4.6 Article

Synthesis, structure and antidiabetic activity of chromium(III) complexes of metformin Schiff-bases

Journal

JOURNAL OF MOLECULAR STRUCTURE
Volume 1108, Issue -, Pages 60-70

Publisher

ELSEVIER
DOI: 10.1016/j.molstruc.2015.11.055

Keywords

Metformin Schiff-bases; Cr3+ complexes; Spectral and thermal properties; Antidiabetes mellitus

Ask authors/readers for more resources

A series of Cr3+ complexes with Schiff-bases of metformin with each of salicylaldehyde (HL1); 2,3-dihydroxybenzaldehyde (H2L2); 2,4-dihydroxybenzaldehyde (H2L3); 2,5-dihydroxybenzaldehyde (H2L4); 3,4-dihydroxybenzaldehyde (H2L5) and 2-hydroxynaphthaldehyde (HL6) were synthesized by template reaction. The new compounds were characterized through elemental analysis, conductivity and magnetic moment measurements, IR, UV Vis., NMR and mass spectroscopy. The complexes have octahedral structure with mu value of hexacoordinated chromium ion. TGA, DTG and DTA analysis confirm the proposed stereochemistry and a mechanism for thermal decomposition was proposed. Thermodynamic parameters are calculated for the second and third decomposition steps. [(CrLCI)-C-4(H2O)(2)].3H(2)O and [CrL5Cl(H2O)(2)].21/2H(2)O were able to produce significant decreases in the blood glucose level. (C) 2015 Elsevier B.V. All rights reserved.

Authors

I am an author on this paper
Click your name to claim this paper and add it to your profile.

Reviews

Primary Rating

4.6
Not enough ratings

Secondary Ratings

Novelty
-
Significance
-
Scientific rigor
-
Rate this paper

Recommended

Article Medicine, Research & Experimental

Saponin-rich extract of Tribulus terrestris alleviates systemic inflammation and insulin resistance in dietary obese female rats: Impact on adipokine/hormonal disturbances

Yousra Abdel-Mottaleb, Howaida S. Ali, Mohamed K. El-Kherbetawy, Amany Y. Elkazzaz, Mohamed H. ElSayed, Amr Elshormilisy, Amira H. Eltrawy, Sally Y. Abed, Asma M. Alshahrani, Abdullah A. Hashish, Eman Saad Alamri, Sawsan A. Zaitone

Summary: This study examines the potential therapeutic effect of a saponin-rich extract of Tribulus terrestris (TTS) on dietary obesity in female rats. The results show that TTS can control inflammatory burden, improve insulin resistance and body weight gain, and ameliorate reproductive system pathologies.

BIOMEDICINE & PHARMACOTHERAPY (2022)

Article Chemistry, Multidisciplinary

Formulation and Characterization of Doxycycline-Loaded Polymeric Nanoparticles for Testing Antitumor/Antiangiogenic Action in Experimental Colon Cancer in Mice

Reem Alshaman, Abdullah Alattar, Rehab M. El-Sayed, Ahmed R. Gardouh, Rabie E. Elshaer, Amany Y. Elkazaz, Mohamed Ahmed Eladl, Mohamed El-Sherbiny, Noha E. Farag, Ahmed Mohsen Hamdan, Sawsan A. Zaitone

Summary: The study formulated doxycycline-loaded polymeric nanoparticles and tested their characteristics and drug release rate. In animal experiments, the doxycycline-loaded nanoparticles showed enhanced antitumor activity and reduced angiogenesis indicators.

NANOMATERIALS (2022)

Article Cardiac & Cardiovascular Systems

Ethnicity affects the risk factors of acute myocardial infarction and should be considered in educational programs

Umar Abdolah Alharbe, Hanad Hassan Alatawi, Palanisamy Amirthalingam, Sultan Mohammed Daghriri, Alanoud Abduallah Alhwiti, Tahani Saud Alenazi, Abdulelah Turki S. Al Ahmare, Sawsan A. Zaitone, Ahmed Aljabri, Ahmed Mohsen Hamdan

Summary: This study compared the risk factors of acute myocardial infarction among Saudi nationals and expatriates and found significant differences, suggesting a potential genetic contribution to the risk factors.

