Fatty acid acylated Fab‐fragments of antibodies to neurospecific proteins as carriers for neuroleptic targeted delivery in brain

Open Access
Publisher Website
Google Scholar
Abstract
A method for targeted delivery of neuroleptics from blood in brain based on using Fab‐fragments of antibodies to antigens of brain glia cells (acid gliofibrillar antigen and α2‐glycoprotein) is suggested. The essence of the technique is that the molecule of neuroleptic (trifluoperazine) is conjugated with Fab‐fragments of these antibodies. The conjugate thus obtained is modified by stearoylchloride in the system of Aerosol OT reversed micelles in octane. The study of the distribution of 125I‐labelled conjugates in the rat organism after intracordial introduction is performed. On the contrary to the nonmodified conjugates and conjugate, containing fatty acylated Fab‐fragments of antibodies, nonspecific to the rat brain, the conjugate of trifluoperazine with stearoylated Fab‐fragments of antibodies to neurospecific antigens accumulate in brain tissues. The drastic increase of the neuroleptic activity of trifluoperazine resulting from its coupling with stearoylated Fab‐fragments of antiglial antibodies is observed.