Polymeric Microspheres Designed to Carry Crystalline Drugs at Their Surface or Inside Cavities and Dimples
Injectable polymer microparticles with the ability to carry and release pharmacologically active agents are attracting more and more interest. This study is focused on the chemical synthesis, characterization, and preliminary exploration of the utility of a new type of injectable drug-releasing poly...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-08-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/15/8/2146 |
| _version_ | 1797583513257508864 |
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| author | Meitong Shen Ling Zheng Leo H. Koole |
| author_facet | Meitong Shen Ling Zheng Leo H. Koole |
| author_sort | Meitong Shen |
| collection | DOAJ |
| description | Injectable polymer microparticles with the ability to carry and release pharmacologically active agents are attracting more and more interest. This study is focused on the chemical synthesis, characterization, and preliminary exploration of the utility of a new type of injectable drug-releasing polymer microparticle. The particles feature a new combination of structural and physico-chemical properties: (i) their geometry deviates from the spherical in the sense that the particles have a cavity; (ii) the particles are porous and can therefore be loaded with crystalline drug formulations; drug crystals can reside at both the particle’s surfaces and inside cavities; (iii) the particles are relatively dense since the polymer network contains covalently bound iodine (approximately 10% by mass); this renders the drug-loaded particles traceable (localizable) by X-ray fluoroscopy. This study presents several examples. First, the particles were loaded with crystalline voriconazole, which is a potent antifungal drug used in ophthalmology to treat fungal keratitis (infection/inflammation of the cornea caused by penetrating fungus). Drug loading as high as 10% by mass (=mass of immobilized drug/(mass of the microparticle + mass of immobilized drug) × 100%) could be achieved. Slow local release of voriconazole from these particles was observed in vitro. These findings hold promise regarding new approaches to treat fungal keratitis. Moreover, this study can help to expand the scope of the transarterial chemoembolization (TACE) technique since it enables the use of higher drug loadings (thus enabling higher local drug concentration or extended therapy duration), as well as application of hydrophobic drugs that cannot be used in combination with existing TACE embolic particles. |
| first_indexed | 2024-03-10T23:39:59Z |
| format | Article |
| id | doaj.art-d621a26d32dd4e9abf6be9a97aac1b0a |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T23:39:59Z |
| publishDate | 2023-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-d621a26d32dd4e9abf6be9a97aac1b0a2023-11-19T02:37:34ZengMDPI AGPharmaceutics1999-49232023-08-01158214610.3390/pharmaceutics15082146Polymeric Microspheres Designed to Carry Crystalline Drugs at Their Surface or Inside Cavities and DimplesMeitong Shen0Ling Zheng1Leo H. Koole2Innovative Bioengineering Laboratory for Ocular Drug Delivery, School of Ophthalmology and Optometry, Eye Hospital of Wenzhou Medical University, Wenzhou Medical University, 270 Xueyuan West Road, Wenzhou 325027, ChinaInnovative Bioengineering Laboratory for Ocular Drug Delivery, School of Ophthalmology and Optometry, Eye Hospital of Wenzhou Medical University, Wenzhou Medical University, 270 Xueyuan West Road, Wenzhou 325027, ChinaInnovative Bioengineering Laboratory for Ocular Drug Delivery, School of Ophthalmology and Optometry, Eye Hospital of Wenzhou Medical University, Wenzhou Medical University, 270 Xueyuan West Road, Wenzhou 325027, ChinaInjectable polymer microparticles with the ability to carry and release pharmacologically active agents are attracting more and more interest. This study is focused on the chemical synthesis, characterization, and preliminary exploration of the utility of a new type of injectable drug-releasing polymer microparticle. The particles feature a new combination of structural and physico-chemical properties: (i) their geometry deviates from the spherical in the sense that the particles have a cavity; (ii) the particles are porous and can therefore be loaded with crystalline drug formulations; drug crystals can reside at both the particle’s surfaces and inside cavities; (iii) the particles are relatively dense since the polymer network contains covalently bound iodine (approximately 10% by mass); this renders the drug-loaded particles traceable (localizable) by X-ray fluoroscopy. This study presents several examples. First, the particles were loaded with crystalline voriconazole, which is a potent antifungal drug used in ophthalmology to treat fungal keratitis (infection/inflammation of the cornea caused by penetrating fungus). Drug loading as high as 10% by mass (=mass of immobilized drug/(mass of the microparticle + mass of immobilized drug) × 100%) could be achieved. Slow local release of voriconazole from these particles was observed in vitro. These findings hold promise regarding new approaches to treat fungal keratitis. Moreover, this study can help to expand the scope of the transarterial chemoembolization (TACE) technique since it enables the use of higher drug loadings (thus enabling higher local drug concentration or extended therapy duration), as well as application of hydrophobic drugs that cannot be used in combination with existing TACE embolic particles.https://www.mdpi.com/1999-4923/15/8/2146drug deliverymicrospherescavitysuspension polymerizationminimally invasive therapykeratitis |
| spellingShingle | Meitong Shen Ling Zheng Leo H. Koole Polymeric Microspheres Designed to Carry Crystalline Drugs at Their Surface or Inside Cavities and Dimples Pharmaceutics drug delivery microspheres cavity suspension polymerization minimally invasive therapy keratitis |
| title | Polymeric Microspheres Designed to Carry Crystalline Drugs at Their Surface or Inside Cavities and Dimples |
| title_full | Polymeric Microspheres Designed to Carry Crystalline Drugs at Their Surface or Inside Cavities and Dimples |
| title_fullStr | Polymeric Microspheres Designed to Carry Crystalline Drugs at Their Surface or Inside Cavities and Dimples |
| title_full_unstemmed | Polymeric Microspheres Designed to Carry Crystalline Drugs at Their Surface or Inside Cavities and Dimples |
| title_short | Polymeric Microspheres Designed to Carry Crystalline Drugs at Their Surface or Inside Cavities and Dimples |
| title_sort | polymeric microspheres designed to carry crystalline drugs at their surface or inside cavities and dimples |
| topic | drug delivery microspheres cavity suspension polymerization minimally invasive therapy keratitis |
| url | https://www.mdpi.com/1999-4923/15/8/2146 |
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