The pH-Dependent Controlled Release of Encapsulated Vitamin B₁ from Liposomal Nanocarrier

• Main Authors: Ádám Juhász, Ditta Ungor, Egon Z. Várkonyi, Norbert Varga, Edit Csapó
• Format: Article
• Language: English
• Published: MDPI AG 2021-09-01
• Series: International Journal of Molecular Sciences
• Subjects: asolectin; liposome; vitamin B₁; nanocarrier; encapsulation; pH-controlled release
• Online Access: https://www.mdpi.com/1422-0067/22/18/9851

In this work, we firstly presented a simple encapsulation method to prepare thiamine hydrochloride (vitamin B₁)-loaded asolectin-based liposomes with average hydrodynamic diameter of ca. 225 and 245 nm under physiological and acidic conditions, respectively. In addition to the optimization of the sonication and magnetic stirring times used for size regulation, the effect of the concentrations of both asolectin carrier and initial vitamin B₁ on the entrapment efficiency (EE %) was also investigated. Thermoanalytical measurements clearly demonstrated that after the successful encapsulation, only weak interactions were discovered between the carriers and the drug molecules. Moreover, the dissolution profiles under physiological (pH = 7.40) and gastric conditions (pH = 1.50) were also registered and the release profiles of our liposomal B₁ system were compared with the dissolution profile of the pure drug solution and a manufactured tablet containing thiamin hydrochloride as active ingredient. The release curves were evaluated by nonlinear fitting of six different kinetic models. The best goodness of fit, where the correlation coefficients in the case of all three systems were larger than 0.98, was reached by application of the well-known second-order kinetic model. Based on the evaluation, it was estimated that our liposomal nanocarrier system shows 4.5-fold and 1.5-fold larger drug retention compared to the unpackaged vitamin B₁ under physiological conditions and in artificial gastric juice, respectively.