Exenatide-loaded inside-porous poly(lactic-co-glycolic acid) microspheres as a long-acting drug delivery system with improved release characteristics
The glucagon-like peptide-1 receptor agonist exenatide (EXT) is an effective treatment for type 2 diabetes. However, this peptide has a short biological half-life and the delayed release characteristic of current formulations limit its clinical application. Herein, we prepared EXT-loaded inside-poro...
| Main Authors: | , , , , , |
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| Format: | Article |
| Language: | English |
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Taylor & Francis Group
2020-01-01
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| Series: | Drug Delivery |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/10717544.2020.1850919 |
| _version_ | 1831554131673743360 |
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| author | Junqiu Zhai Zhanlun Ou Liuting Zhong Yu-e Wang Li-Ping Cao Shixia Guan |
| author_facet | Junqiu Zhai Zhanlun Ou Liuting Zhong Yu-e Wang Li-Ping Cao Shixia Guan |
| author_sort | Junqiu Zhai |
| collection | DOAJ |
| description | The glucagon-like peptide-1 receptor agonist exenatide (EXT) is an effective treatment for type 2 diabetes. However, this peptide has a short biological half-life and the delayed release characteristic of current formulations limit its clinical application. Herein, we prepared EXT-loaded inside-porous poly(d,l-lactic-co-glycolic acid (PLGA) microspheres with outside layers (EXT-PMS) using a W1/O/W2 emulsion method with a microfluidic technique and its fabrication and formulation conditions were systematically investigated. In vitro dissolution experiments showed that the PLGA concentration, proportion of drug and oil phase, and the number and size of pores strongly affected the release behaviors of EXT-PMS. In vitro, the optimized EXT-PMS with large internal pores exhibited rapid and stable release without a lag phase. In a rat model, subcutaneous administration of the product yielded plasma concentrations of EXT that was sustained for 30 days with low burst and no delayed-release effect. The preparation of inside-porous microspheres is lighting up the development of long-acting drug delivery systems for other drugs with favorable release characteristics. |
| first_indexed | 2024-12-17T03:57:51Z |
| format | Article |
| id | doaj.art-7d56e50cc7224b51946679eddd00a3b7 |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-12-17T03:57:51Z |
| publishDate | 2020-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-7d56e50cc7224b51946679eddd00a3b72022-12-21T22:04:35ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642020-01-012711667167510.1080/10717544.2020.18509191850919Exenatide-loaded inside-porous poly(lactic-co-glycolic acid) microspheres as a long-acting drug delivery system with improved release characteristicsJunqiu Zhai0Zhanlun Ou1Liuting Zhong2Yu-e Wang3Li-Ping Cao4Shixia Guan5School of Pharmaceutical Sciences, Guangzhou University of Chinese MedicineSchool of Pharmaceutical Sciences, Guangzhou University of Chinese MedicineSchool of Pharmaceutical Sciences, Guangzhou University of Chinese MedicineSchool of Pharmaceutical Sciences, Guangzhou University of Chinese MedicineShenzhen Bao’an Traditional Chinese Medicine Hospital GroupSchool of Pharmaceutical Sciences, Guangzhou University of Chinese MedicineThe glucagon-like peptide-1 receptor agonist exenatide (EXT) is an effective treatment for type 2 diabetes. However, this peptide has a short biological half-life and the delayed release characteristic of current formulations limit its clinical application. Herein, we prepared EXT-loaded inside-porous poly(d,l-lactic-co-glycolic acid (PLGA) microspheres with outside layers (EXT-PMS) using a W1/O/W2 emulsion method with a microfluidic technique and its fabrication and formulation conditions were systematically investigated. In vitro dissolution experiments showed that the PLGA concentration, proportion of drug and oil phase, and the number and size of pores strongly affected the release behaviors of EXT-PMS. In vitro, the optimized EXT-PMS with large internal pores exhibited rapid and stable release without a lag phase. In a rat model, subcutaneous administration of the product yielded plasma concentrations of EXT that was sustained for 30 days with low burst and no delayed-release effect. The preparation of inside-porous microspheres is lighting up the development of long-acting drug delivery systems for other drugs with favorable release characteristics.http://dx.doi.org/10.1080/10717544.2020.1850919exenatideinside-porous microsphereslong-actingrelease behaviortype 2 diabetes |
| spellingShingle | Junqiu Zhai Zhanlun Ou Liuting Zhong Yu-e Wang Li-Ping Cao Shixia Guan Exenatide-loaded inside-porous poly(lactic-co-glycolic acid) microspheres as a long-acting drug delivery system with improved release characteristics Drug Delivery exenatide inside-porous microspheres long-acting release behavior type 2 diabetes |
| title | Exenatide-loaded inside-porous poly(lactic-co-glycolic acid) microspheres as a long-acting drug delivery system with improved release characteristics |
| title_full | Exenatide-loaded inside-porous poly(lactic-co-glycolic acid) microspheres as a long-acting drug delivery system with improved release characteristics |
| title_fullStr | Exenatide-loaded inside-porous poly(lactic-co-glycolic acid) microspheres as a long-acting drug delivery system with improved release characteristics |
| title_full_unstemmed | Exenatide-loaded inside-porous poly(lactic-co-glycolic acid) microspheres as a long-acting drug delivery system with improved release characteristics |
| title_short | Exenatide-loaded inside-porous poly(lactic-co-glycolic acid) microspheres as a long-acting drug delivery system with improved release characteristics |
| title_sort | exenatide loaded inside porous poly lactic co glycolic acid microspheres as a long acting drug delivery system with improved release characteristics |
| topic | exenatide inside-porous microspheres long-acting release behavior type 2 diabetes |
| url | http://dx.doi.org/10.1080/10717544.2020.1850919 |
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