Transferrin-conjugated solid lipid nanoparticles for enhanced delivery of quinine dihydrochloride to the brain

摘要: Transferrin (Tf)-conjugated solid lipid nanoparticles (SLNs) were investigated for their ability to deliver quinine dihydrochloride the brain, management of cerebral malaria. SLNs prepared by an ethanol injection method using hydrogenated soya phosphatidyl choline (HSPC), triolein, cholesterol and distearylphosphatidylethanolamine (DSPE). Coupling with Tf was achieved incubation quinine-loaded in presence 1-ethyl-3-(3-dimethylaminopropyl) carbodiimide (EDC) hydrochloride phosphate buffered saline (pH 7.4) as a cross-linker. characterized shape, particle size, polydispersity percentage drug entrapment. The 108-126 nm maximum entrapment 38.4-42.7%. Average size increased on coupling but reduced. in-vitro release profile determined dialysis technique; non-conjugated released comparatively more than Tf-SLNs. Fluorescence studies revealed enhanced uptake Tf-SLNs brain tissue compared unconjugated SLNs. In in-vivo performance studies, plasma level distribution after intravenous administration drug-loaded that free drug. Intravenous solution resulted much higher concentrations serum Conjugation significantly which shown recovery dose from following Tf-coupled or solution.