Development of axitinib-loaded polymeric ocular implants for the treatment of posterior ocular diseases.

Autor: Annuryanti F; School of Pharmacy, Queen's University Belfast, Belfast, United Kingdom; Faculty of Pharmacy, Airlangga University, Surabaya, Indonesia., Adhami M; School of Pharmacy, Queen's University Belfast, Belfast, United Kingdom., Abdi U; School of Pharmacy, Queen's University Belfast, Belfast, United Kingdom., Robles JD; School of Pharmacy, Queen's University Belfast, Belfast, United Kingdom; Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Seville, 41012 Seville, Spain., Larrañeta E; School of Pharmacy, Queen's University Belfast, Belfast, United Kingdom., Vora LK; School of Pharmacy, Queen's University Belfast, Belfast, United Kingdom. Electronic address: l.vora@qub.ac.uk., Raghu Raj Singh T; School of Pharmacy, Queen's University Belfast, Belfast, United Kingdom. Electronic address: r.thakur@qub.ac.uk.
Jazyk: angličtina
Zdroj: International journal of pharmaceutics [Int J Pharm] 2024 Dec 18; Vol. 669, pp. 125099. Date of Electronic Publication: 2024 Dec 18.
DOI: 10.1016/j.ijpharm.2024.125099
Abstrakt: Diabetic retinopathy (DR) and age-related macular degeneration (AMD) are the primary causes of vision impairment and blindness worldwide. The current treatment for these diseases is an intravitreal injection of anti-VEGF agents, which are costly and require frequent injections. Implants can be used to sustain the release of drugs and minimize side effects. Axitinib (AX) is a potent VEGF receptor inhibitor and a promising candidate for treating posterior ocular diseases, such as diabetic retinopathy (DR) and age-related macular degeneration (AMD). A sustained release of AX was successfully achieved from 3D-printed AX-loaded implants fabricated using the well-known 3D printing technique, semi-solid extrusion (SSE). AX at concentrations of 10% w/w and 20% w/w was incorporated within the polycaprolactone (PCL) and Precirol®-based matrix. The fabricated implants were characterized via FTIR spectroscopy, SEM imaging, and thermal analysis. The implants were also evaluated for their drug release and biocompatibility. The AX-loaded implants exhibited thermal stability, and no chemical interactions were found between AX and the matrix components. The release mechanism study of AX revealed that the concentration of drug loading influenced AX release from the implant, with a 10% w/w and 20 %w/w of AX showing first-order and Korsmeyer-Peppas mechanism, respectively. A biocompatibility study using ARPE-19 cells confirmed that AX-loaded implants are nontoxic and safe for ocular use.
Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
(Copyright © 2024 The Authors. Published by Elsevier B.V. All rights reserved.)
Databáze: MEDLINE