Synthesis of Carrier-Free Paclitaxel–Curcumin Nanoparticles: The Role of Curcuminoids
The systemic administration of paclitaxel (PTX)-based combinatorial therapies is significantly restricted due to the multidrug resistance. Curcumin (CUR) not only inhibits cancer-cell proliferation but also reverses the PTX resistance. However, achieving codelivery of these two drugs is a challenge...
| Main Authors: | , , , , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-12-01
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| Series: | Bioengineering |
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| Online Access: | https://www.mdpi.com/2306-5354/9/12/815 |
| _version_ | 1797461398757834752 |
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| author | Sena Karaosmanoglu Yunsen Zhang Wenli Zhou Defang Ouyang Xianfeng Chen |
| author_facet | Sena Karaosmanoglu Yunsen Zhang Wenli Zhou Defang Ouyang Xianfeng Chen |
| author_sort | Sena Karaosmanoglu |
| collection | DOAJ |
| description | The systemic administration of paclitaxel (PTX)-based combinatorial therapies is significantly restricted due to the multidrug resistance. Curcumin (CUR) not only inhibits cancer-cell proliferation but also reverses the PTX resistance. However, achieving codelivery of these two drugs is a challenge due to their poor water solubility. Herein, we synthesized carrier-free PTX NPs by a facile nanoprecipitation method with the help of CUR and other curcuminoids present in turmeric extract. The prepared NPs demonstrated spherical morphologies with high conformational stability. Experimental studies showed that the presence of both bisdemethoxycurcumin and demethoxycurcumin is essential for the successful formation of spherical and monodisperse NPs. Computational studies revealed that the presence of the more sterically available curcuminoids BMC and DMC makes the self-assembly procedure more adaptable with a higher number of potential conformations that could give rise to more monodisperse PTX-CUR NPs. Compared with PTX alone, PTX-CUR NPs have shown comparable therapeutic efficiency in vitro and demonstrated a higher cellular internalization, highlighting their potential for in vivo applications. The successful formation of PTX-CUR NPs and the understanding of how multiple drugs behave at the molecular level also provide guidance for developing formulations for the synthesis of high-quality and effective carrier-free nanosystems for biomedical applications. |
| first_indexed | 2024-03-09T17:18:52Z |
| format | Article |
| id | doaj.art-1101a164c4424c74a80e82c8c8f5509b |
| institution | Directory Open Access Journal |
| issn | 2306-5354 |
| language | English |
| last_indexed | 2024-03-09T17:18:52Z |
| publishDate | 2022-12-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Bioengineering |
| spelling | doaj.art-1101a164c4424c74a80e82c8c8f5509b2023-11-24T13:21:31ZengMDPI AGBioengineering2306-53542022-12-0191281510.3390/bioengineering9120815Synthesis of Carrier-Free Paclitaxel–Curcumin Nanoparticles: The Role of CurcuminoidsSena Karaosmanoglu0Yunsen Zhang1Wenli Zhou2Defang Ouyang3Xianfeng Chen4School of Engineering, Institute for Bioengineering, University of Edinburgh, Edinburgh EH9 3JL, UKState Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences (ICMS), University of Macau, Macao 999078, ChinaDepartment of Medical Oncology, Changzheng Hospital, Naval Medical University, Shanghai 200070, ChinaState Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences (ICMS), University of Macau, Macao 999078, ChinaSchool of Engineering, Institute for Bioengineering, University of Edinburgh, Edinburgh EH9 3JL, UKThe systemic administration of paclitaxel (PTX)-based combinatorial therapies is significantly restricted due to the multidrug resistance. Curcumin (CUR) not only inhibits cancer-cell proliferation but also reverses the PTX resistance. However, achieving codelivery of these two drugs is a challenge due to their poor water solubility. Herein, we synthesized carrier-free PTX NPs by a facile nanoprecipitation method with the help of CUR and other curcuminoids present in turmeric extract. The prepared NPs demonstrated spherical morphologies with high conformational stability. Experimental studies showed that the presence of both bisdemethoxycurcumin and demethoxycurcumin is essential for the successful formation of spherical and monodisperse NPs. Computational studies revealed that the presence of the more sterically available curcuminoids BMC and DMC makes the self-assembly procedure more adaptable with a higher number of potential conformations that could give rise to more monodisperse PTX-CUR NPs. Compared with PTX alone, PTX-CUR NPs have shown comparable therapeutic efficiency in vitro and demonstrated a higher cellular internalization, highlighting their potential for in vivo applications. The successful formation of PTX-CUR NPs and the understanding of how multiple drugs behave at the molecular level also provide guidance for developing formulations for the synthesis of high-quality and effective carrier-free nanosystems for biomedical applications.https://www.mdpi.com/2306-5354/9/12/815hydrophobic anticancer drugscurcuminpaclitaxelcarrier-free nanoparticlesself-assemblymolecular modeling |
| spellingShingle | Sena Karaosmanoglu Yunsen Zhang Wenli Zhou Defang Ouyang Xianfeng Chen Synthesis of Carrier-Free Paclitaxel–Curcumin Nanoparticles: The Role of Curcuminoids Bioengineering hydrophobic anticancer drugs curcumin paclitaxel carrier-free nanoparticles self-assembly molecular modeling |
| title | Synthesis of Carrier-Free Paclitaxel–Curcumin Nanoparticles: The Role of Curcuminoids |
| title_full | Synthesis of Carrier-Free Paclitaxel–Curcumin Nanoparticles: The Role of Curcuminoids |
| title_fullStr | Synthesis of Carrier-Free Paclitaxel–Curcumin Nanoparticles: The Role of Curcuminoids |
| title_full_unstemmed | Synthesis of Carrier-Free Paclitaxel–Curcumin Nanoparticles: The Role of Curcuminoids |
| title_short | Synthesis of Carrier-Free Paclitaxel–Curcumin Nanoparticles: The Role of Curcuminoids |
| title_sort | synthesis of carrier free paclitaxel curcumin nanoparticles the role of curcuminoids |
| topic | hydrophobic anticancer drugs curcumin paclitaxel carrier-free nanoparticles self-assembly molecular modeling |
| url | https://www.mdpi.com/2306-5354/9/12/815 |
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