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

• Main Authors: Mária Budai-Szűcs, Eszter L. Kiss, Barnabás Áron Szilágyi, András Szilágyi, Benjámin Gyarmati, Szilvia Berkó, Anita Kovács, Gabriella Horvát, Zoltán Aigner, Judit Soós, Erzsébet Csányi
• Format: Article
• Language: English
• Published: MDPI AG 2018-02-01
• Series: Polymers
• Subjects: thiolated polymer; mucoadhesion; cyclodextrin; in situ gelation; ophthalmic drug delivery
• Online Access: http://www.mdpi.com/2073-4360/10/2/199

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.