High Solubilization and Controlled Release of Paclitaxel Using Thermosponge Nanoparticles for Effective Cancer Therapy
Cancer, which is a leading cause of death, contributes significantly to reducing life expectancy worldwide. Even though paclitaxel (PTX) is known as one of the main anticancer drugs, it has several limitations, including low solubility in aqueous solutions, a limited dosage range, an insufficient re...
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MDPI AG
2021-07-01
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Series: | Pharmaceutics |
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Online Access: | https://www.mdpi.com/1999-4923/13/8/1150 |
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author | Jin Sil Lee Hyeryeon Oh Daekyung Sung Jin Hyung Lee Won Il Choi |
author_facet | Jin Sil Lee Hyeryeon Oh Daekyung Sung Jin Hyung Lee Won Il Choi |
author_sort | Jin Sil Lee |
collection | DOAJ |
description | Cancer, which is a leading cause of death, contributes significantly to reducing life expectancy worldwide. Even though paclitaxel (PTX) is known as one of the main anticancer drugs, it has several limitations, including low solubility in aqueous solutions, a limited dosage range, an insufficient release amount, and patient resistance. To overcome these limitations, we suggest the development of PTX-loaded thermosponge nanoparticles (PTX@TNP), which result in improved anticancer effects, via a simple nanoprecipitation method, which allows the preparation of PTX@TNPs with hydrophobic interactions without any chemical conjugation. Further, to improve the drug content and yield of the prepared complex, the co-organic solvent ratio was optimized. Thus, it was observed that the drug release rate increased as the drug capacity of PTX@TNPs increased. Furthermore, increasing PTX loading led to considerable anticancer activity against multidrug resistance (MDR)-related colorectal cancer cells (HCT 15), implying a synergistic anticancer effect. These results suggest that the solubilization of high drug amounts and the controlled release of poorly water-soluble PTX using TNPs could significantly improve its anticancer therapy, particularly in the treatment of MDR-p-glycoprotein-overexpressing cancers. |
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institution | Directory Open Access Journal |
issn | 1999-4923 |
language | English |
last_indexed | 2024-03-10T08:29:04Z |
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spelling | doaj.art-338105f3c11e48368f725552fdcd25992023-11-22T09:13:13ZengMDPI AGPharmaceutics1999-49232021-07-01138115010.3390/pharmaceutics13081150High Solubilization and Controlled Release of Paclitaxel Using Thermosponge Nanoparticles for Effective Cancer TherapyJin Sil Lee0Hyeryeon Oh1Daekyung Sung2Jin Hyung Lee3Won Il Choi4Center for Convergence Bioceramic Materials, Convergence R&D Division, Korea Institute of Ceramic Engineering and Technology, 202, Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaCenter for Convergence Bioceramic Materials, Convergence R&D Division, Korea Institute of Ceramic Engineering and Technology, 202, Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaCenter for Convergence Bioceramic Materials, Convergence R&D Division, Korea Institute of Ceramic Engineering and Technology, 202, Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaCenter for Convergence Bioceramic Materials, Convergence R&D Division, Korea Institute of Ceramic Engineering and Technology, 202, Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaCenter for Convergence Bioceramic Materials, Convergence R&D Division, Korea Institute of Ceramic Engineering and Technology, 202, Osongsaengmyeong 1-ro, Osong-eup, Heungdeok-gu, Cheongju 28160, KoreaCancer, which is a leading cause of death, contributes significantly to reducing life expectancy worldwide. Even though paclitaxel (PTX) is known as one of the main anticancer drugs, it has several limitations, including low solubility in aqueous solutions, a limited dosage range, an insufficient release amount, and patient resistance. To overcome these limitations, we suggest the development of PTX-loaded thermosponge nanoparticles (PTX@TNP), which result in improved anticancer effects, via a simple nanoprecipitation method, which allows the preparation of PTX@TNPs with hydrophobic interactions without any chemical conjugation. Further, to improve the drug content and yield of the prepared complex, the co-organic solvent ratio was optimized. Thus, it was observed that the drug release rate increased as the drug capacity of PTX@TNPs increased. Furthermore, increasing PTX loading led to considerable anticancer activity against multidrug resistance (MDR)-related colorectal cancer cells (HCT 15), implying a synergistic anticancer effect. These results suggest that the solubilization of high drug amounts and the controlled release of poorly water-soluble PTX using TNPs could significantly improve its anticancer therapy, particularly in the treatment of MDR-p-glycoprotein-overexpressing cancers.https://www.mdpi.com/1999-4923/13/8/1150thermosponge nanoparticlepoorly water-soluble drugpaclitaxelhigh drug loading amountcontrolled releasecancer |
spellingShingle | Jin Sil Lee Hyeryeon Oh Daekyung Sung Jin Hyung Lee Won Il Choi High Solubilization and Controlled Release of Paclitaxel Using Thermosponge Nanoparticles for Effective Cancer Therapy Pharmaceutics thermosponge nanoparticle poorly water-soluble drug paclitaxel high drug loading amount controlled release cancer |
title | High Solubilization and Controlled Release of Paclitaxel Using Thermosponge Nanoparticles for Effective Cancer Therapy |
title_full | High Solubilization and Controlled Release of Paclitaxel Using Thermosponge Nanoparticles for Effective Cancer Therapy |
title_fullStr | High Solubilization and Controlled Release of Paclitaxel Using Thermosponge Nanoparticles for Effective Cancer Therapy |
title_full_unstemmed | High Solubilization and Controlled Release of Paclitaxel Using Thermosponge Nanoparticles for Effective Cancer Therapy |
title_short | High Solubilization and Controlled Release of Paclitaxel Using Thermosponge Nanoparticles for Effective Cancer Therapy |
title_sort | high solubilization and controlled release of paclitaxel using thermosponge nanoparticles for effective cancer therapy |
topic | thermosponge nanoparticle poorly water-soluble drug paclitaxel high drug loading amount controlled release cancer |
url | https://www.mdpi.com/1999-4923/13/8/1150 |
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