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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.
Preparation and Characterization of a Eutectic Mixture of Fenofibric Acid and Nicotinic Acid and Evaluatuion of In Vivo Antihyperlipidemic Activity Deni Anggraini; Hulwa Salsabila; Salman Umar; Yufri Aldi; Erizal Zaini
Science and Technology Indonesia Vol. 7 No. 4 (2022): October
Publisher : Research Center of Inorganic Materials and Coordination Complexes, FMIPA Universitas Sriwijaya

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (1086.036 KB) | DOI: 10.26554/sti.2022.7.4.514-521

Abstract

Fenofibric Acid (FA) is classified under Biopharmaceutical Classification System (BCS) class II due to its poorly soluble in water and high permeability. The present study aimed to prepare the eutectic mixture of FA with nicotinic acid (NA) and characterize its solid state properties and in vitro dissolution rate, along with its in vivo antihyperlipidemic activity. Solvent drop grinding was the method chosen to prepare the eutectic mixture of FA and NA. Solid-state properties were evaluated using thermal analysis Differential Scanning Calorimetry (DSC), crystallographic analysis Powder X-Ray Diffraction (PXRD), FT-IR spectroscopic analysis, and Scanning Electron Microscopy (SEM). To examine in vivo antihyperlipidemic activity, 16 male Swiss Webster rats were injected with 1% hyperlipidemia-inducing solution, followed by the oral administration of 9.45 mg/kg FA and NA (equivalent to 9.45 mg/kg FA), after which the decrease in cholesterol levels was measured. Two-way ANOVA was used to evaluate the data, followed by Duncan’s multiple range test (95% confidence interval). The results proved that FA formed the eutectic mixture with NA at a molar ratio of 6:4. The eutectic mixture of FA-NA had a better solubility and in vitro dissolution rate compared to intact FA, which also led to notably improved antihyperlipidemic activity.
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.
A Comparison Study between Green Synthesis of Microwave Irradiation and Solvent Evaporation Methods in The Formation of p-Methoxycinnamic Acid-Succinic Acid Cocrystals Sulistyowaty, Melanny Ika; Setyawan, Dwi; Prameswari, Putu Pradnya Mimba; Susilo, Raden Joko Kuncoroningrat; Amrillah, Tahta; Zaini, Erizal; Zidan, Sabry A. H.
Science and Technology Indonesia Vol. 9 No. 3 (2024): July
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.2024.9.3.629-636

Abstract

Cocrystal of p-Methoxycinnamate acid-succinic acid has been produced by microwave irradiation and solvent evaporation methods. Cocrystals are formed using succinic acid as the coformer at a molar ratio of 1:1. The formation of cocrystal can be done by solvent evaporation method and microwave radiation method. Physicochemical properties have been studied by FT-IR, DSC, PXRD, and SEM analysis. The solubility test was carried out with pH 6.8 phosphate buffer at a temperature of 25±0.5°C for 5 hours and the dissolution test was carried out with 900 mL pH 6.8 phosphate buffer at a temperature of 37±0.5°C with the speed of 75 rpm using a paddle-type dissolution test apparatus. The solubility of PMCA has increased its solubility in cocrystals by the solvent evaporation method by 1.19 times and by the microwave radiation method by 1.16 times compared to PMCA. The dissolution rate of the cocrystals of the solvent evaporation method increased by 3.50 times and the cocrystals of the microwave radiation method increased by 2.29 times compared to PMCA.
Ketoprofen-Tromethamine: Binary Phase Diagram of Multicomponent Crystal, Dissolution Rate, and Analgesic Activity Evaluation Hasanah, Uswatul; Badriyya, Elsa; Safitri, Reza; Yuliza, Sukma; Ihsan, Ikhwanul; Saafrida; Rosaini, Henni; Jessica, Adhitya; Zaini, Erizal
Science and Technology Indonesia Vol. 9 No. 3 (2024): July
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.2024.9.3.726-734

