Stable Atropine Loaded Film As a Potential Ocular Delivery System For Treatment Of Myopia
© 2021. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature..
PURPOSE: The objective of the present study was to prepare stable and high bioavailability ocular atropine loaded films (ATR-films) as potential ocular drug delivery systems for the treatment of myopia.
METHODS: ATR-films were prepared by the solvent casting method and the physical properties of films were evaluated including thickness, water content, light transparency, disintegration time, and mechanical properties. FT-IR, DSC, XRD, TGA, AFM, and Raman spectroscopy were performed to characterize the film. The stability test was conducted under different conditions, such as high humidity, high temperature, and strong light. The pharmacokinetic study and irritation assessment were conducted in rabbits. The efficacy of ATR-films was evaluated by refraction and ocular biometry in myopia guinea pigs.
RESULT: After optimizing the formulation, the resulting ATR-film was flexible and transparent with lower water content (8.43% ± 1.25). As expected, the ATR-film was stable and hydrolysate was not detected, while the content of hydrolysate in ATR eye drops can reach up to 8.1867% (limit: < 0.2%) in the stability study. The safety assessment both in vitro and in vivo confirmed that the ATR-film was biocompatible. Moreover, the bioavailability (conjunctiva 3.21-fold, cornea 2.87-fold, retina 1.35-fold, sclera 2.05-fold) was greatly improved compared with the ATR eye drops in vivo pharmacokinetic study. The pharmacodynamic study results showed that the ATR-film can slow the progress of form-deprivation myopia (~ 100 ± 0.81D), indicating that it has a certain therapeutic effect on form-deprivation myopia.
CONCLUSION: The ATR-film with good stability and high bioavailability will have great potential for the treatment of myopia.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2021 |
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| Erschienen: |
2021 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:38 |
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| Enthalten in: |
Pharmaceutical research - 38(2021), 11 vom: 12. Nov., Seite 1931-1946 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Ji, Muse [VerfasserIn] |
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| Links: |
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| Themen: |
7C0697DR9I |
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| Anmerkungen: |
Date Completed 28.02.2022 Date Revised 26.04.2023 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1007/s11095-021-03135-4 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM333109643 |
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| 500 | |a Citation Status MEDLINE | ||
| 520 | |a © 2021. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature. | ||
| 520 | |a PURPOSE: The objective of the present study was to prepare stable and high bioavailability ocular atropine loaded films (ATR-films) as potential ocular drug delivery systems for the treatment of myopia | ||
| 520 | |a METHODS: ATR-films were prepared by the solvent casting method and the physical properties of films were evaluated including thickness, water content, light transparency, disintegration time, and mechanical properties. FT-IR, DSC, XRD, TGA, AFM, and Raman spectroscopy were performed to characterize the film. The stability test was conducted under different conditions, such as high humidity, high temperature, and strong light. The pharmacokinetic study and irritation assessment were conducted in rabbits. The efficacy of ATR-films was evaluated by refraction and ocular biometry in myopia guinea pigs | ||
| 520 | |a RESULT: After optimizing the formulation, the resulting ATR-film was flexible and transparent with lower water content (8.43% ± 1.25). As expected, the ATR-film was stable and hydrolysate was not detected, while the content of hydrolysate in ATR eye drops can reach up to 8.1867% (limit: < 0.2%) in the stability study. The safety assessment both in vitro and in vivo confirmed that the ATR-film was biocompatible. Moreover, the bioavailability (conjunctiva 3.21-fold, cornea 2.87-fold, retina 1.35-fold, sclera 2.05-fold) was greatly improved compared with the ATR eye drops in vivo pharmacokinetic study. The pharmacodynamic study results showed that the ATR-film can slow the progress of form-deprivation myopia (~ 100 ± 0.81D), indicating that it has a certain therapeutic effect on form-deprivation myopia | ||
| 520 | |a CONCLUSION: The ATR-film with good stability and high bioavailability will have great potential for the treatment of myopia | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Atropine | |
| 650 | 4 | |a Fast-dissolve | |
| 650 | 4 | |a Form-deprivation | |
| 650 | 4 | |a Myopia | |
| 650 | 4 | |a Ocular film | |
| 650 | 7 | |a Muscarinic Antagonists |2 NLM | |
| 650 | 7 | |a Atropine |2 NLM | |
| 650 | 7 | |a 7C0697DR9I |2 NLM | |
| 700 | 1 | |a Liu, Hongbing |e verfasserin |4 aut | |
| 700 | 1 | |a Ma, Shuting |e verfasserin |4 aut | |
| 700 | 1 | |a Kong, Jun |e verfasserin |4 aut | |
| 700 | 1 | |a Jia, Yannan |e verfasserin |4 aut | |
| 700 | 1 | |a Gou, Jingxin |e verfasserin |4 aut | |
| 700 | 1 | |a Yin, Tian |e verfasserin |4 aut | |
| 700 | 1 | |a He, Haibing |e verfasserin |4 aut | |
| 700 | 1 | |a Zhang, Yu |e verfasserin |4 aut | |
| 700 | 1 | |a Tang, Xing |e verfasserin |4 aut | |
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