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Polymers 2018, 10(2), 199; doi:10.3390/polym10020199

Mucoadhesive Cyclodextrin-Modified Thiolated Poly(aspartic acid) as a Potential Ophthalmic Drug Delivery System

Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary
Soft Matters Group, Department of Physical Chemistry and Materials Science, Budapest University of Technology and Economics, Műegyetem rkp. 3, H-1111 Budapest, Hungary
Department of Ophthalmology, Faculty of Medicine, University of Szeged, Korányi Fasor 10-11, H-6720 Szeged, Hungary
Author to whom correspondence should be addressed.
Received: 5 January 2018 / Revised: 1 February 2018 / Accepted: 14 February 2018 / Published: 16 February 2018
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Thiolated poly(aspartic acid) is known as a good mucoadhesive polymer in aqueous ophthalmic formulations. In this paper, cyclodextrin-modified thiolated poly(aspartic acid) was synthesized for the incorporation of prednisolone, a lipophilic ophthalmic drug, in an aqueous in situ gellable mucoadhesive solution. This polymer combines the advantages of cyclodextrins and thiolated polymers. The formation of the cyclodextrin-drug complex in the gels was analyzed by X-ray powder diffraction. The ocular applicability of the polymer was characterized by means of physicochemical, rheological and drug diffusion tests. It was established that the chemical bonding of the cyclodextrin molecule did not affect the complexation of prednisolone, while the polymer solution preserved its in situ gellable and good mucoadhesive characteristics. The chemical immobilization of cyclodextrin modified the diffusion profile of prednisolone and prolonged drug release was observed. The combination of free and immobilized cyclodextrins provided the best release profile because the free complex can diffuse rapidly, while the bonded complex ensures a prolonged action. View Full-Text
Keywords: thiolated polymer; mucoadhesion; cyclodextrin; in situ gelation; ophthalmic drug delivery thiolated polymer; mucoadhesion; cyclodextrin; in situ gelation; ophthalmic drug delivery

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Budai-Szűcs, M.; Kiss, E.L.; Szilágyi, B.Á.; Szilágyi, A.; Gyarmati, B.; Berkó, S.; Kovács, A.; Horvát, G.; Aigner, Z.; Soós, J.; Csányi, E. Mucoadhesive Cyclodextrin-Modified Thiolated Poly(aspartic acid) as a Potential Ophthalmic Drug Delivery System. Polymers 2018, 10, 199.

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