FRONTIERS IN CARDIOVASCULAR MEDICINE (2022)

Article Chemistry, Analytical

Two Eco-Friendly Chromatographic Methods Evaluated by GAPI for Simultaneous Determination of the Fluoroquinolones Moxifloxacin, Levofloxacin, and Gemifloxacin in Their Pharmaceutical Products

Eman A. Abdel Hameed, Zaitona A. Abd El-Naby, Alaa El Gindy, Roshdy E. Saraya, Aisha Nawaf Al Balawi, Sawsan A. Zaitone, Gasser M. Khairy

Summary: Novel green HPLC and HPTLC chromatographic methods were developed for the concurrent determination of moxifloxacin, levofloxacin, and gemifloxacin. Both methods were optimized, validated, and assessed using the Green analytical procedure index (GAPI). The results showed that these methods are suitable for pharmaceutical analysis and detection of cross-contamination during manufacturing processes.

SEPARATIONS (2022)

Article Medicine, Research & Experimental

Metformin suppresses LRG1 and TGFβ1/ALK1-induced angiogenesis and protects against ultrastructural changes in rat diabetic nephropathy

Hala M. F. Mohammad, Sahar Galal Gouda, Mohamed Ahmed Eladl, Amany Y. Elkazaz, Khaled S. Elbayoumi, Noha E. Farag, Amr Elshormilisy, Buthainah B. Al-Ammash, Ann Hegazy, Sozan M. Abdelkhalig, Abir S. Mohamed, Mohamed El-Dosoky, Sawsan A. Zaitone

Summary: This study investigates the molecular mechanisms leading to DN and the role of LRG1, ALK1, and TGF beta 1 in DN pathologic alterations. It also explores the protective action of metformin against DN and its influence on LRG1 and ALK1/TGF beta 1 induced renal angiogenesis. The results show that metformin has renoprotective effects in a diabetic model, partly mediated by downregulation of LRG1 and TGF beta 1/ALK1-induced renal angiogenesis.

BIOMEDICINE & PHARMACOTHERAPY (2023)

Correction Immunology

Inhibitory effect of valproate sodium on pain behavior in diabetic mice involves suppression of spinal histone deacetylase 1 and inflammatory mediators (vol 70 , pg 16, 2019)

Nehal M. Elsherbiny, Eman Ahmed, Ghada Abdel Kader, Yousra Abdel-mottaleb, Mohamed H. ElSayed, Amal M. Youssef, Sawsan A. Zaitone

INTERNATIONAL IMMUNOPHARMACOLOGY (2023)

Article Medicine, Research & Experimental

Soluble guanylate cyclase agonist, isoliquiritigenin attenuates renal damage and aortic calcification in a rat model of chronic kidney failure

Hebatallah Husseini Atteia, Eman Saad Alamri, Nizar Sirag, Nahla Salah Zidan, Raghad Humod Aljohani, Sharifa Alzahrani, Manar Hamed Arafa, Nanies Sameeh Mohammad, Mervat Elsayed Asker, Sawsan A. Zaitone, Amr Tawfik Sakr

Summary: This study investigated the potential of isoliquiritigenin, a bioflavonoid extracted from licorice roots, as a natural activator for soluble Guanylate Cyclase (sGC) in a chronic kidney disease (CKD) rat model. The results showed that isoliquiritigenin dose-dependently improved CKD-related renal and endothelial dysfunction, reduced fibrosis, apoptosis, and calcification, and attenuated inflammation and oxidative stress. These protective effects were associated with the activation of sGC, increased cGMP and its downstream PKG. However, co-treatment with a selective sGC inhibitor antagonized the therapeutic impact of isoliquiritigenin.

LIFE SCIENCES (2023)

Article Toxicology

Topiramate affords neuroprotection in diabetic neuropathy model via downregulating spinal GFAP/inflammatory burden and improving neurofilament production

Mohammed A. Attia, Nema Soliman, Mohamed Ahmed Eladl, Shymaa E. Bilasy, Taghrid B. El-Abaseri, Howaida S. Ali, Faten Abbas, Dalia Ibrahim, Noura M. S. Osman, Abdullah A. Hashish, Asma Alshahrani, Abir S. Mohamed, Sawsan A. Zaitone

Summary: The current study demonstrated that topiramate has a neuroprotective effect in mouse peripheral diabetic neuropathy and investigated the underlying mechanisms. Treatment with topiramate increased the hotplate latency time and von-Frey test pain threshold, alleviating pain in DN mice. Additionally, topiramate also attenuated axonal degeneration in sciatic nerves and suppressed the expression of GFAP and inflammatory cytokines while enhancing the plasticity of the spinal cord. This study reinforces the neuroprotective role of topiramate and provides insights into its mechanisms in alleviating neuropathy.

