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Drug-Eluting Biodegradable Implants for the Sustained Release of Bisphosphonates
Journal article   Open access   Peer reviewed

Drug-Eluting Biodegradable Implants for the Sustained Release of Bisphosphonates

Cintya Dharmayanti, Todd A. Gillam, Desmond B. Williams and Anton Blencowe
Polymers, Vol.12(12), 2930
2020
PMID: 33297466
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CC BY V4.0 Open Access

Abstract

Physical Sciences Polymer Science Science & Technology
Despite being one of the first-line treatments for osteoporosis, the bisphosphonate drug class exhibits an extremely low oral bioavailability (<1%) due to poor absorption from the gastrointestinal tract. To overcome this, and to explore the potential for sustained drug release, bioerodible poly(lactic acid) (PLA) and poly(D,L-lactide-co-glycolide) (PLGA) implants loaded with the bisphosphonate alendronate sodium (ALN) were prepared via hot-melt extrusion. The rate of drug release in vitro was modulated by tailoring the ratio of lactide to glycolide in the polymer and by altering the ALN-loading of the implants. All investigated implants exhibited sustained ALN release in vitro between 25 to 130 days, where implants of greater glycolide composition and higher ALN-loadings released ALN more rapidly. All PLGA implants demonstrated a sigmoidal release profile, characterised by an initial surface dissolution phase, followed by a period of zero-order drug diffusion, then relaxation or erosion of the polymer chains that caused accelerated release over the subsequent days. Contrastingly, the PLA implants demonstrated a logarithmic release profile, characterised by a gradual decrease in ALN release over time.

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Citation topics
1 Clinical & Life Sciences
1.80 Bone Diseases
1.80.1211 Bisphosphonates
Web Of Science research areas
Polymer Science
ESI research areas
Chemistry
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