Ex Vivo Conjunctival Retention and Transconjunctival Transport of Poorly Soluble Drugs Using Polymeric Micelles
This paper addresses the problem of ocular delivery of lipophilic drugs. The aim of the paper is the evaluation of polymeric micelles, prepared using TPGS (<span style="font-variant: small-caps;">d</span>-α-Tocopheryl polyethylene glycol 1000 succinate), a water-solubl...
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| Format: | Article |
| Language: | English |
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MDPI AG
2019-09-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/11/9/476 |
| _version_ | 1818005625893814272 |
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| author | Silvia Pescina Leticia Grolli Lucca Paolo Govoni Cristina Padula Elena Del Favero Laura Cantù Patrizia Santi Sara Nicoli |
| author_facet | Silvia Pescina Leticia Grolli Lucca Paolo Govoni Cristina Padula Elena Del Favero Laura Cantù Patrizia Santi Sara Nicoli |
| author_sort | Silvia Pescina |
| collection | DOAJ |
| description | This paper addresses the problem of ocular delivery of lipophilic drugs. The aim of the paper is the evaluation of polymeric micelles, prepared using TPGS (<span style="font-variant: small-caps;">d</span>-α-Tocopheryl polyethylene glycol 1000 succinate), a water-soluble derivative of Vitamin E and/or poloxamer 407, as a vehicle for the ocular delivery of dexamethasone, cyclosporine, and econazole nitrate. The research steps were: (1) characterize polymeric micelles by dynamic light scattering (DLS) and X-ray scattering; (2) evaluate the solubility increase of the three drugs; (3) measure the in vitro transport and conjunctiva retention, in comparison to conventional vehicles; (4) investigate the mechanisms of enhancement, by studying drug release from the micelles and transconjunctival permeation of TPGS; and (5) study the effect of micelles application on the histology of conjunctiva. The data obtained demonstrate the application potential of polymeric micelles in ocular delivery, due to their ability to increase the solubility of lipophilic drugs and enhance transport in and across the conjunctival epithelium. The best-performing formulation was the one made of TPGS alone (micelles size ≈ 12 nm), probably because of the higher mobility of these micelles, an enhanced interaction with the conjunctival epithelium, and, possibly, the penetration of intact micelles. |
| first_indexed | 2024-04-14T04:47:28Z |
| format | Article |
| id | doaj.art-9b016fa53352489aac21ef77997e2ccf |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-14T04:47:28Z |
| publishDate | 2019-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-9b016fa53352489aac21ef77997e2ccf2022-12-22T02:11:25ZengMDPI AGPharmaceutics1999-49232019-09-0111947610.3390/pharmaceutics11090476pharmaceutics11090476Ex Vivo Conjunctival Retention and Transconjunctival Transport of Poorly Soluble Drugs Using Polymeric MicellesSilvia Pescina0Leticia Grolli Lucca1Paolo Govoni2Cristina Padula3Elena Del Favero4Laura Cantù5Patrizia Santi6Sara Nicoli7Department of Food and Drug, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, ItalyDepartment of Food and Drug, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, ItalyDepartment of Medicine and Surgery, University of Parma, via Volturno 39, 43126 Parma, ItalyDepartment of Food and Drug, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, ItalyDepartment of Medical Biotechnologies and Translational Medicine, LITA, University of Milan, 20090 Segrate (MI), ItalyDepartment of Medical Biotechnologies and Translational Medicine, LITA, University of Milan, 20090 Segrate (MI), ItalyDepartment of Food and Drug, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, ItalyDepartment of Food and Drug, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, ItalyThis paper addresses the problem of ocular delivery of lipophilic drugs. The aim of the paper is the evaluation of polymeric micelles, prepared using TPGS (<span style="font-variant: small-caps;">d</span>-α-Tocopheryl polyethylene glycol 1000 succinate), a water-soluble derivative of Vitamin E and/or poloxamer 407, as a vehicle for the ocular delivery of dexamethasone, cyclosporine, and econazole nitrate. The research steps were: (1) characterize polymeric micelles by dynamic light scattering (DLS) and X-ray scattering; (2) evaluate the solubility increase of the three drugs; (3) measure the in vitro transport and conjunctiva retention, in comparison to conventional vehicles; (4) investigate the mechanisms of enhancement, by studying drug release from the micelles and transconjunctival permeation of TPGS; and (5) study the effect of micelles application on the histology of conjunctiva. The data obtained demonstrate the application potential of polymeric micelles in ocular delivery, due to their ability to increase the solubility of lipophilic drugs and enhance transport in and across the conjunctival epithelium. The best-performing formulation was the one made of TPGS alone (micelles size ≈ 12 nm), probably because of the higher mobility of these micelles, an enhanced interaction with the conjunctival epithelium, and, possibly, the penetration of intact micelles.https://www.mdpi.com/1999-4923/11/9/476ocular deliverypolymeric micellesconjunctivasmall angle X-ray scattering (SAXS)econazolecyclosporinedexamethasonesolubilityTPGSpoloxamer 407 |
| spellingShingle | Silvia Pescina Leticia Grolli Lucca Paolo Govoni Cristina Padula Elena Del Favero Laura Cantù Patrizia Santi Sara Nicoli Ex Vivo Conjunctival Retention and Transconjunctival Transport of Poorly Soluble Drugs Using Polymeric Micelles Pharmaceutics ocular delivery polymeric micelles conjunctiva small angle X-ray scattering (SAXS) econazole cyclosporine dexamethasone solubility TPGS poloxamer 407 |
| title | Ex Vivo Conjunctival Retention and Transconjunctival Transport of Poorly Soluble Drugs Using Polymeric Micelles |
| title_full | Ex Vivo Conjunctival Retention and Transconjunctival Transport of Poorly Soluble Drugs Using Polymeric Micelles |
| title_fullStr | Ex Vivo Conjunctival Retention and Transconjunctival Transport of Poorly Soluble Drugs Using Polymeric Micelles |
| title_full_unstemmed | Ex Vivo Conjunctival Retention and Transconjunctival Transport of Poorly Soluble Drugs Using Polymeric Micelles |
| title_short | Ex Vivo Conjunctival Retention and Transconjunctival Transport of Poorly Soluble Drugs Using Polymeric Micelles |
| title_sort | ex vivo conjunctival retention and transconjunctival transport of poorly soluble drugs using polymeric micelles |
| topic | ocular delivery polymeric micelles conjunctiva small angle X-ray scattering (SAXS) econazole cyclosporine dexamethasone solubility TPGS poloxamer 407 |
| url | https://www.mdpi.com/1999-4923/11/9/476 |
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