Binary Polymeric Surfactant Mixtures for the Development of Novel Loteprednol Etabonate Nanomicellar Eyedrops
The treatment of several ocular inflammatory conditions affecting different areas of the ocular globe involves the administration of topical ophthalmic formulations containing corticosteroids. This research was aimed at evaluating the solubilising efficacy of 5.0% <i>w</i>/<i>w<...
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| Format: | Article |
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MDPI AG
2023-06-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/16/6/864 |
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| author | Silvia Tampucci Daniela Monti Susi Burgalassi Eleonora Terreni Valentina Paganini Mariacristina Di Gangi Patrizia Chetoni |
| author_facet | Silvia Tampucci Daniela Monti Susi Burgalassi Eleonora Terreni Valentina Paganini Mariacristina Di Gangi Patrizia Chetoni |
| author_sort | Silvia Tampucci |
| collection | DOAJ |
| description | The treatment of several ocular inflammatory conditions affecting different areas of the ocular globe involves the administration of topical ophthalmic formulations containing corticosteroids. This research was aimed at evaluating the solubilising efficacy of 5.0% <i>w</i>/<i>w</i> of different binary mixtures of commercial amphiphilic polymeric surfactants with the purpose of obtaining nanomicellar solutions containing a high amount of loteprednol etabonate (LE). The selected LE-TPGS/HS nanomicelles, containing 0.253 mg/mL of the drug, had a small size (=13.57 nm) and uniform distribution (Polydispersity Index = 0.271), appeared completely transparent and perfectly filterable through 0.2 μm membrane filter, and remained stable up to 30 days at 4 °C. The critical micellar concentration (CMC<sub>TPGS/HS</sub>) was 0.0983 mM and the negative value of the interaction parameter between the polymeric-surfactant-building unit (β<sub>TPGS/HS</sub> = −0.1322) confirmed the ability of the polymeric surfactants to interact, favouring the dissolution of LE into nanomicelles. The disappearance of the endothermic peak of LE in the DSC analysis confirmed the interactions of LE with the polymeric surfactants. LE-TPGS/HS produced in vitro LE which sustained diffusion for 44 h (more than 40% of encapsulated LE). Furthermore, the lack of a significant cytotoxic effect on a sensitive corneal epithelial cell line makes it a candidate for further biological studies. |
| first_indexed | 2024-03-11T02:03:20Z |
| format | Article |
| id | doaj.art-8ebf96ea3ab94224a7ea4771f0d20765 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-11T02:03:20Z |
| publishDate | 2023-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-8ebf96ea3ab94224a7ea4771f0d207652023-11-18T12:02:37ZengMDPI AGPharmaceuticals1424-82472023-06-0116686410.3390/ph16060864Binary Polymeric Surfactant Mixtures for the Development of Novel Loteprednol Etabonate Nanomicellar EyedropsSilvia Tampucci0Daniela Monti1Susi Burgalassi2Eleonora Terreni3Valentina Paganini4Mariacristina Di Gangi5Patrizia Chetoni6Department of Pharmacy, University of Pisa, 56126 Pisa, ItalyDepartment of Pharmacy, University of Pisa, 56126 Pisa, ItalyDepartment of Pharmacy, University of Pisa, 56126 Pisa, ItalyDepartment of Pharmacy, University of Pisa, 56126 Pisa, ItalyDepartment of Pharmacy, University of Pisa, 56126 Pisa, ItalyDepartment of Pharmacy, University of Pisa, 56126 Pisa, ItalyDepartment of Pharmacy, University of Pisa, 56126 Pisa, ItalyThe treatment of several ocular inflammatory conditions affecting different areas of the ocular globe involves the administration of topical ophthalmic formulations containing corticosteroids. This research was aimed at evaluating the solubilising efficacy of 5.0% <i>w</i>/<i>w</i> of different binary mixtures of commercial amphiphilic polymeric surfactants with the purpose of obtaining nanomicellar solutions containing a high amount of loteprednol etabonate (LE). The selected LE-TPGS/HS nanomicelles, containing 0.253 mg/mL of the drug, had a small size (=13.57 nm) and uniform distribution (Polydispersity Index = 0.271), appeared completely transparent and perfectly filterable through 0.2 μm membrane filter, and remained stable up to 30 days at 4 °C. The critical micellar concentration (CMC<sub>TPGS/HS</sub>) was 0.0983 mM and the negative value of the interaction parameter between the polymeric-surfactant-building unit (β<sub>TPGS/HS</sub> = −0.1322) confirmed the ability of the polymeric surfactants to interact, favouring the dissolution of LE into nanomicelles. The disappearance of the endothermic peak of LE in the DSC analysis confirmed the interactions of LE with the polymeric surfactants. LE-TPGS/HS produced in vitro LE which sustained diffusion for 44 h (more than 40% of encapsulated LE). Furthermore, the lack of a significant cytotoxic effect on a sensitive corneal epithelial cell line makes it a candidate for further biological studies.https://www.mdpi.com/1424-8247/16/6/864loteprednol etabonateKolliphor<sup>®</sup> HS-15D-alpha-tocopheryl polyethylene glycol 1000 succinateTPGSocular drug deliverymixed nanomicelles |
| spellingShingle | Silvia Tampucci Daniela Monti Susi Burgalassi Eleonora Terreni Valentina Paganini Mariacristina Di Gangi Patrizia Chetoni Binary Polymeric Surfactant Mixtures for the Development of Novel Loteprednol Etabonate Nanomicellar Eyedrops Pharmaceuticals loteprednol etabonate Kolliphor<sup>®</sup> HS-15 D-alpha-tocopheryl polyethylene glycol 1000 succinate TPGS ocular drug delivery mixed nanomicelles |
| title | Binary Polymeric Surfactant Mixtures for the Development of Novel Loteprednol Etabonate Nanomicellar Eyedrops |
| title_full | Binary Polymeric Surfactant Mixtures for the Development of Novel Loteprednol Etabonate Nanomicellar Eyedrops |
| title_fullStr | Binary Polymeric Surfactant Mixtures for the Development of Novel Loteprednol Etabonate Nanomicellar Eyedrops |
| title_full_unstemmed | Binary Polymeric Surfactant Mixtures for the Development of Novel Loteprednol Etabonate Nanomicellar Eyedrops |
| title_short | Binary Polymeric Surfactant Mixtures for the Development of Novel Loteprednol Etabonate Nanomicellar Eyedrops |
| title_sort | binary polymeric surfactant mixtures for the development of novel loteprednol etabonate nanomicellar eyedrops |
| topic | loteprednol etabonate Kolliphor<sup>®</sup> HS-15 D-alpha-tocopheryl polyethylene glycol 1000 succinate TPGS ocular drug delivery mixed nanomicelles |
| url | https://www.mdpi.com/1424-8247/16/6/864 |
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