Development and evaluation of polycaprolactone-based electrospun nanofibers containing timolol maleate as a sustained-release device for treatment of glaucoma: in vivo evaluation in equine eye.
Abstract: Prolonging the drug release can be a suitable approach to overcome the challenges related to topical ophthalmic administration of drugs especially the ones prescribed for chronic ailments. The sustained delivery of the drug would reduce the required frequency of administration which could extremely improve patient compliance and feeling of well-being. This study aimed to develop nanofibrous inserts for sustained ophthalmic delivery of timolol maleate (TIM) for the treatment of glaucoma. Unassigned: Polycaprolactone-based nanofibers containing TIM were prepared using pure polycaprolactone or a blend of it with cellulose acetate or Eudragit RL100 polymers by the electrospinning method. Following the preparation, polymeric inserts were evaluated for morphological and physicochemical properties. The in vitro drug release was assessed and the in vivo efficacy of a selected insert in decreasing the intraocular pressure (IOP) was also evaluated in the equine eyes. Unassigned: Prepared nanofibers indicated diameter ranged between 122-174 nm. The formulations showed suitable physicochemical properties and stability for ophthalmic administration. In vitro release study showed prolonged release of drug during more than 3 days. In vivo evaluation revealed that the prepared insert is non-irritant and non-toxic to the equine eyes while having suitable efficacy in decreasing the IOP during 6 days. Unassigned: Prepared TIM inserts indicated a higher efficacy than commercial TIM eye drop in lowering IOP during a prolonged period. Thus, these formulations can be considered suitable for enhancing patient compliance by reducing the frequency of administration in the treatment of glaucoma.
Copyright: © 2022 Research in Pharmaceutical Sciences.
Publication Date: 2022-09-08 PubMed ID: 36386485PubMed Central: PMC9661680DOI: 10.4103/1735-5362.355196Google Scholar: Lookup
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Summary
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The research article describes the development and testing of a nanofibre-based delivery device for the sustained release of the drug timolol maleate, specifically for treating glaucoma. This approach aims to improve patient comfort and adherence to treatment by reducing the need for frequent drug administration.
Development of Nanofibrous Inserts
- The researchers created nanofibrous inserts from polycaprolactone (a biodegradable polyester), either alone or mixed with cellulose acetate or Eudragit RL100 polymers. These inserts were designed to gradually release the drug timolol maleate, which is often used in glaucoma treatment.
- This was achieved via an electrospinning process, a common technique for producing nanofibers. Electrospinning utilizes electric force to draw charged threads from a droplet of polymer solution, resulting in ultra-fine fibers with high surface-to-volume ratios, ideal for drug delivery.
Morphological and Physicochemical Evaluations
- After preparation, the researchers examined the morphological features and physical-chemical properties of the polymeric inserts. They found that the diameter of the created nanofibers fell within the range of 122-174 nm.
- The formulations tested exhibited acceptable physicochemical properties and stability for ophthalmic (eye-related) administration, which are crucial considerations for safety and efficacy.
Drug Release and Efficacy Assessment
- The researchers carried out a release study to evaluate how the drug was discharged from the insert over time. The data suggested the drug was slowly and steadily released for more than 3 days, supporting its potential to alleviate the need for frequent drug administration.
- Next, the selected insert was tested for toxicity and irritation in equine eyes and was found to be neither irritant nor toxic. In terms of efficacy, the insert successfully lowered intraocular pressure (a reliable indicator for glaucoma) over a period of six days.
Comparative Efficacy and Conclusion
- When comparing the new timolol maleate inserts to commercially available timolol maleate eye drops, the inserts performed better in lowering intraocular pressure over a more extended period. This suggests that the developed formulations could be more effective and user-friendly than existing options.
- The researchers concluded that these polycaprolactone-based, nanofibre devices could reduce the frequency of administration in glaucoma treatment, thus potentially improving patient compliance and outcomes.
Cite This Article
APA
Mirzaeei S, Faryadras FB, Mehrandish S, Rezaei L, Daneshgar F, Karami A.
(2022).
Development and evaluation of polycaprolactone-based electrospun nanofibers containing timolol maleate as a sustained-release device for treatment of glaucoma: in vivo evaluation in equine eye.
Res Pharm Sci, 17(5), 468-481.
https://doi.org/10.4103/1735-5362.355196 Publication
Researcher Affiliations
- Pharmaceutical Sciences Research Center, Health Institute, Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran.
- Nano Drug Delivery Research Center, Health Technology Institute, Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran.
- Student Research Committee, Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran.
- Research and Development Department, Rahesh Daru Novin Inc., Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran.
- Department of Ophthalmology, Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran.
- Anterior Segment Department, Fellowship of the Cornea, Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran.
- Student Research Committee, Kermanshah University of Medical Sciences, Kermanshah, I.R. Iran.
Conflict of Interest Statement
The authors declared no conflict of interest in this study.
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Citations
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