TOXICOLOGY MECHANISMS AND METHODS (2023)

Article Pharmacology & Pharmacy

Influence of Surface-Modification via PEGylation or Chitosanization of Lipidic Nanocarriers on In Vivo Pharmacokinetic/Pharmacodynamic Profiles of Apixaban

Mohamed F. Zaky, Taha M. Hammady, Shadeed Gad, Abdullah Alattar, Reem Alshaman, Ann Hegazy, Sawsan A. Zaitone, Mamdouh Mostafa Ghorab, Mohamed A. Megahed

Summary: Nanostructured lipid carriers (NLCs) have been studied for their potential to enhance the bioavailability and efficacy of drugs, and the surface modification of NLCs with chitosan and PEGylation has been investigated in this study. The results showed that both chitosanization and PEGylation improved the stability, bioavailability, and pharmacodynamic activity of NLCs loaded with apixaban. Chitosan-modified NLCs displayed better stability and enhanced anticoagulant activity, while PEGylated NLCs showed higher absorption profile in rats.

PHARMACEUTICS (2023)

Article Infectious Diseases

Tamarindus indica Extract as a Promising Antimicrobial and Antivirulence Therapy

Mohamed F. Ghaly, Marzough Aziz Albalawi, Mahmoud M. Bendary, Ahmed Shahin, Mohamed A. Shaheen, Abeer F. Abu Eleneen, Mohammed M. Ghoneim, Ayman Abo Elmaaty, Mohamed F. M. Elrefai, Sawsan A. Zaitone, Amira I. Abousaty

Summary: The worldwide crises of multi-drug-resistant bacterial infections have led to a search for alternative therapies. Our research group evaluated the antimicrobial activities of the ethanolic extract of Tamarindus indica, a traditional medicine. The extract showed promising antimicrobial activities against multi-drug-resistant pathogens, with confirmed mechanisms of action and antivirulence activities. We hope that pharmaceutical companies can utilize our findings to develop a new formulation of T. indica extract with other antibiotics.

ANTIBIOTICS-BASEL (2023)

Article Chemistry, Medicinal

alpha-Hederin Saponin Augments the Chemopreventive Effect of Cisplatin against Ehrlich Tumors and Bioinformatic Approach Identifying the Role of SDF1/CXCR4/p-AKT-1/NF kappa B Signaling

Samah M. M. Elaidy, Mohamed K. K. El-Kherbetawy, Sally Y. Y. Abed, Abdullah Alattar, Reem Alshaman, Mohamed Ahmed Eladl, Eman Saad Alamri, Aisha Nawaf Al Balawi, AbdelNaser Zaid, Amany Y. Y. Elkazzaz, Sozan M. M. Abdelkhalig, Ziad E. E. Hamed, Sawsan A. A. Zaitone

Summary: This study investigated the chemotherapeutic effect of alpha-hederin in combination with cisplatin on Ehrlich solid tumors in mice. The results showed that alpha-hederin significantly enhanced the chemotherapeutic efficacy of cisplatin against Ehrlich solid tumors by suppressing the signaling pathway of SDF1/CXCR4/p-AKT/NF kappa B.

PHARMACEUTICALS (2023)

Article Chemistry, Medicinal

Design and Optimization of Omeprazole-Curcumin-Loaded Hydrogel Beads Coated with Chitosan for Treating Peptic Ulcers

Eman J. Heikal, Rashad M. Kaoud, Shadeed Gad, Hatem I. Mokhtar, Afaf A. Aldahish, Wafa Ali Alzlaiq, Sawsan A. Zaitone, Yasser M. Moustafa, Taha M. Hammady

Summary: This study aimed to develop a pharmaceutical dosage form containing omeprazole and curcumin for treating experimental peptic ulcers. The complex of omeprazole and curcumin was loaded into alginate beads and coated with chitosan for sustained release. The formulated beads showed improved anti-ulcer effectiveness compared to free omeprazole or omeprazole-only-loaded beads. Evaluation: x/10

PHARMACEUTICALS (2023)

Article Polymer Science

Development of Novel pH-Sensitive Eudragit Coated Beads Containing Curcumin-Mesalamine Combination for Colon-Specific Drug Delivery

Eman J. Heikal, Rashad M. Kaoud, Shadeed Gad, Hatem I. Mokhtar, Abdullah Alattar, Reem Alshaman, Sawsan A. Zaitone, Yasser M. Moustafa, Taha M. Hammady

