Thymoquinone (TQ) is a water-insoluble natural compound isolated from that has demonstrated promising chemotherapeutic activity. The purpose of this study was to develop a polymeric nanoscale formulation for TQ to circumvent its delivery challenges. TQ-encapsulated nanoparticles (NPs) were fabricated using methoxy poly(ethylene glycol)--poly(ε-caprolactone) (mPEG-PCL) copolymers by the nanoprecipitation technique. Formulation variables included PCL chain length and NP architecture (matrix-type nanospheres or reservoir-type nanocapsules). The formulations were characterized in terms of their particle size, polydispersity index (PDI), drug loading efficiency, and drug release. An optimized TQ NP formulation in the form of oil-filled nanocapsules (F2-NC) was obtained with a mean hydrodynamic diameter of 117 nm, PDI of 0.16, about 60% loading efficiency, and sustained in vitro drug release. The formulation was then tested in cultured human cancer cell lines to verify its antiproliferative efficacy as a potential anticancer nanomedicine. A pilot pharmacokinetic study was also carried out in healthy mice to evaluate the oral bioavailability of the optimized formulation, which revealed a significant increase in the maximum plasma concentration (C) and a 1.3-fold increase in bioavailability compared to free TQ. Our findings demonstrate that the versatility of polymeric NPs can be effectively applied to design a nanoscale delivery platform for TQ that can overcome its biopharmaceutical limitations.
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http://dx.doi.org/10.3390/pharmaceutics12090811 | DOI Listing |
Int J Biol Macromol
January 2025
Center of Nanoscience, Nanotechnology, and Innovation - CeNano2I, Department of Metallurgical and Materials Engineering, Federal University of Minas Gerais, UFMG, Brazil. Electronic address:
B-cell non-Hodgkin lymphoma (NHL) is the most common hematologic malignancy, capable of invading the brain, meninges, and nerve roots of the brain and spine, leading to high lethality. Herein, we designed and developed novel nanostructures for the first time by biofunctionalizing chitosan with two specific antibodies (i.e.
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January 2025
BK21 Program, Department of Applied Life Science, Konkuk University, Chungju 27478, Republic of Korea.
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January 2025
Molecular Science and Biomedicine Laboratory (MBL), State Key Laboratory of Chemo/Biosensing and Chemometrics, College of Chemistry and Chemical Engineering, Aptamer Engineering Center of Hunan Province, Hunan University, Changsha, Hunan 410082, China.
Adv Healthc Mater
January 2025
Hangzhou Institute of Medicine, Chinese Academy of Sciences, Hangzhou, Zhejiang, 310022, China.
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January 2025
Shanghai Key Laboratory of Hydrogen Science & Center of Hydrogen Science, School of Materials Science and Engineering, Shanghai Jiao Tong University, Shanghai, 200240, China.
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