Development of liposomal formulations of the eggplant glycoalkaloids solasonine and solamargine

• Published in: Journal of drug delivery science and technology Vol. 70; p. 103194
• Main Authors: Tatlıdil, Engin, Çolak, Nergiz Gürbüz, Doğanlar, Sami, Frary, Anne
• Format: Journal Article
• Language: English
• Published: Elsevier B.V 01.04.2022
• Subjects: Biomacromolecules; Genus solanum; Liposomes; Nanocarriers; Skin diseases; Skin diseases; Biomacromolecules; Liposomes; Nanocarriers; Genus solanum
• ISSN: 1773-2247
• DOI: 10.1016/j.jddst.2022.103194

The eggplant glycoalkaloids solasonine and solamargine are efficient biomacromolecules against skin diseases but are water-insoluble which results in inefficient treatment due to inadequate transdermal delivery. To address this problem, several liposomal formulations were prepared and evaluated for parameters including lecithin type, hydration temperature, and pH. The optimal formula with high physical and chemical stability included the lecithin Phospholipon 80H hydrated with 10 mM NaCl (pH 5.5). Solasonine - solamargine loaded liposomes were tested for their physical and chemical stability and drug leakage over a three-month period. Furthermore, the drug release profile of the loaded liposomes was evaluated with different release media. The glycoalkaloids and their liposomal formulations were assessed for their biological activity in culture using HaCaT and SCC-25 cell lines. This work resulted in a biologically effective liposomal formulation that was stable (size <220 nm, PDI <0.25, encapsulation efficiency >80%) for at least three months. [Display omitted] •Solasonine and solamargine were encapsulated and evaluated with a lipid-based nanocarrier for the first time.•A new liposomal formulation that creates small, uniformly formed liposomes with high stability was developed.•NaCl is a better hydration solution than other widely used buffers in terms of creating smaller liposomes.•Biological effects of solasonine and solamargine on squamous cell carcinoma was evaluated for the first time.•Liposomal encapsulation of solasonine and solamargine reduced their toxicity as compared to their free forms.