Polymer‐Lipid Matrices based on Carboxymethyl Cellulose/Solagum and Liposomes for Controlled Release of Folic Acid

• Published in: European journal of lipid science and technology 2023-07, Vol.125 (7), p.n/a
• Main Authors: Batinić, Petar M., Đorđević, Verica B., Obradović, Nataša S., Krstić, Aleksandar D., Stevanović, Sanja I., Balanč, Bojana D., Marković, Smilja B., Pjanović, Rada V., Mijin, Dušan Ž., Bugarski, Branko M.
• Format: Article
• Language: English
• Subjects: Acids; Atomic force microscopy; biopolymer films; Bonding strength; Carboxymethyl cellulose; Carboxymethylcellulose; Cellulose; Chemical bonds; Controlled release; Drug delivery; Encapsulation; Folic acid; Food consumption; Food preferences; Free radicals; Histidine; Homogeneity; Lipids; Liposomes; Mechanical properties; Metabolism; Oxidative stress; Polymers; polymer–lipid interactions; Propylene; Propylene glycol; Scientists; Shelf life; Skin; Sodium carboxymethyl cellulose; Solubility; Storage stability; structural analysis; study of controlled releases; thermal stability; Vitamin B; Vomiting
• ISSN: 1438-7697; 1438-9312
• DOI: 10.1002/ejlt.202200169

Liposome‐encapsulated folic acid is incorporated into the films made from sodium carboxymethyl cellulose (CMC) (2 mas%) and a mixture of CMC and solagum (9:1 w/w) using the film‐forming cast solution method. Histidine is used to increase solubility for folic acid in liposomes (1–5 mg mL−1), and propylene glycol is used as a film plasticizer (2.6 mas%). The obtained films (50–60 µm tick) containing 3.12–20.19 mg of folic acid per gram of film are envisaged to be used as patches for transdermal delivery of folic acid. Therefore, some physical, mechanical, release and structural attributes of the films are scrutinized. Folic acid gives yellow color to the films and contributes to stronger chemical bonds which result in improved strength of the film. Liposomes prolong the release of folic acid from films to 24 h without adverse effects on mechanical properties of the films, but degrade homogeneity of the films, which can be ascribed to its agglomeration within the film matrix as revealed by atomic force microscopy. According to the release at pH 5.5, the film formulation based on a blend of CMC and solagum containing 3 mg mL−1 liposome‐encapsulated folic acid is recommended. Practical Application: Folic acid is effective in reducing oxidative stress levels in the skin and neutralizing the harmful free radicals and is also essential for various metabolic reactions in the body. However, the limited solubility of folic acid linked with its poor absorption in an organism, low storage stability, short half‐life upon oral consumption, specific food preferences of some people, extensive liver metabolism, and pregnancy‐induced vomiting point to a large potential in transdermal usage of folic acid. This has motivated us to design new multicomponent polymer‐lipid systems as an alternative solution to overcome some of these drawbacks. The results obtained for these multicomponent films pointed to their potential for prolonged release of folic acid to 24 h, which can also be useful for scientists interested in encapsulating similar poorly soluble compounds in CMC patches. The finding can be also valuable information for pharmaceutical manufacturers and scientists worldwide. The influence of folic acid‐loaded liposomes incorporated in the complex biopolymer film on the mechanical, release and morphological properties is investigated by the atomic force microscopy, in vitro diffusion tests and the technique which determines force‐displacement at the breaking point.