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Journal : Science and Technology Indonesia

Preparation and Evaluation of Antihypercholesterolemic Activity of Atorvastatin Calcium-Maleic Acid Co-Amorphous Solids Yudi Wicaksono; Shofiatul Izzah Al Amaliyah; Finas Rahmayanti; Viddy Agustian Rosidi; Lina Winarti; Dwi Setyawan
Science and Technology Indonesia Vol. 7 No. 2 (2022): April
Publisher : Research Center of Inorganic Materials and Coordination Complexes, FMIPA Universitas Sriwijaya

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (1488.708 KB) | DOI: 10.26554/sti.2022.7.2.202-207

Abstract

Atorvastatin calcium is a statin drug used for antihypercholesterolemic. The oral bioavailability of atorvastatin calcium is relatively low because it is poorly soluble in water. The low oral bioavailability of the drug causes a decrease in its therapeutic effectiveness. This study aimed to increase the solubility of atorvastatin calcium through the formation of co-amorphous solids and evaluate its activity as antihypercholesterolemic. Atorvastatin calcium was prepared into co-amorphous solids with a maleic acid coformer using the spray drying method. Solids characterization was carried out using Powder X-Ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Fourier Transforms Infra Red (FTIR), and Scanning Electronic Microscopy (SEM). The solubility test was carried out using the shaking method, while the evaluation of antihypercholesterolemic was carried out in vivo in experimental animals. The results of the analysis of diffractograms, thermograms, FTIR spectra, and micrograph images showed that the atorvastatin calcium-maleic acid solids prepared by spray drying were a co-amorphous solid. The atorvastatin calcium-maleic acid co-amorphous solids had a greater solubility in water (p<0.05) when compared to pure atorvastatin calcium. However, the in vivo antihypercholesterolemic activity results in experimental animals showed that the cholesterol-lowering activity of the atorvastatin calcium-maleic acid co-amorphous solidswas not significantly different (p>0.05) with pure atorvastatin calcium. This phenomenon is thought to be because atorvastatin calcium from co-amorphous solids in solution is more present as a charged fraction, affecting the permeability and absorption process.
Increasing the Solubility and Anti-Inflammatory Activity of Curcumin by Cocrystallization Yudi Wicaksono; Kuni Zu’aimah Barikah; Amanda Della Yudatama; Havidhatul Maulia; Nuri; Dwi Setyawan
Science and Technology Indonesia Vol. 8 No. 3 (2023): 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.2023.8.3.501-508

Abstract

Curcumin (CUR) is a polyphenolic compound that exhibits potent anti-inflammatory activity. However, only a tiny amount of CUR is absorbed during oral administration, which is because CUR is difficult to dissolve in water. The aim of the research was to increase the solubility of CUR through the cocrystallization technique using isonicotinamide coformer (INIC) by solvent evaporation. Cocrystal characterization was carried out using a powder X-ray diffractometer (PXRD), a differential scanning calorimeter (DSC), a Fourier transform infrared spectrometer (FTIR), and a scanning electron microscope (SEM). Solubility was evaluated using the shaking method, while the anti-inflammatory activity test was carried out using the carrageenan induced mouse leg edema method. The resulting CUR-INIC (1:1) cocrystal has a diffractogram with new diffraction peaks of 2theta at 15.00, 16.22, and 22.89◦ compared to the individual diffractograms of CUR and INIC. In the cocrystal, CUR and INIC form intermolecular interactions of hydrogen bonds, resulting in a new solid phase with a melting point of 160.1◦C. The solubility of the CUR-INIC cocrystal in water was 73.1±0.23 ug/mL, which increased 14 times compared to the solubility of initial CUR, which was only 5.05±0.07 ug/mL. The CUR-INIC cocrystal showed a percentage of edema inhibition in mice (5 hours) 130% more potent than that of initial CUR. Therefore, CUR-INIC cocrystals can be used to improve CUR solubility to obtain more excellent anti-inflammatory effects.
Quercetin in Drug Carriers: Polymer Composite, Physical Characteristics, and In vitro Study Kurniawan, Muhammad Fariez; Setyawan, Dwi; Hariyadi, Dewi Melani
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.2024.9.2.380-412

