Nepafenac-Loaded Cyclodextrin/Polymer Nanoaggregates: A New Approach to Eye Drop Formulation
The topical administration route is commonly used for targeting therapeutics to the eye; however, improving the bioavailability of drugs applied directly to the eye remains a challenge. Different strategies have been studied to address this challenge. One of them is the use of aggregates that are fo...
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| Format: | Article |
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MDPI AG
2019-01-01
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| Series: | Materials |
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| Online Access: | http://www.mdpi.com/1996-1944/12/2/229 |
| _version_ | 1811338328963809280 |
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| author | Blanca Lorenzo-Veiga Hakon Hrafn Sigurdsson Thorsteinn Loftsson |
| author_facet | Blanca Lorenzo-Veiga Hakon Hrafn Sigurdsson Thorsteinn Loftsson |
| author_sort | Blanca Lorenzo-Veiga |
| collection | DOAJ |
| description | The topical administration route is commonly used for targeting therapeutics to the eye; however, improving the bioavailability of drugs applied directly to the eye remains a challenge. Different strategies have been studied to address this challenge. One of them is the use of aggregates that are formed easily by self-assembly of cyclodextrin (CD)/drug complexes in aqueous solution. The aim of this study was to design a new eye drop formulation based on aggregates formed between CD/drug complexes. For this purpose, the physicochemical properties of the aggregates associated with six CDs and selected water-soluble polymers were analysed. Complex formation was studied using differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR) and 1H nuclear magnetic resonance spectroscopy (1H-NMR). Results showed that HPβCD performed best in terms of solubilization, while γCD performed best in terms of enhancing nanoaggregate formation. Formation of inclusion complexes was confirmed by DSC, FT-IR and 1H-NMR studies. A mixture of 15% (w/v) γCD and 8% (w/v) HPβCD was selected for formulation studies. It was concluded that formulations with aggregate sizes less than 1 µm and viscosity around 10–19 centipoises can be easily prepared using a mixture of CDs. Formulations containing polymeric drug/CD nanoaggregates represent an interesting strategy for enhanced topical delivery of nepafenac. |
| first_indexed | 2024-04-13T18:09:26Z |
| format | Article |
| id | doaj.art-8c3b22dfdf244766951f66814f6459a1 |
| institution | Directory Open Access Journal |
| issn | 1996-1944 |
| language | English |
| last_indexed | 2024-04-13T18:09:26Z |
| publishDate | 2019-01-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Materials |
| spelling | doaj.art-8c3b22dfdf244766951f66814f6459a12022-12-22T02:35:57ZengMDPI AGMaterials1996-19442019-01-0112222910.3390/ma12020229ma12020229Nepafenac-Loaded Cyclodextrin/Polymer Nanoaggregates: A New Approach to Eye Drop FormulationBlanca Lorenzo-Veiga0Hakon Hrafn Sigurdsson1Thorsteinn Loftsson2Faculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, IS-107 Reykjavik, IcelandFaculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, IS-107 Reykjavik, IcelandFaculty of Pharmaceutical Sciences, University of Iceland, Hofsvallagata 53, IS-107 Reykjavik, IcelandThe topical administration route is commonly used for targeting therapeutics to the eye; however, improving the bioavailability of drugs applied directly to the eye remains a challenge. Different strategies have been studied to address this challenge. One of them is the use of aggregates that are formed easily by self-assembly of cyclodextrin (CD)/drug complexes in aqueous solution. The aim of this study was to design a new eye drop formulation based on aggregates formed between CD/drug complexes. For this purpose, the physicochemical properties of the aggregates associated with six CDs and selected water-soluble polymers were analysed. Complex formation was studied using differential scanning calorimetry (DSC), Fourier-transform infrared spectroscopy (FT-IR) and 1H nuclear magnetic resonance spectroscopy (1H-NMR). Results showed that HPβCD performed best in terms of solubilization, while γCD performed best in terms of enhancing nanoaggregate formation. Formation of inclusion complexes was confirmed by DSC, FT-IR and 1H-NMR studies. A mixture of 15% (w/v) γCD and 8% (w/v) HPβCD was selected for formulation studies. It was concluded that formulations with aggregate sizes less than 1 µm and viscosity around 10–19 centipoises can be easily prepared using a mixture of CDs. Formulations containing polymeric drug/CD nanoaggregates represent an interesting strategy for enhanced topical delivery of nepafenac.http://www.mdpi.com/1996-1944/12/2/229cyclodextrinnepafenacpolymercomplexationaggregateself-assembleocular drug delivery |
| spellingShingle | Blanca Lorenzo-Veiga Hakon Hrafn Sigurdsson Thorsteinn Loftsson Nepafenac-Loaded Cyclodextrin/Polymer Nanoaggregates: A New Approach to Eye Drop Formulation Materials cyclodextrin nepafenac polymer complexation aggregate self-assemble ocular drug delivery |
| title | Nepafenac-Loaded Cyclodextrin/Polymer Nanoaggregates: A New Approach to Eye Drop Formulation |
| title_full | Nepafenac-Loaded Cyclodextrin/Polymer Nanoaggregates: A New Approach to Eye Drop Formulation |
| title_fullStr | Nepafenac-Loaded Cyclodextrin/Polymer Nanoaggregates: A New Approach to Eye Drop Formulation |
| title_full_unstemmed | Nepafenac-Loaded Cyclodextrin/Polymer Nanoaggregates: A New Approach to Eye Drop Formulation |
| title_short | Nepafenac-Loaded Cyclodextrin/Polymer Nanoaggregates: A New Approach to Eye Drop Formulation |
| title_sort | nepafenac loaded cyclodextrin polymer nanoaggregates a new approach to eye drop formulation |
| topic | cyclodextrin nepafenac polymer complexation aggregate self-assemble ocular drug delivery |
| url | http://www.mdpi.com/1996-1944/12/2/229 |
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