Microfluidic-Based Formulation of Essential Oils-Loaded Chitosan Coated PLGA Particles Enhances Their Bioavailability and Nematocidal Activity

Helal, Mohamed A.; Abdel-Gawad, Ahmed M.; Kandil, Omnia M.; Khalifa, Marwa M.E.; Morrison, Alison A.; Bartley, David J.; Cave, Gareth W.V.; Elsheikha, Hany M.

Abstract

In this study, poly (lactic-co-glycolic) acid (PLGA) particles were synthesized and coated with chitosan. Three essential oil (EO) components (eugenol, linalool, and geraniol) were entrapped inside these PLGA particles by using the continuous flow-focusing microfluidic method and a partially water-miscible solvent mixture (dichloromethane: acetone mixture (1:10)). Encapsulation of EO components in PLGA particles was confirmed by Fourier transform infrared spectroscopy, thermogravimetric analysis, and X-ray diffraction, with encapsulation efficiencies 95.14%, 79.68%, and 71.34% and loading capacities 8.88%, 8.38%, and 5.65% in particles entrapped with eugenol, linalool, and geraniol, respectively. The EO components’ dissociation from the loaded particles exhibited an initial burst release in the first 8 h followed by a sustained release phase at significantly slower rates from the coated particles, extending beyond 5 days. The EO components encapsulated in chitosan coated particles up to 5 μg/mL were not cytotoxic to bovine gut cell line (FFKD-1-R) and had no adverse effect on cell growth and membrane integrity compared with free EO components or uncoated particles. Chitosan coated PLGA particles loaded with combined EO components (10 µg/mL) significantly inhibited the motility of the larval stage of Haemonchus contortus and Trichostrongylus axei by 76.9%, and completely inhibited the motility of adult worms (p < 0.05). This nematocidal effect was accompanied by considerable cuticular damage in the treated worms, reflecting a synergistic effect of the combined EO components and an additive effect of chitosan. These results show that encapsulation of EO components, with a potent anthelmintic activity, in chitosan coated PLGA particles improve the bioavailability and efficacy of EO components against ovine gastrointestinal nematodes.

Citation

Helal, M. A., Abdel-Gawad, A. M., Kandil, O. M., Khalifa, M. M., Morrison, A. A., Bartley, D. J., …Elsheikha, H. M. (2022). Microfluidic-Based Formulation of Essential Oils-Loaded Chitosan Coated PLGA Particles Enhances Their Bioavailability and Nematocidal Activity. Pharmaceutics, 14(10), Article 2030. https://doi.org/10.3390/pharmaceutics14102030

• Journal Article Type: Article
• Acceptance Date: Sep 19, 2022
• Online Publication Date: Sep 23, 2022
• Publication Date: Oct 1, 2022
• Deposit Date: Oct 2, 2022
• Publicly Available Date: Oct 3, 2022
• Journal: Pharmaceutics
• Electronic ISSN: 1999-4923
• Publisher: MDPI AG
• Peer Reviewed: Peer Reviewed
• Volume: 14
• Issue: 10
• Article Number: 2030
• DOI: https://doi.org/10.3390/pharmaceutics14102030
• Keywords: Pharmaceutical Science
• Public URL: https://nottingham-repository.worktribe.com/output/11755978
• Publisher URL: https://www.mdpi.com/1999-4923/14/10/2030