Ergosterol Liposomes in Lyophilized Formulations for Buccal Administration
Abstract Liposomes are lipidic vesicles used as drug delivery systems which can be stabilized by lyophilization. Buccal mucosa allows local and systemic drug delivery. Ergosterol is the main sterol component in the fungal membrane and has multiple properties. The aim of the present study was to obtain mucadhesive buccal formulations based on phosphatidylcholine and ergosterol liposomes prepared by sonication and stabilized by lyophilization. Different mixtures of liposomes and excipients in blisters with two geometries were lyophilized. The resulting lyophilizates formulations were characterized. The obtained liposomes’ size was between 100 and 200 nm. 97,56 ± 24,63% of the phosphatidylcholine was incorporated to the liposomes and the entrapment efficiency for ergosterol was 12,92 ± 2,24%. The residual moisture of the lyophilizates was less than 3,5%. Lyophilizates containing alginate rapidly disintegrated in contact with salivary fluid, while those with xantham gum swelled gradually. Interaction between mucin and alginate was not detected, but it was between xantham gum and mucin. In conclusion, lyophilizates with alginate are more suitable for orodispersible formulations and those with xantham gum, for controlled release systems.
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Sahatsapan N, Pamornpathomkul B, Rojanarata T, Ngawhirunpat T, Poonkhum R, Opanasopit P, et al. Feasibility of mucoadhesive chitosan maleimide-coated liposomes for improved buccal delivery of a protein drug. J Drug Deliv Sci Technol. 2022; 69:103173.
Terlizzi V, Scudieri P, Bertozzi F, Guerini M, Condrò G, Perugini P. Evaluation of the Mucoadhesive Properties of Chitosan-Based Microstructured Lipid Carrier (CH-MLC). Pharmaceutics. 2022; 14(1):170.
Agüero L, Zaldivar-Silva D, Peña L, Dias M. Alginate microparticles as oral colon drug delivery device: A review. Carbohydr Polym. 2017; 168:32-43.
Ahmad M, Ritzoulis C, Chen J, Meigui H, Bushra R, Jin Y, et al. Xanthan gum − mucin complexation: Molecular interactions, thermodynamics, and rheological analysis. Food Hydrocoll. 2021; 114:106579.
Ali J, Bong Lee J, Gittings S, Iachelini A, Bennett J, Cram A, et al. Development and optimisation of simulated salivary fluid for biorelevant oral cavity dissolution. Eur J Pharm Biopharm. 2021; 160:125-33.
Boddupalli BM, Mohammed ZNK, Nath A. R, Banji D. Mucoadhesive drug delivery system: An overview. J Adv Pharm Technol Res. 2010; 1(4):381-7.
Charles J, Stewart M. Colorirnetric Determination of Phospholipids with Ammonium Ferrothiocyanate. Anal Biochem. 1980; 104(1):10-14.
Degobert G, Aydin D, Mosqueira F, Araújo RS. Lyophilization of Nanocapsules: Instability Sources, Formulation and Process Parameters.Pharmaceutics. 2021; 13(8):1112.
Franzé S, Selmin F, Samaritani E, Minghetti P, Cilurzo F. Lyophilization of Liposomal Formulations: Still Necessary, Still Challenging. Pharmaceutics. 2018; 10(3):139.
Kuwabara N, Ohta-Shimizu M, Fuwa F, Tomitsuka E, Sato S, Nakagawa S. Ergosterol increases 7-dehydrocholesterol, a cholesterol precursor, and decreases cholesterol in human HepG2 cells. Lipids. 2022; 57(6):303-11.
Liu P, Chen G, Zhang J. A Review of Liposomes as a Drug Delivery System: Current Status of Approved Products, Regulatory Environments, and Future Perspectives. Molecules. 2022; 27(4):1372.
Nsengiyumva EM, Alexandridis P. Xanthan gum in aqueous solutions: Fundamentals and applications. Int J Biol Macromol. 2022; 216:583-604.
Rangsinth P, Sharika R, Pattarachotanant N, Duangjan C, Wongwan C, Sillapachaiyaporn C, et al. Potential Beneficial Effects and Pharmacological Properties of Ergosterol, a Common Bioactive Compound in Edible Mushrooms. Foods. 2023; 12(13):2529.
Real Farmacopea Española. AEMPS; 2015.
Sahatsapan N, Pamornpathomkul B, Rojanarata T, Ngawhirunpat T, Poonkhum R, Opanasopit P, et al. Feasibility of mucoadhesive chitosan maleimide-coated liposomes for improved buccal delivery of a protein drug. J Drug Deliv Sci Technol. 2022; 69:103173.
Terlizzi V, Scudieri P, Bertozzi F, Guerini M, Condrò G, Perugini P. Evaluation of the Mucoadhesive Properties of Chitosan-Based Microstructured Lipid Carrier (CH-MLC). Pharmaceutics. 2022; 14(1):170.
Barbero, J., Sánchez Navarro, A., & de Jesús-Valle, M. J. (2024). Ergosterol Liposomes in Lyophilized Formulations for Buccal Administration. FarmaJournal, 9(2), 7–17. https://doi.org/10.14201/fj202492717
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