Poly(HEMA)/cyclodextrin‐based hydrogels for subconjunctival delivery of cyclosporin A

Abstract

To enhance the solubility and ocular permeability of immunosuppressive agent, cyclosporine A (CsA), three types of delivery systems were prepared using (2‐hydroxypropyl)‐β‐cyclodextrin (HPβCD), and 2‐hydroxyethyl methacrylate (HEMA). Those systems are (i) hydrogels of HPβCD with crosslinking agent ethylene glycol diglycidylether, (ii) poly(HEMA) hydrogels, and (iii) different amounts of HPβCD‐containing poly(HEMA) hydrogels indicated as poly(HEMA‐co‐HPβCD). In the presence of HEMA, hydrogels have desired mechanical integrity with lower equilibrium content than that of hydrogels without HEMA. CsA was loaded into the HPβCD‐based hydrogels by embedding from its aqueous suspensions in higher amounts than that of the poly(HEMA) hydrogels that were loaded by CsA–HPβCD complex solution. Although the poly(HEMA) hydrogels are releasing total CsA in 3 days, long‐term release was realized from HPβCD‐based hydrogels. For subconjunctival administration, regarding to the amounts of loaded CsA, release profiles, and mechanical integrity, the most suitable system is poly(HEMA‐co‐HPβCD) hydrogels in high HPβCD content. © 2014 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2014, 131, 40397.

Applications of Macrocyclic Host Molecules in Immune Modulation and Therapeutic Delivery

“…Researchers have used these hydrogel formulations to deliver cyclosporin A (CsA), an immunosuppressant used to prevent organ transplant rejection and whose systemic administration is limited by off-target effects (Liddicoat and Lavelle, 2019 ; Park et al, 2020 ). Hydrogels prepared from poly(HEMA-co-HP-β-CD) provided controlled release of CsA over 2 months in vitro , with potential applications in subjunctival delivery following corneal graft procedures (Başbag et al, 2014 ). For the promotion of burn wound healing, dual delivery strategies have been described, including in situ polymerizable hydrogels for affinity-based release of resveratrol (an anti-inflammatory) and a plasmid encoding vascular endothelial growth factor (to promote vascularization) (Wang et al, 2019 ).…”

Poly(2-hydroxyethylmethacrylate-graft-folic acid), synthesis, solubility enhancement, and release dynamic of folic acid

“…The data obtained revealed that the swelling process was controlled by second-order kinetics, while the ibuprofen diffusion through the polymer matrix obeyed to the Fickian model. Başbağ et al [33] have prepared three types of delivery polymer systems based on (2-hydroxypropyl)-β-cyclodextrin (HPβCD) and 2-hydroxyethyl methacrylate (HEMA). The resulting materials are poly(HPβCD-co-HEMA) hydrogels containing different HPβCD contents.…”