Development of sorafenib loaded nanoparticles to improve oral bioavailability using a quality by design approach

Park, Sang Yeob; Kang, Zion; Thapa, P.; Jin, Yong Suk; Park, Joo Won; Lim, Hye Jung; Lee, Jae Young; Lee, Sa-Won; Seo, Min-Hyo; Kim, Min‐Soo; Jeong, Seong Hoon

doi:10.1016/j.ijpharm.2019.05.064

Cited by 45 publications

(26 citation statements)

References 51 publications

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“…Similarly, the oral bioavailability and solubility of curcumin (a polyphenol and turmeric compound) can be improved by loading into PEGylated SL NPs (Ban et al, 2020). The bioavailability and solubility of many other potential drugs such as astilbin, sorafenib, apigenin, and astaxanthin also have been reported to be improved following the encapsulation into NPs (Huang et al, 2019;Liu et al, 2019;Park et al, 2019;Zheng and Zhang, 2019). Together, the data above suggest that NPs can potentially increase the solubility and bioavailability of less-soluble drugs, therefore improving their efficacy.…”

Section: Nps Improve the Solubility And Bioavailability Of Conventionmentioning

confidence: 99%

The Application of Nanotechnology for the Diagnosis and Treatment of Brain Diseases and Disorders

Ngowi

Wang

Qian

et al. 2021

Front. Bioeng. Biotechnol.

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Brain is by far the most complex organ in the body. It is involved in the regulation of cognitive, behavioral, and emotional activities. The organ is also a target for many diseases and disorders ranging from injuries to cancers and neurodegenerative diseases. Brain diseases are the main causes of disability and one of the leading causes of deaths. Several drugs that have shown potential in improving brain structure and functioning in animal models face many challenges including the delivery, specificity, and toxicity. For many years, researchers have been facing challenge of developing drugs that can cross the physical (blood–brain barrier), electrical, and chemical barriers of the brain and target the desired region with few adverse events. In recent years, nanotechnology emerged as an important technique for modifying and manipulating different objects at the molecular level to obtain desired features. The technique has proven to be useful in diagnosis as well as treatments of brain diseases and disorders by facilitating the delivery of drugs and improving their efficacy. As the subject is still hot, and new research findings are emerging, it is clear that nanotechnology could upgrade health care systems by providing easy and highly efficient diagnostic and treatment methods. In this review, we will focus on the application of nanotechnology in the diagnosis and treatment of brain diseases and disorders by illuminating the potential of nanoparticles.

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Section: Nps Improve the Solubility And Bioavailability Of Conventionmentioning

confidence: 99%

The Application of Nanotechnology for the Diagnosis and Treatment of Brain Diseases and Disorders

Ngowi

Wang

Qian

et al. 2021

Front. Bioeng. Biotechnol.

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“…Therefore, the optimum point was identified in the region where the concentration of SLS was 1.0 mg/mL, to minimize the use of the surfactant. Based on the desirability function, the optimal values of the parameters were obtained by graphical and numerical analyses using Design Expert ® 11.0 and the formulation that could produce robust products with the targeted quality characteristics was determined [41][42][43]. The combined formulation (PVP VA64, PVP K12, and SLS) that maximized the desirability function was identified (10.0 mg/mL, 5.0 mg/mL, and 1.0 mg/mL).…”

Section: Establishment Of the Design Spacementioning

confidence: 99%

Development of a Resveratrol Nanosuspension Using the Antisolvent Precipitation Method without Solvent Removal, Based on a Quality by Design (QbD) Approach

