Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effect
Abstract Background Carvedilol, the anti-hypertensive drug, has poor bioavailability when administered orally. Ethosomes-mediated transdermal delivery is considered a potential route of administration to increase the bioavailability of carvedilol. The central composite design could be used as a tool...
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| Format: | Article |
| Language: | English |
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BMC
2021-04-01
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| Series: | Journal of Nanobiotechnology |
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| Online Access: | https://doi.org/10.1186/s12951-021-00833-4 |
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| author | Padmanabha Rao Amarachinta Garima Sharma Noufel Samed Ananda Kumar Chettupalli Madhusudhan Alle Jin-Chul Kim |
| author_facet | Padmanabha Rao Amarachinta Garima Sharma Noufel Samed Ananda Kumar Chettupalli Madhusudhan Alle Jin-Chul Kim |
| author_sort | Padmanabha Rao Amarachinta |
| collection | DOAJ |
| description | Abstract Background Carvedilol, the anti-hypertensive drug, has poor bioavailability when administered orally. Ethosomes-mediated transdermal delivery is considered a potential route of administration to increase the bioavailability of carvedilol. The central composite design could be used as a tool to optimize ethosomal formulation. Thus, this study aims to optimize carvedilol-loaded ethosomes using central composite design, followed by incorporation of synthesized ethosomes into hydrogels for transdermal delivery of carvedilol. Results The optimized carvedilol-loaded ethosomes were spherical in shape. The optimized ethosomes had mean particle size of 130 ± 1.72 nm, entrapment efficiency of 99.12 ± 2.96%, cumulative drug release of 97.89 ± 3.7%, zeta potential of − 31 ± 1.8 mV, and polydispersity index of 0.230 ± 0.03. The in-vitro drug release showed sustained release of carvedilol from ethosomes and ethosomal hydrogel. Compared to free carvedilol-loaded hydrogel, the ethosomal gel showed increased penetration of carvedilol through the skin. Moreover, ethosomal hydrogels showed a gradual reduction in blood pressure for 24 h in rats. Conclusions Taken together, central composite design can be used for successful optimization of carvedilol-loaded ethosomes formulation, which can serve as the promising transdermal delivery system for carvedilol. Moreover the carvedilol-loaded ethosomal gel can extend the anti-hypertensive effect of carvedilol for a longer time, as compared to free carvedilol, suggesting its therapeutic potential in future clinics. |
| first_indexed | 2024-04-11T09:38:01Z |
| format | Article |
| id | doaj.art-bf9d238ef0994cef95339e837837f563 |
| institution | Directory Open Access Journal |
| issn | 1477-3155 |
| language | English |
| last_indexed | 2024-04-11T09:38:01Z |
| publishDate | 2021-04-01 |
| publisher | BMC |
| record_format | Article |
| series | Journal of Nanobiotechnology |
| spelling | doaj.art-bf9d238ef0994cef95339e837837f5632022-12-22T04:31:28ZengBMCJournal of Nanobiotechnology1477-31552021-04-0119111510.1186/s12951-021-00833-4Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effectPadmanabha Rao Amarachinta0Garima Sharma1Noufel Samed2Ananda Kumar Chettupalli3Madhusudhan Alle4Jin-Chul Kim5School of Pharmacy, Anurag UniversityDepartment of Biomedical Science & Institute of Bioscience and Biotechnology, Kangwon National UniversityDepartment of Biomedical Science & Institute of Bioscience and Biotechnology, Kangwon National UniversitySchool of Pharmacy, Anurag UniversityDepartment of Biomedical Science & Institute of Bioscience and Biotechnology, Kangwon National UniversityDepartment of Biomedical Science & Institute of Bioscience and Biotechnology, Kangwon National UniversityAbstract Background Carvedilol, the anti-hypertensive drug, has poor bioavailability when administered orally. Ethosomes-mediated transdermal delivery is considered a potential route of administration to increase the bioavailability of carvedilol. The central composite design could be used as a tool to optimize ethosomal formulation. Thus, this study aims to optimize carvedilol-loaded ethosomes using central composite design, followed by incorporation of synthesized ethosomes into hydrogels for transdermal delivery of carvedilol. Results The optimized carvedilol-loaded ethosomes were spherical in shape. The optimized ethosomes had mean particle size of 130 ± 1.72 nm, entrapment efficiency of 99.12 ± 2.96%, cumulative drug release of 97.89 ± 3.7%, zeta potential of − 31 ± 1.8 mV, and polydispersity index of 0.230 ± 0.03. The in-vitro drug release showed sustained release of carvedilol from ethosomes and ethosomal hydrogel. Compared to free carvedilol-loaded hydrogel, the ethosomal gel showed increased penetration of carvedilol through the skin. Moreover, ethosomal hydrogels showed a gradual reduction in blood pressure for 24 h in rats. Conclusions Taken together, central composite design can be used for successful optimization of carvedilol-loaded ethosomes formulation, which can serve as the promising transdermal delivery system for carvedilol. Moreover the carvedilol-loaded ethosomal gel can extend the anti-hypertensive effect of carvedilol for a longer time, as compared to free carvedilol, suggesting its therapeutic potential in future clinics.https://doi.org/10.1186/s12951-021-00833-4EthosomesCarvedilolCentral composite design (CCD)Ethosomal gelAnti-hypertension |
| spellingShingle | Padmanabha Rao Amarachinta Garima Sharma Noufel Samed Ananda Kumar Chettupalli Madhusudhan Alle Jin-Chul Kim Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effect Journal of Nanobiotechnology Ethosomes Carvedilol Central composite design (CCD) Ethosomal gel Anti-hypertension |
| title | Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effect |
| title_full | Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effect |
| title_fullStr | Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effect |
| title_full_unstemmed | Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effect |
| title_short | Central composite design for the development of carvedilol-loaded transdermal ethosomal hydrogel for extended and enhanced anti-hypertensive effect |
| title_sort | central composite design for the development of carvedilol loaded transdermal ethosomal hydrogel for extended and enhanced anti hypertensive effect |
| topic | Ethosomes Carvedilol Central composite design (CCD) Ethosomal gel Anti-hypertension |
| url | https://doi.org/10.1186/s12951-021-00833-4 |
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