Summary: This research developed a drug delivery system by coating alginate/chitosan beads with Eudragit (R) S-100 to target the colon and effectively treat colitis. The coated beads showed controlled release of curcumin/mesalamine at different pH levels. The optimized formula demonstrated high entrapment efficiency, swelling, and bead size. It significantly reduced colitis, indicating its potential for treating ulcerative colitis.
Article Medicine, Research & Experimental

Memantine mitigates ROS/TXNIP/NLRP3 signaling and protects against mouse diabetic retinopathy: Histopathologic, ultrastructural and bioinformatic studies

Mohammed H. ElSayed, Khaled S. Elbayoumi, Mohamed Ahmed Eladl, Abeer A. K. Mohamed, Ann Hegazy, Nagla A. El-Sherbeeny, Mohammed A. Attia, Fatma Azzahraa Hisham, Mohamed A. K. Saleh, Abdelhakeem Elaskary, Khaled Morsi, Amna M. A. Mustsafa, Eman T. Enan, Sawsan A. Zaitone

Summary: Diabetic retinopathy (DRET) can lead to vision loss in adults, but there are limited therapeutic options available. This study investigated the neuroprotective effect of memantine, an anti-Alzheimer drug, in experimental DRET and its impact on ROS/TXNIP/NLRP3 signaling cascade. The results demonstrated that memantine attenuated retinal damage and reduced inflammation in DRET.

BIOMEDICINE & PHARMACOTHERAPY (2023)

Article Pharmacology & Pharmacy

Marula oil nanoemulsion improves motor function in experimental parkinsonism via mitigation of inflammation and oxidative stress

Reem Alshaman, Mona Qushawy, Hatem I. Mokhtar, Angie M. Ameen, Rehab M. El-Sayed, Eman Saad Alamri, Lamiaa M. Elabbasy, Ahmed M. N. Helaly, Walid F. Elkhatib, Eidah M. Alyahya, Sawsan A. Zaitone

Summary: This study demonstrated that treatment with M-Oil or M-NE improved motor performance in mice with experimental PD, enhanced anti-inflammatory and antioxidant actions, downregulated inflammatory markers and malondialdehyde levels, and improved physical characteristics by formulating M-Oil as M-NE.

FRONTIERS IN PHARMACOLOGY (2023)

Article Chemistry, Physical

Nine Cd2+ complexes containing 3,5-dimethylpyrazole and carboxylic acids: Synthesis, spectroscopic and crystallographic characterization

Xinlei Chen, Shiyi Chen, Xuele Lin, Jingxuan Zhou, Xingjun Gao, Yaoqi Zhen, Xiaodan Ma, Shouwen Jin, Linfang Shi, Hui Liu, Daqi Wang

Summary: Nine mixed-ligand Cd2+ complexes with different geometric structures were synthesized and characterized. The complexes exhibit various coordination modes and form both intra- and intermolecular hydrogen bonds.

JOURNAL OF MOLECULAR STRUCTURE (2024)

Article Chemistry, Physical

Investigation on photo-isomeric impurity of Roxadustat: Structure conformation, physicochemical characterization, interconversion feasibility and in vitro toxicological evaluation

Rupali Mahajan, Abhishek Sharma, Bhagyashree Patra, Lijo Mani, Parul Grover, Sandeep Kumar, Santosh Kumar Guru, Gananadhamu Samanthula, Amol G. Dikundwar, Amit Asthana

Summary: This research article provides a comprehensive characterization and toxicological assessment of a photoisomeric impurity of the antianemic drug Roxadustat. The impurity has a distinct structure compared to the drug and its formation due to light exposure is a concern. Through various experiments, including single crystal XRD, physicochemical characterization, and in vitro cytotoxicity assays, the researchers confirmed the structure of the impurity, evaluated its conversion with Roxadustat, and assessed its toxicological activity. These findings contribute to the understanding of drug stability, safety, and formulation development.

JOURNAL OF MOLECULAR STRUCTURE (2024)

Article Chemistry, Physical

Enhancing the optical, electrical, dielectric properties and antimicrobial activity of chitosan/gelatin incorporated with Co-doped ZnO nanoparticles: Nanocomposites for use in energy storage and food packaging

Laila S. Alqarni, Azzah M. Alghamdi, Nuha Y. Elamin, A. Rajeh

Summary: The solution casting method was used to produce a new type of nanocomposites made of chitosan, gelatin, and co-doped ZnO nanoparticles. The addition of 3.5% co-doped ZnO nanoparticles improved the physicochemical characteristics and antimicrobial effects of the nanocomposites, indicating their significant potential in food packaging and energy storage.

