Bioavailability Enhancement of Paclitaxel via a Novel Oral Drug Delivery System: Paclitaxel-Loaded Glycyrrhizic Acid Micelles
Paclitaxel (PTX, taxol), a classical antitumor drug against a wide range of tumors, shows poor oral bioavailability. In order to improve the oral bioavailability of PTX, glycyrrhizic acid (GA) was used as the carrier in this study. This was the first report on the preparation, characterization and t...
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doaj-21301e6036d54100ae5d4225feffe5532020-11-25T00:14:02ZengMDPI AGMolecules1420-30492015-03-012034337435610.3390/molecules20034337molecules20034337Bioavailability Enhancement of Paclitaxel via a Novel Oral Drug Delivery System: Paclitaxel-Loaded Glycyrrhizic Acid MicellesFu-Heng Yang0Qing Zhang1Qian-Ying Liang2Sheng-Qi Wang3Bo-Xin Zhao4Ya-Tian Wang5Yun Cai6Guo-Feng Li7Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, ChinaDepartment of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, ChinaDepartment of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, ChinaDepartment of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, ChinaDepartment of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, ChinaDepartment of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, ChinaDepartment of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, ChinaDepartment of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, ChinaPaclitaxel (PTX, taxol), a classical antitumor drug against a wide range of tumors, shows poor oral bioavailability. In order to improve the oral bioavailability of PTX, glycyrrhizic acid (GA) was used as the carrier in this study. This was the first report on the preparation, characterization and the pharmacokinetic study in rats of PTX-loaded GA micelles The PTX-loaded micelles, prepared with ultrasonic dispersion method, displayed small particle sizes and spherical shapes. Differential scanning calorimeter (DSC) thermograms indicated that PTX was entrapped in the GA micelles and existed as an amorphous state. The encapsulation efficiency was about 90%, and the drug loading rate could reach up to 7.90%. PTX-loaded GA micelles displayed a delayed drug release compared to Taxol in the in vitro release experiment. In pharmacokinetic study via oral administration, the area under the plasma concentration-time curve (AUC0→24 h) of PTX-loaded GA micelles was about six times higher than that of Taxol (p < 0.05). The significant oral absorption enhancement of PTX from PTX-loaded GA micelles could be largely due to the increased absorption in jejunum and colon intestine. All these results suggested that GA would be a promising carrier for the oral delivery of PTX.http://www.mdpi.com/1420-3049/20/3/4337glycyrrhizic acidmicellesoral bioavailabilitypaclitaxel |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Fu-Heng Yang Qing Zhang Qian-Ying Liang Sheng-Qi Wang Bo-Xin Zhao Ya-Tian Wang Yun Cai Guo-Feng Li |
spellingShingle |
Fu-Heng Yang Qing Zhang Qian-Ying Liang Sheng-Qi Wang Bo-Xin Zhao Ya-Tian Wang Yun Cai Guo-Feng Li Bioavailability Enhancement of Paclitaxel via a Novel Oral Drug Delivery System: Paclitaxel-Loaded Glycyrrhizic Acid Micelles Molecules glycyrrhizic acid micelles oral bioavailability paclitaxel |
author_facet |
Fu-Heng Yang Qing Zhang Qian-Ying Liang Sheng-Qi Wang Bo-Xin Zhao Ya-Tian Wang Yun Cai Guo-Feng Li |
author_sort |
Fu-Heng Yang |
title |
Bioavailability Enhancement of Paclitaxel via a Novel Oral Drug Delivery System: Paclitaxel-Loaded Glycyrrhizic Acid Micelles |
title_short |
Bioavailability Enhancement of Paclitaxel via a Novel Oral Drug Delivery System: Paclitaxel-Loaded Glycyrrhizic Acid Micelles |
title_full |
Bioavailability Enhancement of Paclitaxel via a Novel Oral Drug Delivery System: Paclitaxel-Loaded Glycyrrhizic Acid Micelles |
title_fullStr |
Bioavailability Enhancement of Paclitaxel via a Novel Oral Drug Delivery System: Paclitaxel-Loaded Glycyrrhizic Acid Micelles |
title_full_unstemmed |
Bioavailability Enhancement of Paclitaxel via a Novel Oral Drug Delivery System: Paclitaxel-Loaded Glycyrrhizic Acid Micelles |
title_sort |
bioavailability enhancement of paclitaxel via a novel oral drug delivery system: paclitaxel-loaded glycyrrhizic acid micelles |
publisher |
MDPI AG |
series |
Molecules |
issn |
1420-3049 |
publishDate |
2015-03-01 |
description |
Paclitaxel (PTX, taxol), a classical antitumor drug against a wide range of tumors, shows poor oral bioavailability. In order to improve the oral bioavailability of PTX, glycyrrhizic acid (GA) was used as the carrier in this study. This was the first report on the preparation, characterization and the pharmacokinetic study in rats of PTX-loaded GA micelles The PTX-loaded micelles, prepared with ultrasonic dispersion method, displayed small particle sizes and spherical shapes. Differential scanning calorimeter (DSC) thermograms indicated that PTX was entrapped in the GA micelles and existed as an amorphous state. The encapsulation efficiency was about 90%, and the drug loading rate could reach up to 7.90%. PTX-loaded GA micelles displayed a delayed drug release compared to Taxol in the in vitro release experiment. In pharmacokinetic study via oral administration, the area under the plasma concentration-time curve (AUC0→24 h) of PTX-loaded GA micelles was about six times higher than that of Taxol (p < 0.05). The significant oral absorption enhancement of PTX from PTX-loaded GA micelles could be largely due to the increased absorption in jejunum and colon intestine. All these results suggested that GA would be a promising carrier for the oral delivery of PTX. |
topic |
glycyrrhizic acid micelles oral bioavailability paclitaxel |
url |
http://www.mdpi.com/1420-3049/20/3/4337 |
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