Abstract

Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID) whose formulation options are limited due to its low dissolution rate in aqueous media. This research aimed to enhance the solubility of ketoprofen in distilled water and to compare the anti-inflammatory and analgesic effects of its resulting multicomponent crystal with tromethamine. The binary phase diagram of ketoprofen-tromethamine was created across molar ratios ranging from 1:9 to 9:1. The multicomponent crystal comprising ketoprofen and tromethamine in the selected ratio was synthesized using a solvent drop grinding method and subjected to further characterization for thermal properties, crystallinity, chemical groups, and morphology. The dissolution rate assessments were evaluated in CO2-free distilled water. Pharmacological analyses examined the anti-inflammatory and analgesic effects of the multicomponent crystal. The binary phase analysis identified the 5:5 (1:1) molar ratio as optimal in forming a multicomponent crystal. Thermograms and diffractograms revealed crystalline alterations attributed to a new crystalline phase. The new multicomponent crystal exhibited approximately 2.7 times higher dissolution rate after 30 minutes, outperforming pure ketoprofen. Pharmacological assessments demonstrated superior analgesic effects of the multicomponent crystal. In summary, the ketoprofen-tromethamine cocrystal in 1:1 molar ratio offers enhanced dissolution rate and provides better analgesic activity than ketoprofen alone.
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.
Ticagrelor Solubility and Dissolution Rate Enhancement Using Mesoporous Silica SBA-15 Hasanah, Uswatul; Rizky, Fattihatul; Mohd Amin, Mohd Cairul Iqbal; Zaini, Erizal
Science and Technology Indonesia Vol. 10 No. 2 (2025): 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.2025.10.2.598-604

Abstract

Ticagrelor is a triazolopyrimidine antiplatelet agent with poor water solubility. Ticagrelor was incorporated into mesoporous silica SBA15 in this study to evaluate its physical stability and improve its solubility and dissolution rate. TEOS was employed as a silica precursor and Pluronic P123 as a template to synthesize SBA-15. Ticagrelor was loaded into SBA-15 at a mass ratio of 1:1. Physicochemical characterization was conducted using nitrogen adsorption-desorption isotherm analysis, powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), fourier-transform infrared spectroscopy (FT-IR), and scanning electron microscopy (SEM). Ticagrelor solubility and dissolution were tested using distilled water as the medium. To evaluate the physical stability, Ticagrelor-SBA-15 was stored in a climatic chamber at 75% RH and 40°C for a month and analyzed using PXRD. Physicochemical characterization indicated efficient adsorption of ticagrelor into the SBA-15 pores, resulting in an amorphous form of solid material. Meanwhile, solubility and dissolution rate testing showed respective increases of 1.33 times and 1.74 times with significant differences (p<0.05) while maintaining its physical stability after storage for one month. Based on this study, it can be concluded that the incorporation of  mesoporous SBA-15 significantly enhances ticagrelor’s solubility and dissolution rate while maintaining stability.
Amine-Functionalized Mesoporous Silica SBA-15 for Enhanced Solubility and Release Rate of Gliclazide Sayyidina, Fasqina; Gumala, Azhoma; Zaini, Erizal; Hanifa, Dini; Hasanah, Uswatul
Science and Technology Indonesia Vol. 10 No. 3 (2025): July
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.2025.10.3.963-971

