Preparation of Naringenin Nanosuspension and Its Antitussive and Expectorant Effects

Abstract

Naringenin (NRG) is a natural flavonoid compound abundantly present in citrus fruits and has the potential to treat respiratory disorders. However, the clinical therapeutic effect of NRG is limited by its low bioavailability due to poor solubility. To enhance the solubility, naringenin nanosuspensions (NRG-NSps) were prepared by applying tocopherol polyethylene glycol succinate (TPGS) as the nanocarrier via the media-milling method. The particle size, morphology, and drug-loading content of NRG-NSps were examined, and the stability was evaluated by detecting particle size changes in different physiological media. NRG-NSps exhibited a flaky appearance with a mean diameter of 216.9 nm, and the drug-loading content was 66.7%. NRG-NSps exhibited good storage stability and media stability. NRG-NSps presented a sustainable release profile, and the cumulative drug-release rate approached approximately 95% within 7 d. NRG-NSps improved the antitussive effect significantly compared with the original NRG, the cough frequency was decreased from 22 to 15 times, and the cough incubation period was prolonged from 85.3 to 121.6 s. Besides, NRG-NSps also enhanced expectorant effects significantly, and phenol red secretion was increased from 1.02 to 1.45 μg/mL. These results indicate that NRG-NSps could enhance the bioavailability of NRG significantly and possess a potential clinical application.

Optimization of Naringenin Nanoparticles to Improve the Antitussive Effects on Post-Infectious Cough

“…After optimizing the preparation conditions, the NRG NPs with a hydrodynamic diameter of 182.2 nm (PDI ~0.28) were obtained (Figure 1a). Transmission electron microscopy (TEM) results showed that the NRG NPs presented a sheet-like morphology (Figure 1b), which is consistent with our previous report [36].…”

“…Among them, TPGS has been utilized broadly as a nanocarrier to encapsulate NRG, because of its excellent amphiphilic properties, entrapment efficacy, and biosafety [34,35]. In our previous study, we prepared the NRG nanoparticles (NPs) with TPGS as a drug carrier via wet media milling, and the obtained NRG NPs exhibited good antitussive and expectorant effects [36].…”

Naringenin Ultrafine Powder Was Prepared by a New Anti-Solvent Recrystallization Method

“…The experimental reaction was carried out at 37°C. At a fixed time (5,15,30,45,60,75, 90 and 120 min), 0.2 mL samples were taken from each index at 8 different time points; the HPLC method was used to measure the dissolution rate of the samples and to draw the curve. The HPLC conditions were as follows: C18 column (4.6 × 100 mm 2 , 5 µm, Agilent LTD, Palo Alto, CA, USA).…”

“…However, raw naringenin directly isolated from plants exhibits a poor dissolution rate and low bioavailability, which greatly limits its clinical application [14]. Dong et al reported that reducing the particle sizes of insoluble substances by increasing their specific surface area is an effective method for increasing dissolution rate [15]. The bioavailability of these substances is effectively increased by preparation with ultrafine technology [16].…”

Preparation, Characterization, and Evaluation of Breviscapine Nanosuspension and Its Freeze-Dried Powder

“…The preparation technology of NS can be divided into top-down and bottom-up methods [ 17 ]. In the top-down approach, two methods have been commonly used: wet stirred media milling (WSMM) and high-pressure homogenization [ 23 ]. WSMM is the most widely used and preferred method for preparing drug nanosuspensions because the top-down approach can efficiently produce small particles and does not require organic solvents, making them more viable in industrial production.…”