Polymeric nanoparticles developed by vitamin E-modified aliphatic polycarbonate polymer to promote oral absorption of oleanolic acid
Oleanolic acid (OA) exhibited good pharmacological activities in the clinical treatment of hypoglycemia, immune regulation, acute jaundice and chronic toxic hepatitis. However, the oral delivery of OA is greatly limited by its inferior water solubility and poor intestinal mucosa permeability. Herein...
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| Format: | Article |
| Language: | English |
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Elsevier
2017-11-01
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| Series: | Asian Journal of Pharmaceutical Sciences |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1818087617304695 |
| _version_ | 1819112299158306816 |
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| author | Wenjuan Zhang Chufan Liang Hao Liu Zhenbao Li Rui Chen Mei Zhou Dan Li Qing Ye Cong Luo Jin Sun |
| author_facet | Wenjuan Zhang Chufan Liang Hao Liu Zhenbao Li Rui Chen Mei Zhou Dan Li Qing Ye Cong Luo Jin Sun |
| author_sort | Wenjuan Zhang |
| collection | DOAJ |
| description | Oleanolic acid (OA) exhibited good pharmacological activities in the clinical treatment of hypoglycemia, immune regulation, acute jaundice and chronic toxic hepatitis. However, the oral delivery of OA is greatly limited by its inferior water solubility and poor intestinal mucosa permeability. Herein, we developed a novel polymeric nanoparticle (NP) delivery system based on vitamin E modified aliphatic polycarbonate (mPEG-PCC-VE) to facilitate oral absorption of OA. OA encapsulated mPEG-PCC-VE NPs (OA/mPEG-PCC-VE NPs) showed uniform particle size of about 170 nm with high drug loading capability (8.9%). Furthermore, the polymeric mPEG-PCC-VE NPs, with good colloidal stability and pH-sensitive drug release characteristics, significantly enhanced the in vitro dissolution of OA in the alkaline medium. The in situ single pass intestinal perfusion (SPIP) studies performed on rats demonstrated that the OA/mPEG-PCC-VE NPs showed significantly improved permeability in the whole intestinal tract when compared to OA solution, especially for duodenum and colon. As a result, the in vivo pharmacokinetics study indicated that the bioavailability of OA/mPEG-PCC-VE NPs showed 1.5-fold higher than commercially available OA tablets. These results suggest that mPEG-PCC-VE NPs are a promising platform to facilitate the oral delivery of OA. |
| first_indexed | 2024-12-22T04:11:18Z |
| format | Article |
| id | doaj.art-12c9d26036564e95bb951bd9208ff3f5 |
| institution | Directory Open Access Journal |
| issn | 1818-0876 |
| language | English |
| last_indexed | 2024-12-22T04:11:18Z |
| publishDate | 2017-11-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Asian Journal of Pharmaceutical Sciences |
| spelling | doaj.art-12c9d26036564e95bb951bd9208ff3f52022-12-21T18:39:31ZengElsevierAsian Journal of Pharmaceutical Sciences1818-08762017-11-0112658659310.1016/j.ajps.2017.08.003Polymeric nanoparticles developed by vitamin E-modified aliphatic polycarbonate polymer to promote oral absorption of oleanolic acidWenjuan Zhang0Chufan Liang1Hao Liu2Zhenbao Li3Rui Chen4Mei Zhou5Dan Li6Qing Ye7Cong Luo8Jin Sun9School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, ChinaHAISCO (Shenyang) Pharmaceutical Co. Ltd., Shenyang, ChinaSchool of Pharmacy, BioMolecular Sciences Department, The University of Mississippi, Oxford, MS 38677, USASchool of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, ChinaSchool of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, ChinaSchool of Continuing Education, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, ChinaSchool of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, ChinaSchool of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, ChinaSchool of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, ChinaSchool of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang 110016, ChinaOleanolic acid (OA) exhibited good pharmacological activities in the clinical treatment of hypoglycemia, immune regulation, acute jaundice and chronic toxic hepatitis. However, the oral delivery of OA is greatly limited by its inferior water solubility and poor intestinal mucosa permeability. Herein, we developed a novel polymeric nanoparticle (NP) delivery system based on vitamin E modified aliphatic polycarbonate (mPEG-PCC-VE) to facilitate oral absorption of OA. OA encapsulated mPEG-PCC-VE NPs (OA/mPEG-PCC-VE NPs) showed uniform particle size of about 170 nm with high drug loading capability (8.9%). Furthermore, the polymeric mPEG-PCC-VE NPs, with good colloidal stability and pH-sensitive drug release characteristics, significantly enhanced the in vitro dissolution of OA in the alkaline medium. The in situ single pass intestinal perfusion (SPIP) studies performed on rats demonstrated that the OA/mPEG-PCC-VE NPs showed significantly improved permeability in the whole intestinal tract when compared to OA solution, especially for duodenum and colon. As a result, the in vivo pharmacokinetics study indicated that the bioavailability of OA/mPEG-PCC-VE NPs showed 1.5-fold higher than commercially available OA tablets. These results suggest that mPEG-PCC-VE NPs are a promising platform to facilitate the oral delivery of OA.http://www.sciencedirect.com/science/article/pii/S1818087617304695Oleanolic acidPolymeric nanoparticlesmPEG-PCC-VEOral delivery |
| spellingShingle | Wenjuan Zhang Chufan Liang Hao Liu Zhenbao Li Rui Chen Mei Zhou Dan Li Qing Ye Cong Luo Jin Sun Polymeric nanoparticles developed by vitamin E-modified aliphatic polycarbonate polymer to promote oral absorption of oleanolic acid Asian Journal of Pharmaceutical Sciences Oleanolic acid Polymeric nanoparticles mPEG-PCC-VE Oral delivery |
| title | Polymeric nanoparticles developed by vitamin E-modified aliphatic polycarbonate polymer to promote oral absorption of oleanolic acid |
| title_full | Polymeric nanoparticles developed by vitamin E-modified aliphatic polycarbonate polymer to promote oral absorption of oleanolic acid |
| title_fullStr | Polymeric nanoparticles developed by vitamin E-modified aliphatic polycarbonate polymer to promote oral absorption of oleanolic acid |
| title_full_unstemmed | Polymeric nanoparticles developed by vitamin E-modified aliphatic polycarbonate polymer to promote oral absorption of oleanolic acid |
| title_short | Polymeric nanoparticles developed by vitamin E-modified aliphatic polycarbonate polymer to promote oral absorption of oleanolic acid |
| title_sort | polymeric nanoparticles developed by vitamin e modified aliphatic polycarbonate polymer to promote oral absorption of oleanolic acid |
| topic | Oleanolic acid Polymeric nanoparticles mPEG-PCC-VE Oral delivery |
| url | http://www.sciencedirect.com/science/article/pii/S1818087617304695 |
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