Thiolated poly(aspartic acid) as potential in situ gelling, ocular mucoadhesive drug delivery system.

Autor: Horvát G; Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary., Gyarmati B; Soft Matters Group, Department of Physical Chemistry and Materials Science, Budapest University of Technology and Economics, Budafoki út 8., H-1111 Budapest, Hungary., Berkó S; Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary., Szabó-Révész P; Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary., Szilágyi BÁ; Soft Matters Group, Department of Physical Chemistry and Materials Science, Budapest University of Technology and Economics, Budafoki út 8., H-1111 Budapest, Hungary., Szilágyi A; Soft Matters Group, Department of Physical Chemistry and Materials Science, Budapest University of Technology and Economics, Budafoki út 8., H-1111 Budapest, Hungary., Soós J; Department of Ophthalmology, Faculty of Medicine, University of Szeged, Korányi fasor 10-11, H-6720 Szeged, Hungary., Sandri G; Department of Drug Sciences, Faculty of Pharmacy, University of Pavia, viale Taramelli 12, 27100 Pavia, Italy., Bonferoni MC; Department of Drug Sciences, Faculty of Pharmacy, University of Pavia, viale Taramelli 12, 27100 Pavia, Italy., Rossi S; Department of Drug Sciences, Faculty of Pharmacy, University of Pavia, viale Taramelli 12, 27100 Pavia, Italy., Ferrari F; Department of Drug Sciences, Faculty of Pharmacy, University of Pavia, viale Taramelli 12, 27100 Pavia, Italy., Caramella C; Department of Drug Sciences, Faculty of Pharmacy, University of Pavia, viale Taramelli 12, 27100 Pavia, Italy., Csányi E; Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary. Electronic address: csanyi@pharm.u-szeged.hu., Budai-Szűcs M; Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary.
Jazyk: angličtina
Zdroj: European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences [Eur J Pharm Sci] 2015 Jan 25; Vol. 67, pp. 1-11. Date of Electronic Publication: 2014 Nov 04.
DOI: 10.1016/j.ejps.2014.10.013
Abstrakt: The ophthalmic formulations on the market suffer from poor bioavailability, and it would therefore be useful to design a new formulation which is able to prolong the residence time and reduce the administration frequency. Polymer matrices which exhibit strong mucoadhesion are promising platforms in ocular drug delivery from the aspect of improved bioavailability. In the present study, an in situ gelling, mucoadhesive drug delivery system was fabricated from thiolated poly(aspartic acid) (ThioPASP). The thiol groups of ThioPASP are able to form disulphide linkages with the mucin glycoproteins and prolong the residence time on the eye. The effects of the thiol groups on the structure, swelling behaviour and mucoadhesive character of the gel and on the drug release profile were determined. The gel structure was characterized by means of rheology. The ThioPASP gel was demonstrated by rheology, tensile test and 'wash away' measurements to display strong mucoadhesion. The drug release from the ThioPASP gel was studied on a vertical Franz diffusion cell: a burst release of sodium diclofenac occurred in the first hour, followed by sustained release of the encapsulated drug for up to 24h. The results proved the importance of the presence of the thiol groups and suggested that a ThioPASP formulation can be useful as an in situ gelling, ocular dosage form.
(Copyright © 2014 Elsevier B.V. All rights reserved.)
Databáze: MEDLINE
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