS process were negligible. Under optimal conditions, spherical sulfasalazine crystals with a mean size of 0.91 µm were generated, and this study demonstrated the feasibility for tuning the solid-state characteristics of API through the SAS process.

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“…In the past few years, many strategies have been adopted to improve the solubility, dissolution and oral bioavailability of insoluble drugs (Jog & Burgess, 2017). Among them, drug nanocrystalline technology has become one of the most attractive alternative methods by reducing drug particles to submicron (100-1000 nm) or even nanometer (1-100 nm) sizes (Bao, Mitragotri, & Tong, 2013;Verma, Huey, & Burgess, 2009).…”

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confidence: 99%

A rapid and sensitive method for quantification of ibrutinib in rat plasma by UPLC–ESI–MS/MS: validation and application to pharmacokinetic studies of a novel ibrutinib nanocrystalline

Sun¹,

Cheng²,

Kong³

et al. 2019

Biomedical Chromatography

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Ibrutinib has an excellent effect in the treatment of mantle cell lymphoma so it has attracted much attention. A novel ibrutinib nanocrystalline was exploited in our study to improve the bioavailability. A fast and reliable UPLC–MS/MS method was established for the accurate quantification of ibrutinib in rat plasma. The chromatographic separation was achieved by an Agilent zorbax SB‐C18 rapid solution HD column (2.1 × 50 mm, 1.8 μm). The mobile phase consisted of deionized water (containing 10 mm ammonium acetate and 0.1% formic acid) and pure acetonitrile. Isocratic elution (water–acetonitrile 10:90, v/v) was adopted and the flow rate was 0.4 mL/min. Column temperature was set to 40°C. Vilazodone was used as the internal standard in this analytical method. Multiple reaction monitoring mode with positive electrospray ionization was selected to detect ibrutinib and vilazodone. Acetonitrile was used to precipitate protein to extract plasma samples. There was no endogenous interference for both ibrutinib and vilazodone and the linear range of this method was 1–2000 ng/mL. The recoveries were 98.4, 97.4 and 102.7% at low, medium and high concentrations. Accordingly, the matrix effect was 96.6, 111.1 and 99.6%. The pharmacokinetic difference between ibrutinib crude and a novel ibrutinib nanocrystalline in rats was investigated by this validated method successfully. The peak concentration and area under the concentration–time curve showed significant differences in gender and the bioavailability was improved after oral administration of ibrutinib nanocrystalline.

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Pharmaceutical Amorphous Nanoparticles

Cited by 146 publications

References 170 publications

Preparation and Characterization of Itraconazole- or Miconazole-Loaded PLGA Microspheres

Preparation and Characterization of Itraconazole- or Miconazole-Loaded PLGA Microspheres

Recrystallization and Production of Spherical Submicron Particles of Sulfasalazine Using a Supercritical Antisolvent Process

A rapid and sensitive method for quantification of ibrutinib in rat plasma by UPLC–ESI–MS/MS: validation and application to pharmacokinetic studies of a novel ibrutinib nanocrystalline

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