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Controlled release from aspirin based linear biodegradable poly (anhydride esters) for anti-inflammatory activity

Dasgupta, Queeny and Movva, Sahitya and Chatterjee, Kaushik and Madras, Giridhar (2017) Controlled release from aspirin based linear biodegradable poly (anhydride esters) for anti-inflammatory activity. In: INTERNATIONAL JOURNAL OF PHARMACEUTICS, 528 (1-2). pp. 732-740.

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Official URL: http://doi.org/10.1016/j.ijpharm.2017.06.065


This work reports the synthesis of a novel, aspirin-loaded, linear poly (anhydride ester) and provides mechanistic insights into the release of aspirin from this polymer for anti-inflammatory activity. As compared to conventional drug delivery systems that rely on diffusion based release, incorporation of bioactives in the polymer backbone is challenging and high loading is difficult to achieve. In the present study, we exploit the pentafunctional sugar alcohol (xylitol) to provide sites for drug (aspirin) attachment at its non-terminal -OH groups. The terminal -OH groups are polymerized with a diacid anhydride. The hydrolysis of the anhydride and ester bonds under physiological conditions release aspirin from the matrix. The resulting poly(anhydride ester) has high drug loading (53%) and displays controlled release kinetics of aspirin. The polymer releases 8.5 % and 20%, of the loaded drug in one and four weeks, respectively and has a release rate constant of 0.0035 h (0.61). The release rate is suitable for its use as an anti-inflammatory agent without being cytotoxic. The polymer exhibits good cytocompatibility and anti-inflammatory properties and may find applications as injectable or as an implantable bioactive material. The physical insights into the release mechanism can provide development of other drug loaded polymers. (C) 2017 Elsevier B.V. All rights reserved.

Item Type: Journal Article
Additional Information: Copy right for this article belongs to the ELSEVIER SCIENCE BV, PO BOX 211, 1000 AE AMSTERDAM, NETHERLANDS
Department/Centre: Division of Mechanical Sciences > Materials Engineering (formerly Metallurgy)
Date Deposited: 16 Sep 2017 05:47
Last Modified: 16 Sep 2017 05:47
URI: http://eprints.iisc.ac.in/id/eprint/57820

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