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Open AccessArticle

Development of a Thymoquinone Polymeric Anticancer Nanomedicine through Optimization of Polymer Molecular Weight and Nanoparticle Architecture

1
Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman 11733, Jordan
2
Department of Biopharmaceutics and Clinical Pharmacy, School of Pharmacy, University of Jordan, Amman 11942, Jordan
3
Smart Medical Labs, Amman 11180, Jordan
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(9), 811; https://doi.org/10.3390/pharmaceutics12090811
Received: 3 August 2020 / Revised: 12 August 2020 / Accepted: 24 August 2020 / Published: 27 August 2020
(This article belongs to the Special Issue Nano-Micro Encapsulation of Drugs)
Thymoquinone (TQ) is a water-insoluble natural compound isolated from Nigella sativa 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)-b-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 (Cmax) 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. View Full-Text
Keywords: thymoquinone; polymeric nanoparticles; mPEG-PCL; anticancer nanomedicine; drug delivery thymoquinone; polymeric nanoparticles; mPEG-PCL; anticancer nanomedicine; drug delivery
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MDPI and ACS Style

Sunoqrot, S.; Alfaraj, M.; Hammad, A.M.; Kasabri, V.; Shalabi, D.; Deeb, A.A.; Hasan Ibrahim, L.; Shnewer, K.; Yousef, I. Development of a Thymoquinone Polymeric Anticancer Nanomedicine through Optimization of Polymer Molecular Weight and Nanoparticle Architecture. Pharmaceutics 2020, 12, 811.

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