Abstract
Background: The aim of this study was to develop and compare polymeric micelles of fucoidan, a sulfated polysaccharide, and hydrophobic drugs such as paclitaxel and curcumin. Paclitaxel and curcumin are both known for their medicinal properties, including anticancer efficacy. However, their very low water solubility, absorption and rapid metabolism leads to reduced bioavailability. To redress these problems and enhance anti-cancer therapeutics using fucoidan, polymeric micelles were synthesized from conjugates of fucoidan and hydrophobic drugs.
Methods: The chemical conjugation of fucoidan and hydrophobic drugs has been achieved by utilizing reactive functional groups on the molecules, such as carboxylic groups and hydroxyl groups.
Results: The micelles revealed a homogeneous spherical morphology, size, negative surface charge. Fourier transform infrared spectroscopy was used to investigate the physicochemical properties of the polymeric micelles, which form a self-assembled polymeric micelle in aqueous medium. The results of the in vitro release of curcumin and fucoidan showed that their release rates were higher at a pH of 4.5 than at a pH of 7.4. In contrast, the paclitaxel conjugate had a similar release profile at pH of 4.5 and pH of 7.4.
Conclusion: In the present work, we also found an effective drug delivery system that had the ability to release two types of anticancer drugs, fucoidan and hydrophobic drugs, in the tumour environment.
Keywords: Fucoidan, micelle, dual drug delivery, conjugate, paclitaxel, curcumin.
Anti-Cancer Agents in Medicinal Chemistry
Title:A Comparison of Fucoidan Conjugated to Paclitaxel and Curcumin for the Dual Delivery of Cancer Therapeutic Agents
Volume: 18 Issue: 9
Author(s): Nam H. Phan, Thao T. Ly, Minh N. Pham, Thinh D. Luu, Toi V. Vo, Phuong H.L. Tran and Thao T.D. Tran*
Affiliation:
- Department for Management of Science and Technology Development, Ton Duc Thang University, Ho Chi Minh City,Vietnam
Keywords: Fucoidan, micelle, dual drug delivery, conjugate, paclitaxel, curcumin.
Abstract: Background: The aim of this study was to develop and compare polymeric micelles of fucoidan, a sulfated polysaccharide, and hydrophobic drugs such as paclitaxel and curcumin. Paclitaxel and curcumin are both known for their medicinal properties, including anticancer efficacy. However, their very low water solubility, absorption and rapid metabolism leads to reduced bioavailability. To redress these problems and enhance anti-cancer therapeutics using fucoidan, polymeric micelles were synthesized from conjugates of fucoidan and hydrophobic drugs.
Methods: The chemical conjugation of fucoidan and hydrophobic drugs has been achieved by utilizing reactive functional groups on the molecules, such as carboxylic groups and hydroxyl groups.
Results: The micelles revealed a homogeneous spherical morphology, size, negative surface charge. Fourier transform infrared spectroscopy was used to investigate the physicochemical properties of the polymeric micelles, which form a self-assembled polymeric micelle in aqueous medium. The results of the in vitro release of curcumin and fucoidan showed that their release rates were higher at a pH of 4.5 than at a pH of 7.4. In contrast, the paclitaxel conjugate had a similar release profile at pH of 4.5 and pH of 7.4.
Conclusion: In the present work, we also found an effective drug delivery system that had the ability to release two types of anticancer drugs, fucoidan and hydrophobic drugs, in the tumour environment.
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Cite this article as:
Phan H. Nam, Ly T. Thao, Pham N. Minh, Luu D. Thinh, Vo V. Toi, Tran H.L. Phuong and Tran T.D. Thao*, A Comparison of Fucoidan Conjugated to Paclitaxel and Curcumin for the Dual Delivery of Cancer Therapeutic Agents, Anti-Cancer Agents in Medicinal Chemistry 2018; 18 (9) . https://dx.doi.org/10.2174/1871520617666171121125845
DOI https://dx.doi.org/10.2174/1871520617666171121125845 |
Print ISSN 1871-5206 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5992 |
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