JOURNAL OF MOLECULAR STRUCTURE (2024)

Article Chemistry, Physical

Unraveling non-covalent interactions in bis-chalcone: A crystallographic and theoretical studies

Ruchi Gaur

Summary: The structure and intermolecular interactions of a newly synthesized bis-chalcone THXA were studied using experimental and computational methods. The importance of non-covalent interactions such as pi center dot center dot center dot pi, C-H center dot center dot center dot S, and C-H center dot center dot center dot pi was revealed.

JOURNAL OF MOLECULAR STRUCTURE (2024)

Article Chemistry, Physical

Hyaluronic acid drug conjugates for the treatment of skin hyperpigmentation

Andrii Bazylevich, Leonid Patsenker, Sarit Aviel-Ronen, Gary Gellerman

Summary: Drug combination therapy is commonly used for treating various skin disorders, but its effectiveness is often limited. In this study, researchers synthesized conjugates of anti-pigmenting drugs and hyaluronic acid (HA) to improve treatment efficacy. These HA-drug conjugates exhibited measurable drug release profiles and demonstrated superior depigmentation effects compared to control groups in a swine model.

JOURNAL OF MOLECULAR STRUCTURE (2024)

Article Chemistry, Physical

Molecular structures of eight hydrogen bond-mediated minoxidil adducts from different aryl acids

Xiaodan Ma, Xinlei Chen, Yaoqi Zhen, Xunjie Zheng, Chengzhe Shi, Shouwen Jin, Bin Liu, Bin Chen, Daqi Wang

Summary: Cocrystallization experiments between minoxidil and aryl acids coformers resulted in the successful formation of multi-component samples. The nature of these samples was determined using various techniques and their structural and supramolecular aspects were investigated. The outcomes revealed the importance of nonbonding contacts and different types of interactions in stabilizing and expanding the crystal structures.

JOURNAL OF MOLECULAR STRUCTURE (2024)

Article Chemistry, Physical

Nucleophilic transformation of 3-substituted-6,8-dimethylchromones with phenylhydrazine under various reaction conditions: Theoretical, spectroscopic characterization and in silico ADME studies

Najla A. Alshaye, Magdy A. Ibrahim, Al-Shimaa Badran

Summary: The chemical behavior of 3-substituted-6,8-dimethylchromones towards phenylhydrazine was examined. Different reaction conditions produced various products, and the molecular geometries and reactivity descriptors of the compounds were also investigated. The results suggest that these compounds are suitable for nonlinear optical applications.

JOURNAL OF MOLECULAR STRUCTURE (2024)

Article Chemistry, Physical

Synthesis, spectroscopic characterizations, DFT calculations and molecular docking studies of new quinoline-oxirane/piperidine/morpholine hybrids from quinoline gem-dicyanoepoxide

Hayette Alliouche, Houria Bouria, Rafik Bensegueni, Mounia Guergouri, Abdelmalek Bouraiou, Ali Belfaitah

Summary: In this paper, a combined experimental and theoretical study was conducted to synthesize and characterize new 2-quinolone-piperidine and -morpholine hybrids. The results from experiments were validated using computational calculations, and the affinity between these compounds and Acetylcholinesterase/Butyrylcholinesterase was estimated through molecular docking.

JOURNAL OF MOLECULAR STRUCTURE (2024)

Article Chemistry, Physical

A significantly fluorescence-enhanced probe for Al3+based on a new AIEgens Mn-based metal-organic frameworks

Wei-Min Chen, Juan-Juan Shao, Yi Zhang, Zhen-Dong Xue, Peng-Lai Liu, Jian-Ling Ni, Li-Zhuang Chen, Qiang Gao, Fang-Ming Wang

Summary: This study synthesized and characterized a novel Mn-based LMOF, and achieved good results in detecting heavy metal Al3+ in water, showing good stability, high selectivity and sensitivity. This provides new insights into the potential applications of Mn-based MOFs in chemical sensing.

