Sustained release studies on 3-hydroxyflavone-loaded eudragit nanofibers to combat inflammatory conditions

Abstract

The strategy for this study is the fabrication of biocompatible eudragit (RS100) nanofiber carrying a newly synthesised 3-hydroxyflavone with potential anti-inflammatory property for sustained delivery in the periodontal pocket. As this compound is proved to be biocompatible and exhibiting promising biological activities, it is taken as a molecule of choice. The polymer solution with bioactive compound was electrospun to yield nanofiber scaffolds which were characterized using FESEM, PXRD, FTIR, UV spectroscopy and TGA. The developed nanofibers exhibited bead-free and randomly arranged structures with a diameter range of 261 nm-285 nm.

Highlights

The monolithic electrospun eudragit nanofibers, loaded with newly synthesised flavonoid derivative resulted with sustained release profile.

The kinetics of the release process followed Korsmeyer-Peppas model.

The diameter of the nanofiber increased upon increasing the concentration of the compound.

A good biocompatibility and anti-inflammatory properties are revealed by the fabricated system.

The amorphous nature of the polymer is depicted by its low degree of crystallinity whereas the values increased profusely for compound loaded samples indicating the semicrystalline nature. The evaluation of surface wettability by the apparent contact angle measurement showed a hydrophilic nature of the mat with θ=82.8 º upon increasing the concentration. This is followed by an increase in swelling ability which is conducive to increased proliferation and the cell attachment characteristics required by the periodontal barrier membrane. Furthermore, upon dissolution, nanofibers showed a release of 49.26% of the encapsulated drug for approximately 32 hours in an in-vitro model with R² (0.9863) fitting to Korsmeyer Peppas model suggesting a diffusion mechanism.

In addition, cell viability greater than 90% was obtained from in-vitro study. Concomitantly, in-vivo biocompatibility studied using Drosophila melanogaster model depicted 82% of the survival rate. The drug also showed an astonishing effect again albumin denaturation (>80%). All the results were compared with standard drug diclofenac diethylamine at the same concentration. The results thus revealed the suitability of the fabricated nanofiber mat with potential application in combating periodontal infections.

Materials

The polymer used in the experiment was Eudragit (RS100) (C19H34ClNO6) (Molecular weight – 32,000 g/mol) which was obtained as test sample from Evonik Industries, Germany. Diclofenac diethylamine was obtained from Srikem Laboratories Pvt. Limited, Mumbai. Acetone (M. W. 58.08) and N, N-dimethylformamaide (M. W. 73.09), ethanol, hydrogen peroxide (30%) were procured from Merck, India. Artificial saliva solution was prepared in the laboratory that has a composition of Na2HPO4 (0.26 g/L), NaCl.

Kakunje Shreevani, Badiadka Narayana, Balladka Kunhanna Sarojini, Bikrodi Sesappa Dayananda, Aroor Ganesha, Punchappady Devasya Rekha, Raifa Abdul Aziz, Shamprasad Varija Raghu, Sustained release studies on 3-hydroxyflavone-loaded eudragit nanofibers to combat inflammatory conditions, Journal of Drug Delivery Science and Technology, 2025, 106677, ISSN 1773-2247, https://doi.org/10.1016/j.jddst.2025.106677.