Kuk

et al. 2019

Pharmaceutics

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The purpose of this study was to develop a resveratrol nanosuspension with enhanced oral bioavailability, based on an understanding of the formulation and process parameters of nanosuspensions and using a quality by design (QbD) approach. Particularly, the antisolvent method, which requires no solvent removal and no heating, is newly applied to prepare resveratrol nanosuspension. To ensure the quality of the resveratrol nanosuspensions, a quality target product profile (QTPP) was defined. The particle size (z-average, d90), zeta potential, and drug content parameters affecting the QTPP were selected as critical quality attributes (CQAs). The optimum composition obtained using a 3-factor, 3-level Box–Behnken design was as follows: polyvinylpyrrolidone vinyl acetate (10 mg/mL), polyvinylpyrrolidone K12 (5 mg/mL), sodium lauryl sulfate (1 mg/mL), and diethylene glycol monoethyl ether (DEGEE, 5% v/v) at a resveratrol concentration of 5 mg/mL. The initial particle size (z-average) was 46.3 nm and the zeta potential was −38.02 mV. The robustness of the antisolvent process using the optimized composition conditions was ensured by a full factorial design. The dissolution rate of the optimized resveratrol nanosuspension was significantly greater than that of the resveratrol raw material. An in vivo pharmacokinetic study in rats showed that the area under the plasma concentration versus time curve (AUC0–12h) and the maximum plasma concentration (Cmax) respectively, than those of the resveratrol raw material. Therefore, the prepara values of the resveratrol nanosuspension were approximately 1.6- and 5.7-fold higher,tion of a resveratrol nanosuspension using the QbD approach may be an effective strategy for the development of a new dosage form of resveratrol, with enhanced oral bioavailability.

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“…SYO-1644 is a sorafenib-loaded nanoparticle formed by applying Nanoparticulation Using Fat and Supercritical Fluid (NUFS TM ) technology to improve the solubility. [ 10 ]. A higher solubility profile was achieved for SYO-1644 by optimizing the particle size and dissolution profile using design space [ 10 ].…”

Section: Introductionmentioning

confidence: 99%

“…[ 10 ]. A higher solubility profile was achieved for SYO-1644 by optimizing the particle size and dissolution profile using design space [ 10 ]. This was confirmed in a pharmacokinetic study in beagle dogs [ 10 ].…”

Section: Introductionmentioning

confidence: 99%

Population Pharmacokinetic Modelling and Simulation to Determine the Optimal Dose of Nanoparticulated Sorafenib to the Reference Sorafenib

Huh

Hwang

Park³

et al. 2021

Pharmaceutics

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Sorafenib, an oral multikinase inhibitor, exhibits a highly variable absorption profile due to enterohepatic reabsorption and poor solubility. SYO-1644 improved the solubility of sorafenib by nanoparticulation technology leading to enhanced bioavailability. To evaluate the pharmacokinetically equivalent dose of SYO-1644 to the reference Nexavar® 200 mg, a randomized, open-label, replicated two-period study was conducted in healthy volunteers. A total of 32 subjects orally received a single dose of the following assigned treatment under a fasted state in the first period and repeated once more in the second period with a two-week washout: SYO-1644 100, 150 and 200 mg and Nexavar® 200 mg. Pharmacokinetic (PK) samples were collected up to 168 h post-dose. The PK profile was evaluated by both non-compartmental analysis and population PK method. With the final model, 2 × 2 crossover trial scenarios with Nexavar® 200 mg and each dose of SYO-1644 ranging from 100 to 150 mg were repeated 500 times by Monte Carlo simulation, and the proportion of bioequivalence achievement was assessed. Transit absorption compartments, followed by a one-compartment model with first-order elimination and enterohepatic reabsorption components were selected as the final model. The simulation results demonstrated that the SYO-1644 dose between 120 and 125 mg could yielded the highest proportion of bioequivalence.

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Development of sorafenib loaded nanoparticles to improve oral bioavailability using a quality by design approach

Cited by 45 publications

References 51 publications

The Application of Nanotechnology for the Diagnosis and Treatment of Brain Diseases and Disorders

The Application of Nanotechnology for the Diagnosis and Treatment of Brain Diseases and Disorders

Development of a Resveratrol Nanosuspension Using the Antisolvent Precipitation Method without Solvent Removal, Based on a Quality by Design (QbD) Approach

Population Pharmacokinetic Modelling and Simulation to Determine the Optimal Dose of Nanoparticulated Sorafenib to the Reference Sorafenib

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