Preparation, characterization, and in vivo study of rhein-loaded poly(lactic-co-glycolic acid) nanoparticles for oral delivery
A novel rhein formulation based on poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) suitable for oral administration was developed in this study. The designed nanosystems were obtained by a modified spontaneous emulsification solvent diffusion method. The morphology of rhein-loaded PLGA NPs...
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| Format: | Online |
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Dove Medical Press
2015
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| Online Access: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4410823/ |
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pubmed-44108232015-05-08 Preparation, characterization, and in vivo study of rhein-loaded poly(lactic-co-glycolic acid) nanoparticles for oral delivery Yuan, Zheng Gu, Xinhua Original Research A novel rhein formulation based on poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) suitable for oral administration was developed in this study. The designed nanosystems were obtained by a modified spontaneous emulsification solvent diffusion method. The morphology of rhein-loaded PLGA NPs showed a spherical shape with a smooth surface, without any particle aggregation. Mean size of the NPs was 140.5±4.3 nm, and the zeta potential was −16.9±3.1 mV. The average drug loading was 3.9%±0.7%, and encapsulation efficiency was 84.5%±6.2%. Meanwhile, NPs are characterized by the slower release (only about 70% of rhein is released within 5 hours), and the model that fitted best for rhein released from the NPs was Higuchi kinetic model with correlation coefficient r=0.9993, revealing that rhein could be controlled released from the NPs. In vivo, NPs altered the distribution of rhein, and the half-life after oral administration was prolonged remarkably more than those of suspensions (22.6 hours vs 4.3 hours). The pharmacokinetic results indicated that the NPs had sustained-release efficacy. The area under the curve0–∞ of the NPs formulation was 3.07-fold higher than that of suspensions, suggesting that the encapsulated rhein had almost been absorbed in rats over the period of 12 hours. Although rhein-loaded PLGA NP formulations are hopefully used as a chemotherapeutic or adjuvant agent for human gastric cancer (SGC-7901), their in vivo antitumor effect and mechanisms at the molecular level still need further study. Dove Medical Press 2015-04-21 /pmc/articles/PMC4410823/ /pubmed/25960633 http://dx.doi.org/10.2147/DDDT.S81320 Text en © 2015 Yuan and Gu. This work is published by Dove Medical Press Limited, and licensed under Creative Commons Attribution – Non Commercial (unported, v3.0) License The full terms of the License are available at http://creativecommons.org/licenses/by-nc/3.0/. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. |
| repository_type |
Open Access Journal |
| institution_category |
Foreign Institution |
| institution |
US National Center for Biotechnology Information |
| building |
NCBI PubMed |
| collection |
Online Access |
| language |
English |
| format |
Online |
| author |
Yuan, Zheng Gu, Xinhua |
| spellingShingle |
Yuan, Zheng Gu, Xinhua Preparation, characterization, and in vivo study of rhein-loaded poly(lactic-co-glycolic acid) nanoparticles for oral delivery |
| author_facet |
Yuan, Zheng Gu, Xinhua |
| author_sort |
Yuan, Zheng |
| title |
Preparation, characterization, and in vivo study of rhein-loaded poly(lactic-co-glycolic acid) nanoparticles for oral delivery |
| title_short |
Preparation, characterization, and in vivo study of rhein-loaded poly(lactic-co-glycolic acid) nanoparticles for oral delivery |
| title_full |
Preparation, characterization, and in vivo study of rhein-loaded poly(lactic-co-glycolic acid) nanoparticles for oral delivery |
| title_fullStr |
Preparation, characterization, and in vivo study of rhein-loaded poly(lactic-co-glycolic acid) nanoparticles for oral delivery |
| title_full_unstemmed |
Preparation, characterization, and in vivo study of rhein-loaded poly(lactic-co-glycolic acid) nanoparticles for oral delivery |
| title_sort |
preparation, characterization, and in vivo study of rhein-loaded poly(lactic-co-glycolic acid) nanoparticles for oral delivery |
| description |
A novel rhein formulation based on poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) suitable for oral administration was developed in this study. The designed nanosystems were obtained by a modified spontaneous emulsification solvent diffusion method. The morphology of rhein-loaded PLGA NPs showed a spherical shape with a smooth surface, without any particle aggregation. Mean size of the NPs was 140.5±4.3 nm, and the zeta potential was −16.9±3.1 mV. The average drug loading was 3.9%±0.7%, and encapsulation efficiency was 84.5%±6.2%. Meanwhile, NPs are characterized by the slower release (only about 70% of rhein is released within 5 hours), and the model that fitted best for rhein released from the NPs was Higuchi kinetic model with correlation coefficient r=0.9993, revealing that rhein could be controlled released from the NPs. In vivo, NPs altered the distribution of rhein, and the half-life after oral administration was prolonged remarkably more than those of suspensions (22.6 hours vs 4.3 hours). The pharmacokinetic results indicated that the NPs had sustained-release efficacy. The area under the curve0–∞ of the NPs formulation was 3.07-fold higher than that of suspensions, suggesting that the encapsulated rhein had almost been absorbed in rats over the period of 12 hours. Although rhein-loaded PLGA NP formulations are hopefully used as a chemotherapeutic or adjuvant agent for human gastric cancer (SGC-7901), their in vivo antitumor effect and mechanisms at the molecular level still need further study. |
| publisher |
Dove Medical Press |
| publishDate |
2015 |
| url |
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4410823/ |
| _version_ |
1613216023142465536 |