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. 2022 Oct 24;7(44):39907-39912.
doi: 10.1021/acsomega.2c04021. eCollection 2022 Nov 8.

Preparation and Characterization of Aprepitant Solid Dispersion with HPMCAS-LF

Jinwen Liu  1   2 , Yongji Li  2 , Wuliji Ao  3 , Yingge Xiao  1 , Meirong Bai  4 , Shuyan Li  1
Affiliations

Preparation and Characterization of Aprepitant Solid Dispersion with HPMCAS-LF

Jinwen Liu et al. ACS Omega. .

Abstract

This study focused on improving the physicochemical characteristics of aprepitant with poor water solubility by preparing solid dispersion (SD). To prepare the SD with HPMCAS-LF, the solvent evaporation method was applied. Based on dissolution analysis, the dissolution rate of SD increased by five times compared with aprepitant. In addition, scanning electron microscopy (SEM), X-ray powder diffraction (XRPD), and differential scanning calorimetry (DSC) results suggested the presence of amorphous-form aprepitant inside SD. According to Fourier transform infrared (FTIR) spectroscopy, intermolecular hydrogen bonds were detected between polymer and aprepitant. The Caco-2 cell experiment proved that SD did not lower the transepithelial electrical resistance (TEER) values but improved the permeation amount of aprepitant. Additionally, the SD of aprepitant displayed excellent stability.

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Conflict of interest statement

The authors declare no competing financial interest.

Figures

Figure 1
Figure 1
Aprepitant and SD dissolution profiles under diverse aprepitant/HPMCAS-LF ratios (1:5, 1:4, 1:3). All points stand for mean ± SD (n = 3).
Figure 2
Figure 2
DSC curves for (A) aprepitant, (B) HPMCAS-LF, (C) 1:4 physical mixture, and (D) SD.
Figure 3
Figure 3
XRPD spectra for (A) aprepitant, (B) HPMCAS-LF, (C) 1:4 physical mixture, and (D) 1:4 SD.
Figure 4
Figure 4
FTIR spectra of (A) aprepitant, (B) HPMCAS-LF, (C) 1:4 physical mixture, and (D) 1:4 SD.
Figure 5
Figure 5
SEM photomicrographs of 1:4 PM (A), 1:4 SD (10000X) (B), and 1:4 SD (50000X) (C).
Figure 6
Figure 6
Amount of aprepitant permeated through Caco-2 cells.
Figure 7
Figure 7
TEER values for the Caco-2 cells pre- and postpermeation tests.
Figure 8
Figure 8
Aprepitant dissolution rate of diverse samples within 30 min.
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