Abstract

Quercetin is a highly prevalent flavonoid commonly found in a wide variety of fruits and vegetables. This compound has various biological actions, indicating great potential in preventing diseases and promoting health but the disadvantages include low solubility and instability. The disadvantages can be overcome by using a polymer composite in the form of microspheres in the formulation. Therefore, this study aimed to review various uses of polymers in delivering quercetin compounds. The results showed that various polymers in microspheres have been formulated with quercetin to minimize the weaknesses. The delivery systems developed and reported from several related studies include microencapsulation, microcapsules, microparticles, microspheres, solid lipid microparticles (SLM), and nanoparticles. Polymers including Gelatine, Maltodextrin and Inulin, Carnauba wax, Poly (lactic-co-glycolic acid (PLGA), Gyceryl behenate, Pectin, Nano-hydroxyapatite, Polycaprolactone, Starch, Chitosan, Eudragit S 100, Sodium Alginate, Ethyl cellulose, and Alumina efficiently improved the properties of quercetin, enabling the utilization as a controlled drug delivery agent. Therefore, developing a quercetin delivery system using composite polymers presents both an opportunity and a challenge for future applications.
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.
Ferulic Acid-Nicotinamide Cocrystal: Synthesis, Experimental, and Computation Study Pujiono, Fery Eko; Ekowati, Juni; Amrillah, Tahta; Setyawan, Dwi
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.2025.10.2.402-410

Abstract

Ferulic acid-nicotinamide cocrystals have been successfully synthesized using the solvent evaporation method. In this case, nicotinamide which acts as a coformer is mixed with ferulic acid with a 1:1 molar ratio via dissolving process in ethanol. The obtained cocrystals were characterized through Differential Scanning Calorimetric (DSC), Powder X-Ray Diffraction (PXRD), Fourier-transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), and computational analyses. The DSC characterization revealed distinct endothermic peaks at 99.5°C and 128.5°C with a W-shaped profile. This result is different from the thermal behavior of pure ferulic acid which indicates that the ferulic acid-nicotinamide cocrystal is successfully formed. This result is also supported by the PXRD result which reveals distinct peaks at 5.24°, 16.31°, and 34.69° belong to crystal deformation of ferulic acid cocrystal due to the coexistence of nicotinamide coformer. The FTIR data also further indicate the formation of cocrystals marked by the disappearance of the NH(v) functional group at 3400 cm−1 and the emergence of a fuse-like peak at around 1600 cm−1 corresponding to the C-O(v) and NH() functional groups. SEM analysis also demonstrated morphological differences between the obtained cocrystal with pure ferulic acid crystals. The pure ferulic acid crystals exhibit a rectangular shape, whereas the cocrystals display a sword-like morphology. The phenomenon of cocrystal formation was also studied using computational studies through Density Functional Theory (DFT) and Quantum Theory of Atoms in Molecules (QTAIM) which confirmed that the cocrystals were stabilized through intermolecular hydrogen bonding.
Adsorptions of Sodium Ion/Atom on Graphene Quantum Dots for Battery Applications: A DFT Study Mulya, Fadjar; Nugroho, Muhammad Adi; Kuamit, Thanawit; Setyawan, Dwi
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.2025.10.2.614-621

Abstract

Sodium-ion batteries (SIBs) are emerging as a cost-effective and sustainable alternative to lithium-ion batteries, yet they face challenges such as lower energy density and electrode material instability. This study explores the potential of coronene and circumcoronene-based graphene quantum dots (GQDs) as anode materials for SIBs, focusing on three adsorption areas: central, intermediate, and edge, under two battery conditions: charging and discharging. By addressing these limitations through advanced nanostructuring, we employeddensityfunctional theory (DFT) withtheM06-2X/6-31G+(d)leveloftheorytoconductcomprehensive analyses of sodium adsorption on GQDs. Our findings reveal that both coronene and circumcoronene GQDs preferentially adsorb sodium at the edge areas due to the highest energy adsorption. In discharging conditions, coronene exhibited an adsorption energy of-1.09 kcal/mol, while circumcoronene showed-9.84 kcal/mol. In charging conditions, the adsorption energies were-33.44 kcal/mol for coronene and-37.19 kcal/mol for circumcoronene. Additionally, the energy gap of GQDs was significantly reduced after sodium adsorption, from 5.84 eV to 1.38 eV for coronene and from 4.33 eV to 1.63 eV for circumcoronene. Both GQDs showed theoretical voltages in the range of 1.40 to 1.47 V for coronene and 1.19 to 1.22 V for circumcoronene, respectively. Conclusively, our study recommends circumcoronene as large-sized GQDs as optimal SIB anode materials, offering higher adsorption energy, good conductivity, and reasonable electrochemical performance. This research addresses a theoretical gap by illuminating the impact of Na adsorption on GQDmolecular and electronic structures, aiding in the design of enhanced capacity nano-anodes for SIBs.
Pectin Red Dragon Fruit Peel Pectin-Based Microspheres for Oral Quercetin Delivery: Characterization, Stability Study, Digestion Resistance, and Cytotoxicity Against HeLa Cells Kurniawan, Muhammad Fariez; Setyawan, Dwi; Hariyadi, Dewi Melani
Science and Technology Indonesia Vol. 10 No. 4 (2025): October
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.2025.10.4.1049-1073

