Wettability and contact angle affect precorneal retention and pharmacodynamic behavior of microspheres
In the present study, we describe the development of betaxolol hydrochloride and montmorillonite with ion exchange in a single formulation to create a novel micro-interactive dual-functioning sustained-release delivery system (MIDFDS) for the treatment of glaucoma. Betaxolol hydrochloride molecule w...
| Main Authors: | , , , , , , , , , , , , , , |
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| Format: | Article |
| Language: | English |
| Published: |
Taylor & Francis Group
2021-01-01
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| Series: | Drug Delivery |
| Subjects: | |
| Online Access: | http://dx.doi.org/10.1080/10717544.2021.1981493 |
| _version_ | 1818334079540527104 |
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| author | Hanyu Liu Xinyue Han Huamei Li Qi Tao Jie Hu Shuo Liu Huaixin Liu Jun Zhou Wei Li Fan Yang Qineng Ping Shijie Wei Hongmei Liu Huaqing Lin Dongzhi Hou |
| author_facet | Hanyu Liu Xinyue Han Huamei Li Qi Tao Jie Hu Shuo Liu Huaixin Liu Jun Zhou Wei Li Fan Yang Qineng Ping Shijie Wei Hongmei Liu Huaqing Lin Dongzhi Hou |
| author_sort | Hanyu Liu |
| collection | DOAJ |
| description | In the present study, we describe the development of betaxolol hydrochloride and montmorillonite with ion exchange in a single formulation to create a novel micro-interactive dual-functioning sustained-release delivery system (MIDFDS) for the treatment of glaucoma. Betaxolol hydrochloride molecule was loaded onto the montmorillonite by ion exchange and MIDFDS formation was confirmed by XPS data. MIDFDS showed similar physicochemical properties to those of Betoptic, such as particle size, pH, osmotic pressure, and rheological properties. Nevertheless, the microdialysis and intraocular pressure test revealed better in vivo performance of MIDFDS, such as pharmacokinetics and pharmacodynamics. With regards to wettability, MIDFDS had a larger contact angle (54.66 ± 5.35°) than Betoptic (36.68 ± 1.77°), enabling the MIDFDS (2.93 s) to spread slower on the cornea than Betoptic (2.50 s). Moderate spreading behavior and oppositely charged electrostatic micro-interactions had a comprehensive influence on micro-interactions with the tear film residue, resulting in a longer precorneal retention time. Furthermore, MIDFDS had a significant sustained-release effect, with complete release near the cornea. The dual-functioning sustained-release carrier together with prolonged pre-corneal retention time (80 min) provided sufficiently high drug concentrations in the aqueous humor to achieve a more stable and long-term IOP reduction for 10 h. In addition, cytotoxicity and hemolysis tests showed that MIDFDS had better biocompatibility than Betoptic. The dual-functioning microspheres presented in this study provide the possibility for improved compliance due to low cytotoxicity and hemolysis, which suggests promising clinical implications. |
| first_indexed | 2024-12-13T14:01:50Z |
| format | Article |
| id | doaj.art-af7c0daefaa44bde99ee01821fc319a6 |
| institution | Directory Open Access Journal |
| issn | 1071-7544 1521-0464 |
| language | English |
| last_indexed | 2024-12-13T14:01:50Z |
| publishDate | 2021-01-01 |
| publisher | Taylor & Francis Group |
| record_format | Article |
| series | Drug Delivery |
| spelling | doaj.art-af7c0daefaa44bde99ee01821fc319a62022-12-21T23:42:42ZengTaylor & Francis GroupDrug Delivery1071-75441521-04642021-01-012812011202310.1080/10717544.2021.19814931981493Wettability and contact angle affect precorneal retention and pharmacodynamic behavior of microspheresHanyu Liu0Xinyue Han1Huamei Li2Qi Tao3Jie Hu4Shuo Liu5Huaixin Liu6Jun Zhou7Wei Li8Fan Yang9Qineng Ping10Shijie Wei11Hongmei Liu12Huaqing Lin13Dongzhi Hou14Guangdong Engineering and Technology Research Center of Topical Precise Drug Delivery System, College of Pharmacy, Guangdong Pharmaceutical UniversityGuangdong Engineering and Technology Research Center of Topical Precise Drug Delivery System, College of Pharmacy, Guangdong Pharmaceutical UniversityGuangdong Engineering and Technology Research Center of Topical Precise Drug Delivery System, College of Pharmacy, Guangdong Pharmaceutical UniversityCAS Key Laboratory of Mineralogy and Metallogeny & Guangdong Provincial Key Laboratory of Mineral Physics and Materials, Guangzhou Institute of Geochemistry, Chinese Academy of Sciences (CAS)Guangdong Engineering