Green One-Pot Synthesis of Thiazole Scaffolds Catalyzed by Reusable NiFe2O4 Nanoparticles: In Silico Binding Affinity and In Vitro Anticancer Activity Studies DOI Creative Commons

Satish Gudala,

Archi Sharma,

Aruna Lankada

et al.

ACS Omega, Journal Year: 2024, Volume and Issue: 9(36), P. 38262 - 38271

Published: Aug. 29, 2024

A facile, green, one-pot multicomponent synthesis strategy was employed to fabricate novel thiazole scaffolds incorporating phthalazine, pyridazine, and pyrido-pyridazine derivatives (4a–4o). This synthetic route entailed the reaction of an α-halo carbonyl compound (1) with thiosemicarbazide (2) various anhydrides (3a–3o), utilizing NiFe2O4 nanoparticles as a reusable catalyst in ethanol:water (1:1) solvent system. The cytotoxicity synthesized compounds meticulously assessed against three cancer cell lines, A375, HeLa, MCF-7, employing IC50 values (μM) benchmark, compared reference drug erlotinib. Compound 4n displayed remarkable efficacy A375 (0.87 ± 0.31 μM), HeLa (1.38 1.24 MCF-7 (1.13 0.96 μM) significantly surpassing erlotinib's values. Additionally, 4k, 4l, 4m, 4o demonstrated notable across all tested indicating their potential effective anticancer agents. In silico docking studies Hsp82 Hsp90 proteins indicated that ligands 4c, 4j, 4o, 4l had superior binding affinities ADME analysis showed 4n, favorable pharmacokinetic profiles, including nontoxicity, high human intestinal absorption, low CYP inhibitory promiscuity. Structure–activity relationship revealed cyano benzylidene substitutions enhanced activity. Overall, compounds, particularly efficacy, interactions, promising making them strong candidates for further development

Language: Английский

Self-Emulsifying Drug Delivery Systems (SEDDS): Transition from Liquid to Solid—A Comprehensive Review of Formulation, Characterization, Applications, and Future Trends DOI Creative Commons
Prateek Uttreja, Indrajeet Karnik,

Ahmed Adel Ali Youssef

et al.

Pharmaceutics, Journal Year: 2025, Volume and Issue: 17(1), P. 63 - 63

Published: Jan. 5, 2025

Self-emulsifying drug delivery systems (SEDDS) represent an innovative approach to improving the solubility and bioavailability of poorly water-soluble drugs, addressing significant challenges associated with oral delivery. This review highlights advancements applications SEDDS, including their transition from liquid solid forms, while formulation strategies, characterization techniques, future prospects in pharmaceutical sciences. The systematically analyzes existing studies on focusing classification into forms preparation methods, spray drying, hot-melt extrusion, adsorption onto carriers. Characterization techniques such as droplet size analysis, dissolution studies, solid-state evaluations are detailed. Additionally, emerging trends, 3D printing, hybrid systems, supersaturable SEDDS (Su-SEDDS), explored. Liquid (L-SEDDS) enhance absorption by forming emulsions upon contact gastrointestinal fluids. However, they suffer stability leakage issues. Transitioning (S-SEDDS) has resolved these limitations, offering enhanced stability, scalability, patient compliance. Innovations personalized 3D-printed biologics delivery, targeted demonstrate potential for diverse therapeutic applications. Computational modeling silico approaches further accelerate optimization. have revolutionized enabling precise, patient-centric therapies. While scalability excipient toxicity persist, technologies multidisciplinary collaborations paving way next-generation SEDDS. Their adaptability medicine solidify role a cornerstone modern development.

Language: Английский

Citations

3
Design and development of Dasatinib nanoemulsions for ocular delivery: In vitro characterization, biocompatibility, and Ex vivo ocular irritation study DOI

Richa Khadke,

Amol Shete,

Akanksha Dashawant

et al.

International Journal of Pharmaceutics, Journal Year: 2025, Volume and Issue: unknown, P. 125504 - 125504

Published: March 1, 2025

Language: Английский

Citations

0
Nanoemulsion for enhanced absorption and anti-tumor activity of dasatinib DOI
Dina A. Eltahan, Rania K. Eid, Shimaa M. Ashmawy

et al.

Journal of Drug Delivery Science and Technology, Journal Year: 2025, Volume and Issue: unknown, P. 106870 - 106870

Published: March 1, 2025

Language: Английский

Citations

0
Green One-Pot Synthesis of Thiazole Scaffolds Catalyzed by Reusable NiFe2O4 Nanoparticles: In Silico Binding Affinity and In Vitro Anticancer Activity Studies DOI Creative Commons

Satish Gudala,

Archi Sharma,

Aruna Lankada

et al.

ACS Omega, Journal Year: 2024, Volume and Issue: 9(36), P. 38262 - 38271

Published: Aug. 29, 2024

A facile, green, one-pot multicomponent synthesis strategy was employed to fabricate novel thiazole scaffolds incorporating phthalazine, pyridazine, and pyrido-pyridazine derivatives (4a–4o). This synthetic route entailed the reaction of an α-halo carbonyl compound (1) with thiosemicarbazide (2) various anhydrides (3a–3o), utilizing NiFe2O4 nanoparticles as a reusable catalyst in ethanol:water (1:1) solvent system. The cytotoxicity synthesized compounds meticulously assessed against three cancer cell lines, A375, HeLa, MCF-7, employing IC50 values (μM) benchmark, compared reference drug erlotinib. Compound 4n displayed remarkable efficacy A375 (0.87 ± 0.31 μM), HeLa (1.38 1.24 MCF-7 (1.13 0.96 μM) significantly surpassing erlotinib's values. Additionally, 4k, 4l, 4m, 4o demonstrated notable across all tested indicating their potential effective anticancer agents. In silico docking studies Hsp82 Hsp90 proteins indicated that ligands 4c, 4j, 4o, 4l had superior binding affinities ADME analysis showed 4n, favorable pharmacokinetic profiles, including nontoxicity, high human intestinal absorption, low CYP inhibitory promiscuity. Structure–activity relationship revealed cyano benzylidene substitutions enhanced activity. Overall, compounds, particularly efficacy, interactions, promising making them strong candidates for further development

Language: Английский

Citations

0