Abstract

This study aims to evaluate the potential of red dragon fruit skin pectin to be used as a polymer compared with commercial pectin in the quercetin microsphere. Microspheres were made using the ionic gelation technique. Ten formulas were created, utilizing pectin from red dragon skin extracted with oxalic acid (OA75), citric acid (CA75), acetic acid (AA75), and commercial pectin at 1% and 1.5% concentrations. A gel permeation chromatography test (GPC) was performed to evaluate pectin’s molecule weight. Parameters were assessed, including yield, moisture content (MC), Carr’s Index, Hausner ratio, swelling index, Fourier Transform Infrared Spectroscopy (FTIR), particle size, polydispersity index (PDI), drug loading (DL), encapsulation efficiency (EE), Scanning Electron Microscope (SEM), in vitro drug release, accelerated stability test at a temperature of 40±2oC and RH 75±5% for 3 months and thermal stability test in the form of DSC and XRD at the same temperature and humidity for 9 months, digestion resistance with incubation in artificial stomach and intestinal solution for 4 hours continued with cytotoxicity test on HeLa cells with MTT Assays. Results of FTIR indicate a strong interaction between quercetin and pectin in forming a stable microsphere structure; SEM showed the spheres morphologically. The kinetics of quercetin release from microspheres was the Korsmeyer-Peppas model. DL and EE had no significant differences for 3 months and no significant changes in the glass transition in the DSC test during testing until month 9. The FF formulation (1.5% AA75) had the highest cytotoxic activity against HeLa cells and a high Selectivity Index.
Microwave-Assisted Synthesis: A Green Chemistry Approach for Drug Cocrystals Synthesis Puspita, Oktavia Eka; Sulistyowaty, Melanny Ika; Salam, Rudy; Setyawan, Dwi
Science and Technology Indonesia Vol. 10 No. 4 (2025): October
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.2025.10.4.1130-1147

Abstract

Microwave-assisted synthesis (MAS) presents a promising approach to the formation of pharmaceutical cocrystals, offering notable improvements in solubility, dissolution rate, stability, and bioavailability of active pharmaceutical ingredients (APIs). This review aims to evaluate the potential of MAS as a green and efficient strategy for drug cocrystal synthesis, particularly in comparison to conventional methods such as solvent evaporation, slurry crystallisation, and grinding techniques. A systematic literature review was conducted following PRISMA (Preferred Reporting Items for Systematic Reviews and Meta-Analyses) guidelines, to ensure a comprehensive selection of relevant studies. The analysis focused on reported synthesis methods, cocrystal formation under microwave exposure, reaction conditions, yields, purity, and scalability outcomes of MAS compared to conventional techniques. This review also highlight current applications, critical synthesis parameters, and challenges such as penetration depth, reaction uniformity, and thermal control. Findings indicate that MAS significantly reduces reaction time, minimizes solvent use, and enhances product purity and yield. Its compatibility with solvent-free or minimal-solvent processes aligns closely with green chemistry principles, making it a sustainable alternative. Furthermore, MAS effectively addresses solubility mismatches and process inefficiencies commonly encountered in traditional methods. The future prospect of MAS lies in its integration with continuous manufacturing, automation, and drug repurposing efforts, which could revolutionize pharmaceutical formulation by accelerating innovation while adhering to environmental and regulatory standards.
Enhancing In Vitro Dissolution of Ferulic Acid Through Co-Crystal Formation Using Malonic Acid and Nicotinamide Co-formers Setyawan, Dwi; Soraya, Yasmin; Ekowati, Juni; Winantari, Agnes Nuniek; Rani, Karina Citra; Kanzaffa, Firly Afnauriza Tedja; Pujiono, Ferry Eko
Science and Technology Indonesia Vol. 10 No. 4 (2025): October
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.2025.10.4.1255-1269

