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Article

Ex Vivo Conjunctival Retention and Transconjunctival Transport of Poorly Soluble Drugs Using Polymeric Micelles

1
Department of Food and Drug, University of Parma, Parco Area delle Scienze 27/A, 43124 Parma, Italy
2
Department of Medicine and Surgery, University of Parma, via Volturno 39, 43126 Parma, Italy
3
Department of Medical Biotechnologies and Translational Medicine, LITA, University of Milan, 20090 Segrate (MI), Italy
*
Author to whom correspondence should be addressed.
Pharmaceutics 2019, 11(9), 476; https://doi.org/10.3390/pharmaceutics11090476
Received: 15 July 2019 / Revised: 10 September 2019 / Accepted: 10 September 2019 / Published: 14 September 2019
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 (d-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. View Full-Text
Keywords: ocular delivery; polymeric micelles; conjunctiva; small angle X-ray scattering (SAXS); econazole; cyclosporine; dexamethasone; solubility; TPGS; poloxamer 407 ocular delivery; polymeric micelles; conjunctiva; small angle X-ray scattering (SAXS); econazole; cyclosporine; dexamethasone; solubility; TPGS; poloxamer 407
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MDPI and ACS Style

Pescina, S.; Grolli Lucca, L.; Govoni, P.; Padula, C.; Del Favero, E.; Cantù, L.; Santi, P.; Nicoli, S. Ex Vivo Conjunctival Retention and Transconjunctival Transport of Poorly Soluble Drugs Using Polymeric Micelles. Pharmaceutics 2019, 11, 476. https://doi.org/10.3390/pharmaceutics11090476

AMA Style

Pescina S, Grolli Lucca L, Govoni P, Padula C, Del Favero E, Cantù L, Santi P, Nicoli S. Ex Vivo Conjunctival Retention and Transconjunctival Transport of Poorly Soluble Drugs Using Polymeric Micelles. Pharmaceutics. 2019; 11(9):476. https://doi.org/10.3390/pharmaceutics11090476

Chicago/Turabian Style

Pescina, Silvia, Leticia Grolli Lucca, Paolo Govoni, Cristina Padula, Elena Del Favero, Laura Cantù, Patrizia Santi, and Sara Nicoli. 2019. "Ex Vivo Conjunctival Retention and Transconjunctival Transport of Poorly Soluble Drugs Using Polymeric Micelles" Pharmaceutics 11, no. 9: 476. https://doi.org/10.3390/pharmaceutics11090476

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