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...

Full description

Bibliographic Details
Main Authors: Jin Sil Lee, Hyeryeon Oh, Daekyung Sung, Jin Hyung Lee, Won Il Choi
Format: Article
Language:English
Published: MDPI AG 2021-07-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/13/8/1150
_version_ 1797522416873766912
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.
first_indexed 2024-03-10T08:29:04Z
format Article
id doaj.art-338105f3c11e48368f725552fdcd2599
institution Directory Open Access Journal
issn 1999-4923
language English
last_indexed 2024-03-10T08:29:04Z
publishDate 2021-07-01
publisher MDPI AG
record_format Article
series Pharmaceutics
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
work_keys_str_mv AT jinsillee highsolubilizationandcontrolledreleaseofpaclitaxelusingthermospongenanoparticlesforeffectivecancertherapy
AT hyeryeonoh highsolubilizationandcontrolledreleaseofpaclitaxelusingthermospongenanoparticlesforeffectivecancertherapy
AT daekyungsung highsolubilizationandcontrolledreleaseofpaclitaxelusingthermospongenanoparticlesforeffectivecancertherapy
AT jinhyunglee highsolubilizationandcontrolledreleaseofpaclitaxelusingthermospongenanoparticlesforeffectivecancertherapy
AT wonilchoi highsolubilizationandcontrolledreleaseofpaclitaxelusingthermospongenanoparticlesforeffectivecancertherapy