Abstract

Ferulic acid is categorized as a Biopharmaceutical Classification System (BCS) class II drug, which exhibits low solubility in water (0.91 mg/mL). The formation of a co-crystal using malonic acid and nicotinamide as co-formers by the microwave irradiation method is an approach to enhance its solubility and dissolution. This study aims to evaluate the effect of co-crystal formation using these two co-formers at a 1:1 molar ratio on the solubility and dissolution of ferulic acid. The result emphasizes the formation of new peaks and peak shifting compared to the pure materials characterized from the Fourier Transform Infrared (FT-IR) spectrum. Moreover, the Differential Scanning Calorimetry (DSC) thermogram exhibits the differences in the co-crystal melting point compared to the pure drug and co-former, indicating the alteration of molecular structure on the crystal lattice of ferulic acid caused by the strong interaction between supramolecular homomer and heteromeric synthon. The formation of a new crystalline phase is also observed from the X-ray Diffraction (XRD) diffractogram, suggesting the formation of a different phase from its co-crystal component. The morphology characterization using Scanning Electron Microscope (SEM) revealed that the ferulic acid crystal habit changes into different forms, which is acclaimed as a co-crystal formation. The results of this study also disclosed that the co-crystal formation of ferulic acid significantly enhances ferulic acid solubility and dissolution characteristics compared to the pure drug and physical mixture (p < 0.05). The enhancement of solubility is 11.85% and 10.39% for ferulic acid–malonic acid and ferulic acid–nicotinamide co-crystal, respectively. Moreover, the dissolution rate of ferulic acid increases 3.50-fold and 3.61-fold from the formation of those co-crystals. Therefore, the formation of ferulic acid–malonic acid as well as ferulic acid–nicotinamide co-crystals in a 1:1 molar ratio by the microwave irradiation method is effective in improving ferulic acid solubility and dissolution.
Co-Authors AA Sudharmawan, AA Abdulkadir Rahardjanto, Abdulkadir Achmad Radjaram Agnes Nuniek Winanta Ahmad Zainul AM Mufarrih Amanda Della Yudatama Astuti, Ely Setyo Atok Miftachul Hudha Auzal Halim Bambang Widjaja Bambang Widjaja Bambang Widjaja Bambang Widjaja Betari, Sita Desti Bhisma Murti Bidarinjani, Mouria D Budianta, D Dafa C, Muhammad Dewanthy, Kyrana Sekar Dewi Isadiartuti Dewi Melani Hariyadi Dicky Pratama Dina Ayu Fatmawati Diyah, Nuzul Wahyuning Ekojono Ekojono Erizal Zaini Fadjar Mulya Fajar R, Allak Farid, Saif Aiman Fatati, Muhibbah Fatkur Rhohman, Fatkur Fauzi Ahmad Muda Fauzia, Alfi Nur Fendy Hardian Permana Ferdinand Hukama Taqwa Fery Eko Pujiono, Fery Eko Fikria, Laila Hidayatul Finas Rahmayanti Gatot Sugiarto Gilkes, Robert Hafidz, Moh Handayani, Ning Rahayu Hartanto, Agus Dwi Havidhatul Maulia Herlina Hanum, Herlina HERMANU JOEBAGIO Ichsan Luqmana Indra Putra, Ichsan Luqmana Indra Idha Kusumawati Iin Hindun Ina Sholihah Widiati, Ina Sholihah Indah Sayekti Indah Sayekti, Indah Juni Ekowati Kanzaffa, Firly Afnauriza Tedja Kuamit, Thanawit Kuni Zu’aimah Barikah Kurdi Wijaya, Moh Kurniawan, Muhammad Fariez Lina Winarti Maghzarini, Nessa Regitha Marcellino Rudyanto Maren, A Maria Lucia Ardhani Dwi Lestari Martinus, Ali Melanny Ika Sulistyowaty Misbahul Munir Moh. Mirza Nuryady Muhammad Adi Nugroho Muhammad Setiyawan Muhibbah Fatat Muhibbah Fatati Ningsih, Cica Trimandasari Noorma Rosita Novira Widajanti, Novira Nugroho, Surya Adi Nurhayati Damiri Nuri Nuruddin, Mahrus Naufal Nurwidodo, Nurwidodo Oktavia Eka Puspita, Oktavia Eka Paramita, Diajeng Putri Paserena, Karinda Dwi Prameswari, Putu Pradnya Mimba Pratiwi, Ambar Priatna, S J Pujiono, Ferry Eko Raden Joko Kuncoroningrat Susilo Rani, Karina Citra Refraugati, Irwandi Retno Sari Rohana, Melissa Rosalin Ismayoeng Gusdian Rudy Salam, Rudy Samsun hadi Sari, Ketut Intan Yunika Septiani, Annisa Eka Shofiatul Izzah Al Amaliyah Siammita, Dhea Anansya Siswandono, S. Siswandono, Siswandono Soraya, Yasmin Sukma Adhi Permata Sundani N. Soewandhi, Sundani N. Syafi'ie, Hisyam Tahta Amrillah Tongway, David Tri Agus Siswoyo Utami, Inggita Viddy Agustian Rosidi Wahyu Prihanta Warsito Warsito Widji Soeratri Winantari, Agnes Nuniek Yuanita Windusari Yudi Wicaksono Yudi Wicaksono Yudi Wicaksono Yuli Ainun Najih Zidan, Sabry A. H. Zimy Fianti Ningtyas Zimy Fianti Ningtyas, Zimy Fianti