and Technology Research Center of Topical Precise Drug Delivery System, College of Pharmacy, Guangdong Pharmaceutical UniversityGuangdong Engineering and Technology Research Center of Topical Precise Drug Delivery System, College of Pharmacy, Guangdong Pharmaceutical UniversityGuangdong Engineering and Technology Research Center of Topical Precise Drug Delivery System, College of Pharmacy, Guangdong Pharmaceutical UniversityDepartment of English Language and Literature, University College LondonGuangzhou Institute For Drug ControlGuangdong Engineering and Technology Research Center of Topical Precise Drug Delivery System, College of Pharmacy, Guangdong Pharmaceutical UniversityCollege of Pharmacy, China Pharmaceutical UniversityGuangdong Engineering and Technology Research Center of Topical Precise Drug Delivery System, College of Pharmacy, Guangdong Pharmaceutical UniversityCAS Key Laboratory of Mineralogy and Metallogeny & Guangdong Provincial Key Laboratory of Mineral Physics and Materials, Guangzhou Institute of Geochemistry, Chinese Academy of Sciences (CAS)Guangdong Engineering and Technology Research Center of Topical Precise Drug Delivery System, College of Pharmacy, Guangdong Pharmaceutical UniversityGuangdong Engineering and Technology Research Center of Topical Precise Drug Delivery System, College of Pharmacy, Guangdong Pharmaceutical UniversityIn the present study, we describe the development of betaxolol hydrochloride and montmorillonite with ion exchange in a single formulation to create a novel micro-interactive dual-functioning sustained-release delivery system (MIDFDS) for the treatment of glaucoma. Betaxolol hydrochloride molecule was loaded onto the montmorillonite by ion exchange and MIDFDS formation was confirmed by XPS data. MIDFDS showed similar physicochemical properties to those of Betoptic, such as particle size, pH, osmotic pressure, and rheological properties. Nevertheless, the microdialysis and intraocular pressure test revealed better in vivo performance of MIDFDS, such as pharmacokinetics and pharmacodynamics. With regards to wettability, MIDFDS had a larger contact angle (54.66 ± 5.35°) than Betoptic (36.68 ± 1.77°), enabling the MIDFDS (2.93 s) to spread slower on the cornea than Betoptic (2.50 s). Moderate spreading behavior and oppositely charged electrostatic micro-interactions had a comprehensive influence on micro-interactions with the tear film residue, resulting in a longer precorneal retention time. Furthermore, MIDFDS had a significant sustained-release effect, with complete release near the cornea. The dual-functioning sustained-release carrier together with prolonged pre-corneal retention time (80 min) provided sufficiently high drug concentrations in the aqueous humor to achieve a more stable and long-term IOP reduction for 10 h. In addition, cytotoxicity and hemolysis tests showed that MIDFDS had better biocompatibility than Betoptic. The dual-functioning microspheres presented in this study provide the possibility for improved compliance due to low cytotoxicity and hemolysis, which suggests promising clinical implications.http://dx.doi.org/10.1080/10717544.2021.1981493glaucomamontmorilloniteeudragitmicrospherecontact angle |
| spellingShingle | Hanyu Liu Xinyue Han Huamei Li Qi Tao Jie Hu Shuo Liu Huaixin Liu Jun Zhou Wei Li Fan Yang Qineng Ping Shijie Wei Hongmei Liu Huaqing Lin Dongzhi Hou Wettability and contact angle affect precorneal retention and pharmacodynamic behavior of microspheres Drug Delivery glaucoma montmorillonite eudragit microsphere contact angle |
| title | Wettability and contact angle affect precorneal retention and pharmacodynamic behavior of microspheres |
| title_full | Wettability and contact angle affect precorneal retention and pharmacodynamic behavior of microspheres |
| title_fullStr | Wettability and contact angle affect precorneal retention and pharmacodynamic behavior of microspheres |
| title_full_unstemmed | Wettability and contact angle affect precorneal retention and pharmacodynamic behavior of microspheres |
| title_short | Wettability and contact angle affect precorneal retention and pharmacodynamic behavior of microspheres |
| title_sort | wettability and contact angle affect precorneal retention and pharmacodynamic behavior of microspheres |
| topic | glaucoma montmorillonite eudragit microsphere contact angle |
| url | http://dx.doi.org/10.1080/10717544.2021.1981493 |
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