Abstract

Gliclazide (GLI), a sulfonylurea-class antidiabetic drug, exhibits poor aqueous solubility, limiting its bioavailability. This study aimed to enhance gliclazide’s solubility and dissolution rate by adsorbing it into mesoporous silica SBA-15 and amine-functionalized SBA-15 (SBA-15-A). SBA-15 was synthesized using Pluronic® P123 as a template and tetraethyl orthosilicate (TEOS) as the silica precursor, while 3-aminopropyltriethoxysilane (APTES) was used to introduce amine functional groups. Gliclazide was loaded into SBA-15 and SBA-15-A at a 1:3 mass ratio. The materials (GLI, SBA-15, SBA-15-A, GLI-SBA, and GLI-SBA-A) were characterized using nitrogen adsorption-desorption isotherms, differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), transmission electron microscopy (TEM), and powder X-ray diffraction (PXRD). Characterization revealed that the pore diameters of SBA-15 and SBA-15-A were 6.079 nm and 5.483 nm, respectively. FT-IR confirmed the interaction between gliclazide and the mesoporous carriers. SEM and TEM analysis showed crystalline gliclazide and rod-shaped morphologies for the mesopores samples. DSC and PXRD results indicated that most of the gliclazide had been converted to an amorphous form. Solubility testing over 24 hours showed that GLI-SBA and GLI-SBA-A improved gliclazide solubility by 1.375- and 2.334-fold, respectively, compared to pure gliclazide. Dissolution testing in distilled water revealed a 6.033-fold and 3.887-fold increase in the release rate at 5 minutes for GLI-SBA and GLI-SBA-A, respectively. Both solubility and release rate improvements were statistically significant (p <0.05). These findings suggest that amine functionalization of SBA-15 effectively enhances the solubility and dissolution rate of gliclazide.
Co-Authors -, Salman Adhitya Jessica Agusri Boestari Agustina, Annisa Akmal Djamaan Amri Bakhtiar Andarifera, Alya Zahira Annisa Agustina Aprilianti, Hizra Dwi Arif, Zhafira Asiska Permata Dewi Asiska Permata Dewi Asiska Permatadewi Auzal Halim Auzal Halim Azzahra, Cindy Maynia Ben, Elfi Sahlan Deni Anggraini Deni Noviza Dhea Sultana Lutfiyah DINI HANIFA, DINI Dwi Setyawan Ellyza Nasrul Elpa Giovana Zola Elsa Badriyya Elvi Rahma Yulisman Elvita Sari Fadhila, Muthia Fauzi Saputra Fifi Harmely Friardi Ismed Gaesari, Sherly Rahmah Gaesari, Sherly Rahmah Gumala, Azhoma Habibie Deswilyaz Ghiffari Hansen Nasif Haq AH, Ahdi Dinil Hasmiwati Helen Sonita Henny Lucida Hulwa Salsabila Ihsan, Ikhwanul Ima Kurniati Irna Kurniati Jessica, Adhitya Kiki Rizky Wirza Kurniati, Irna Lili Fitriani Mai Efdi Maria Dona Octavia Melanny Ika Sulistyowaty Melisa Melisa Melzi Octaviani Mohd Amin, Mohd Cairul Iqbal Muhammad Taher Muthia Fadhila Mutiara Zulkarnaini Najmi Hilaliyati Netty Novitasari Nova Syafni Novica Sari Prameswari, Putu Pradnya Mimba Raden Joko Kuncoroningrat Susilo Rahmadasmi, Nola Rahmadevi Rahmi Nofita Rahmi Yosmar Rahmi Yosmar Resva Meinisasti Revila, Gusti Reza Safitri Rifka Naura Rini Agustin Rini Agustin Rizky, Fattihatul Rosaini, Henni Rose Intan Perma Sari Rustini Rustini Rustini Rustini S, Agnes Saafrida Saafrida Saafrida Saafrida Saafrida Salman - Salman - Salman Salman Salman Umar Sari, Elvita Sayyidina, Fasqina Simbolon, Clara Alverina Sundani N. Soewandhi Sundani N. Soewandhi, Sundani N. Syofyan Syofyan SYUKRAN HAMDENI Syukriati Chaira Tahta Amrillah Trisfa Augia Try Andy Sahputra Try Andy Sahputra Usman, Hendrizal Uswatul Hasanah Uswatul Hasanah, Uswatul Verlia Nisrina Putri Vike Zulia Putri Vina Oktavia Yeni Novita Sari Yeyet C. Sumirtapura Yufri Aldi Yuliza, Sukma Yuska Noviyanty Zahara Gayo Zidan, Sabry A. H. Zulhadjri Zulhadjri