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Journal : Science and Technology Indonesia

Crystal Engineering Approach in Physicochemical Properties Modifications of Phytochemical Dhea Sultana Lutfiyah; Lili Fitriani; Muhammad Taher; Erizal Zaini
Science and Technology Indonesia Vol. 7 No. 3 (2022): July
Publisher : Research Center of Inorganic Materials and Coordination Complexes, FMIPA Universitas Sriwijaya

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (1878.126 KB) | DOI: 10.26554/sti.2022.7.3.353-371

Abstract

Phytochemicals have been used to reduce the risk of diseases and maintain good health and well-being. However, most phytochemicals have a limitation in their physicochemical properties, which can be modified by reforming the shape of the crystals. Therefore, crystal engineering is a promising approach to optimize physicochemical characteristics of the active pharmaceutical ingredients (APIs) in a phytochemical without altering its pharmacological efficacy. Hence, this paper reviews current strategies for the use of crystal engineering to optimize physicochemical properties of phytochemicals, which is followed by the design of the synthesis and characterization of particular phytochemicals, including piperine (PIP), quercetin (QUE), curcumin (CUR), genistein (GEN), and myricetin (MYR). The literature indicates that crystal engineering of multicomponent crystals (MCCs) enhances phytochemical physicochemical properties, including solubility, dissolution rate, stability, and permeability. The MCCs provide a lower lattice energy and noncovalent bonding, which translate into lower melting points and weak intermolecular interactions that generate greater solubility, higher dissolution rate, and better stability of the APIs. Nevertheless, the absence of reported studies of phytochemical crystal engineering leads to a lack of variation in the selection of coformers, methods of preparation, and improvement of physicochemical properties. Therefore, more extensive evaluation of the design and physicochemical characteristics of phytochemicals using MCCs is necessary and manifests the opportunity to enhance the application of phytochemicals in the pharmaceutical industry.
Improvement of Solubility Usnic Acid Loaded on Mesoporous Silica SBA-15 and Physicochemical Characterization Fitriani, Lili; Azzahra, Cindy Maynia; Jessica, Adhitya; Hasanah, Uswatul; Zaini, Erizal
Science and Technology Indonesia Vol. 9 No. 2 (2024): April
Publisher : Research Center of Inorganic Materials and Coordination Complexes, FMIPA Universitas Sriwijaya

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.26554/sti.2024.9.2.251-259

Abstract

Usnic acid, a secondary metabolite of lichen Usnea sp., has several pharmacological activities, but it is poorly soluble in water. This study aimed to improve the solubility and dissolution rate of usnic acid loaded in mesoporous silica SBA-15 at a mass ratio of 1:1. and evaluate its physical stability. Physicochemical characterization was carried out via the nitrogen adsorption desorption isotherm, differential scanning calorimetry (DSC), Fourier transform infrared (FTIR) spectroscopy, and powder X-ray diffraction (PXRD). Usnic acid-loaded SBA-15 was stored at 40 °C with various relative humidities (RH) and then analyzed by PXRD for the physical stability. Usnic acid adsorbed well in the pores of SBA-15, as shown by a decrease in the volume pore and surface area of SBA-15 according to the nitrogen adsorption. Moreover, usnic acid-SBA-15 showed a decrease in the degree of crystallinity according to PXRD analysis and no melting point based on DSC analysis. The FTIR spectrum of usnic acid–SBA-15 corresponds to the spectra of each raw material. The solubility of usnic acid increased 5.15 times after adsorbed on SBA-15. The dissolution rate also showed a significant increase (p < 0.05) from 19.51% to 84.27%. Usnic acid–SBA-15 was relatively stable at RH 75%. Thus, the adsorption of usnic acid on SBA-15 can increase its solubility, dissolution rate, and physical stability.
Enhancing the Solubility and Dissolution Rate of Tenoxicam through Co-Amorphous Formation with Meglumine by a Solvent Dropped Grinding Method Fitriani, Lili; Arif, Zhafira; Hasanah, Uswatul; Zaini, Erizal
Science and Technology Indonesia Vol. 10 No. 1 (2025): January
Publisher : Research Center of Inorganic Materials and Coordination Complexes, FMIPA Universitas Sriwijaya

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.26554/sti.2025.10.1.131-138

Abstract

Tenoxicam is a non-steroidal anti-inflammatory drug (NSAID), one of the oxicam group. It is categorized as Biopharmaceutical Classification System class II, as its low solubility and high permeability. The aims of this research were to enhance the solubility and dissolution rate of tenoxicam by its modification into a co-amorphous phase with meglumine at a molar 1:1 ratio. The co amorphous form of tenoxicam-meglumine was prepared by a solvent drop grinding method, and characterized by thermal analysis using differential scanning calorimetry (DSC), solid phase by powder X-ray diffraction (PXRD), identification of functional group by Fourier-transform infrared (FT-IR) spectroscopy, and morphology by polarized light microscopy (PLM) and scanning electron microscopy (SEM). The solubility test was conducted in water, whereas the dissolution test was performed in 0.1 N HCl solution and water. The DSC thermogram demonstrated a decrease in the endothermic peak of the co-amorphous tenoxicam-meglumine. The PXRD diffractogram revealed a reduction in the peak intensity of the X-ray diffraction, which formed a halo pattern. The FT-IR spectroscopy analysis indicated the formation of the co-amorphous system. The co-amorphous of tenoxicam-meglumine solubility’s increased by 42.71-fold as compared to intact tenoxicam. The co-amorphous tenoxicam meglumine exhibited a dissolution rate of 92.71% and 100% in 0.1 N HCl and distilled water, respectively, after 60 minutes, and resulting in separate increases in dissolution efficiency by 3.05 and 9.12-times in 0.1 N HCl and distilled water. In summary, the formation of the co-amorphous phase of tenoxicam and meglumine successfully enhanced the solubility and dissolution of tenoxicam.