Antibiotic-based small molecular micelles combined with photodynamic therapy for bacterial infections
The appearance of multidrug-resistant bacteria and the formation of bacterial biofilms have necessitated the development of alternative antimicrobial therapeutics. Antibiotics conjugated with or embedded in nano-drug carriers show a great potential and advantage over free drugs, but the mass proport...
| Main Authors: | , , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2023-05-01
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| Series: | Asian Journal of Pharmaceutical Sciences |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1818087623000375 |
| _version_ | 1797794000381411328 |
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| author | Lijiao Yang Shaomin Song Meihui Yin Min Yang Daoping Yan Xiaohui Wan Jipeng Xiao Yuchen Jiang Yongchao Yao Jianbin Luo |
| author_facet | Lijiao Yang Shaomin Song Meihui Yin Min Yang Daoping Yan Xiaohui Wan Jipeng Xiao Yuchen Jiang Yongchao Yao Jianbin Luo |
| author_sort | Lijiao Yang |
| collection | DOAJ |
| description | The appearance of multidrug-resistant bacteria and the formation of bacterial biofilms have necessitated the development of alternative antimicrobial therapeutics. Antibiotics conjugated with or embedded in nano-drug carriers show a great potential and advantage over free drugs, but the mass proportion of carriers generally exceeds 90% of the nano-drug, resulting in low drug loading and limited therapeutic output. Herein, we fabricated a nanocarrier using antibiotics as the building blocks, minimizing the use of carrier materials, significantly increasing the drug loading content and treatment effect. Firstly, we conjugated betaine carboxylate with ciprofloxacin (CIP) through an ester bond to form the amphiphilic conjugate (CIP-CB), which self-assembled into micelles (CIP-CBMs) in aqueous solutions, with a CIP loading content as high as 65.4% and pH-induced surface charge reversal properties. Secondly, a model photosensitizer (5, 10, 15, 20-tetraphenylporphyrin (TPP)) was encapsulated in CIP-CBMs, generating infection-targeted photodynamic/antibiotic combined nanomedicines (denoted as TPP@CIP-CBMs). Upon accumulation at infection sites or in deep bacterial biofilms, the ester bond between the betaine carboxylate and CIP is cleaved to release free TPP and CIP, leading to a synergetic antibacterial and antibiofilm activity in vitro and in vivo. |
| first_indexed | 2024-03-13T02:56:25Z |
| format | Article |
| id | doaj.art-58c7e685b5c245ceb5287a54c8bcc9f0 |
| institution | Directory Open Access Journal |
| issn | 1818-0876 |
| language | English |
| last_indexed | 2024-03-13T02:56:25Z |
| publishDate | 2023-05-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Asian Journal of Pharmaceutical Sciences |
| spelling | doaj.art-58c7e685b5c245ceb5287a54c8bcc9f02023-06-28T04:29:20ZengElsevierAsian Journal of Pharmaceutical Sciences1818-08762023-05-01183100810Antibiotic-based small molecular micelles combined with photodynamic therapy for bacterial infectionsLijiao Yang0Shaomin Song1Meihui Yin2Min Yang3Daoping Yan4Xiaohui Wan5Jipeng Xiao6Yuchen Jiang7Yongchao Yao8Jianbin Luo9College of Chemistry and Environment, Southwest Minzu University, Chengdu 610041, ChinaCollege of Chemistry and Environment, Southwest Minzu University, Chengdu 610041, ChinaCollege of Chemistry and Environment, Southwest Minzu University, Chengdu 610041, ChinaCollege of Chemistry and Environment, Southwest Minzu University, Chengdu 610041, ChinaCollege of Chemistry and Environment, Southwest Minzu University, Chengdu 610041, ChinaCollege of Chemistry and Environment, Southwest Minzu University, Chengdu 610041, ChinaCollege of Chemistry and Environment, Southwest Minzu University, Chengdu 610041, ChinaCorresponding authors.; College of Chemistry and Environment, Southwest Minzu University, Chengdu 610041, ChinaCorresponding authors.; College of Chemistry and Environment, Southwest Minzu University, Chengdu 610041, ChinaCorresponding authors.; College of Chemistry and Environment, Southwest Minzu University, Chengdu 610041, ChinaThe appearance of multidrug-resistant bacteria and the formation of bacterial biofilms have necessitated the development of alternative antimicrobial therapeutics. Antibiotics conjugated with or embedded in nano-drug carriers show a great potential and advantage over free drugs, but the mass proportion of carriers generally exceeds 90% of the nano-drug, resulting in low drug loading and limited therapeutic output. Herein, we fabricated a nanocarrier using antibiotics as the building blocks, minimizing the use of carrier materials, significantly increasing the drug loading content and treatment effect. Firstly, we conjugated betaine carboxylate with ciprofloxacin (CIP) through an ester bond to form the amphiphilic conjugate (CIP-CB), which self-assembled into micelles (CIP-CBMs) in aqueous solutions, with a CIP loading content as high as 65.4% and pH-induced surface charge reversal properties. Secondly, a model photosensitizer (5, 10, 15, 20-tetraphenylporphyrin (TPP)) was encapsulated in CIP-CBMs, generating infection-targeted photodynamic/antibiotic combined nanomedicines (denoted as TPP@CIP-CBMs). Upon accumulation at infection sites or in deep bacterial biofilms, the ester bond between the betaine carboxylate and CIP is cleaved to release free TPP and CIP, leading to a synergetic antibacterial and antibiofilm activity in vitro and in vivo.http://www.sciencedirect.com/science/article/pii/S1818087623000375Antibiotics based micellesChemo-photodynamic therapyAntibiofilmpH responsiveMultidrug-resistant |
| spellingShingle | Lijiao Yang Shaomin Song Meihui Yin Min Yang Daoping Yan Xiaohui Wan Jipeng Xiao Yuchen Jiang Yongchao Yao Jianbin Luo Antibiotic-based small molecular micelles combined with photodynamic therapy for bacterial infections Asian Journal of Pharmaceutical Sciences Antibiotics based micelles Chemo-photodynamic therapy Antibiofilm pH responsive Multidrug-resistant |
| title | Antibiotic-based small molecular micelles combined with photodynamic therapy for bacterial infections |
| title_full | Antibiotic-based small molecular micelles combined with photodynamic therapy for bacterial infections |
| title_fullStr | Antibiotic-based small molecular micelles combined with photodynamic therapy for bacterial infections |
| title_full_unstemmed | Antibiotic-based small molecular micelles combined with photodynamic therapy for bacterial infections |
| title_short | Antibiotic-based small molecular micelles combined with photodynamic therapy for bacterial infections |
| title_sort | antibiotic based small molecular micelles combined with photodynamic therapy for bacterial infections |
| topic | Antibiotics based micelles Chemo-photodynamic therapy Antibiofilm pH responsive Multidrug-resistant |
| url | http://www.sciencedirect.com/science/article/pii/S1818087623000375 |
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