JOURNAL OF MOLECULAR STRUCTURE (2024)

Article Chemistry, Physical

One-pot cocrystallization of mononuclear and 1D cobalt(II) complexes based on flexible triclopyr and 2,2′-bipyridine coligands: Structural analyses, conformation comparison, non-covalent interactions and magnetic properties

Jun-Xia Li, Yi-Jing Lu, Ke-Ying Quan, Li-Bing Wu, Xun Feng, Wei-Zhou Wang

Summary: This study synthesized two cobalt(II) complexes and analyzed their crystal structures using single-crystal X-ray diffraction. The results showed that the crystal structures of these complexes were different, and they exhibited different crystal packing and magnetic properties.

JOURNAL OF MOLECULAR STRUCTURE (2024)

Article Chemistry, Physical

Synthesis and characterization of supramolecular assembly probenecid cocrystal

Yang Li, Yan Zhang, Hong Xu, Min Li, Zhen Li, Zi-yu Song, Ji-shi Chen, Yan-Jun Liu, Yong Sun, Zhao Yang

Summary: This study reports the synthesis and solid-state characterization of a new pharmaceutical cocrystal, PRO-BPE, which can enhance the solubility of the highly water-insoluble prodrug probenecid. The PRO-BPE cocrystals were found to have superior water solubility compared to pure PRO. This research provides valuable insights into improving the solubility of poorly soluble drugs.

JOURNAL OF MOLECULAR STRUCTURE (2024)

Article Chemistry, Physical

Water soluble spiropyran for Hg2+sensing in water

Lucas G. B. Felicio, Bianca B. M. Vieira, Ivana S. Lula, Renata Diniz, Frank Alexis, Flavio B. Miguz, Frederico B. De Sousa

Summary: A novel spiropyran derivative was synthesized for heavy metals sensing in water. The results demonstrated that the new derivative can serve as a rapid, sensitive, and simple tool for detecting Hg2+ ions in water with high selectivity.

JOURNAL OF MOLECULAR STRUCTURE (2024)

Article Chemistry, Physical

Preparation and performance of superhydrophobic surfaces with low surface energy modified attapulgite

Junqing Meng, Jie Wang, Lijuan Wang, Chunhui Lyu, Haiyan Chen, Yingpei Lyu, Baisheng Nie

Summary: Material modification with low surface energy can achieve lower surface free energy on micro-and nano-rough structures, which is crucial for developing superhydrophobic surfaces. In this study, attapulgite (APT) was modified with alkylamine, alkylammonium salt, and stearic acid, and the interaction between low surface materials and attapulgite was explained. The results showed that the hydrophobicity of APT was significantly modified by the modifiers, and the surface free energy of the composites first decreased and then increased with increasing molecular number of low surface energy monomers.

JOURNAL OF MOLECULAR STRUCTURE (2024)

Article Chemistry, Physical

One-pot synthesis of ligand-free highly active Pd catalyst supported on NiFe spinel oxide for Suzuki-Miyaura cross-coupling reaction

Karan Goswami, Dipak Das, Parthasarathi Bera, Sounak Roy, Md. Motin Seikh, Prasanta Kumar Sinha, Arup Gayen

Summary: This work presents the development of a simple and highly active heterogeneous Pd catalyst for Suzuki-Miyaura carbon-carbon cross-coupling reaction. The NiPdFe-1 catalyst shows the best activity and stability among the prepared catalysts. It efficiently promotes the coupling reaction between aryl bromide and phenyl boronic acid under mild reaction conditions with high isolated yields.

JOURNAL OF MOLECULAR STRUCTURE (2024)

Article Chemistry, Physical

Design, development and characterization of the Apremilast and Indomethacin coamorphous system

Ekta Pardhi, Devendra Singh Tomar, Rahul Khemchandani, Gananadhamu Samanthula, Pankaj Kumar Singh, Neelesh Kumar Mehra

Summary: The main aim of this study was to prepare a drug-drug coamorphous system to improve the physiochemical properties, solubility and stability of Apremilast and Indomethacin. Various solid-state characterization techniques were used to characterize the prepared system. Molecular level interactions were studied using molecular modeling and ATR-FTIR and 1H NMR. Solubility and dissolution studies showed the benefits of the coamorphous system. The system was found to be stable for a period of five months. Permeation study also demonstrated improved flux for both drugs compared to their crystalline forms. The coamorphous system showed anti-psoriatic and anti-melanogenic activity based on molecular docking results. Overall, the developed CAM-based supersaturated system exhibited improved physicochemical properties and physical stability.

JOURNAL OF MOLECULAR STRUCTURE (2024)