Related Experiment Video
Updated: Aug 17, 2026

Solid Lipid Nanoparticles (SLNs) for Intracellular Targeting Applications
Published on: November 17, 2015
Benznidazole vs benznidazole in multilamellar liposomes: how different they interact with blood components?
Maria Jose Morilla1, Maria Jimena Prieto, Eder Lilia Romero
1Laboratorio de Diseño de Estrategias de Targeting de Drogas, Departamento de Ciencia y Tecnología, Universidad Nacional de Quilmes, Roque Saenz Peña 180, Bernal, 1876, Buenos Aires, Argentina.
Abstract:
In spite of its widespread use, benznidazole's (BNZ) toxicity and low efficacy remains as major drawbacks that impair successful treatments against Chagas disease. Previously, attempting to increase the selectivity and reduce its toxicity on infected tissues, multilamellar liposomes (MLV) composed of hydrogenated soybean phosphatidylcholine (HSPC): distearoyl-phosphatidylglycerol (DSPG): cholesterol (CHOL) 2:1:2 mol:mol loaded with BNZ (MLV-BNZ) were designed. In this work we compared different properties of MLV-BNZ with those of BNZ. Opposite to other hydrophobic drugs, the results indicated that slight changes of BNZ's association degree to proteins and lipoproteins should not modify the percentage of unbound drug available to exert pharmacological action. On the other hand, when loaded in MLV, BNZ reduced its association to plasma proteins in 45% and became refractory to the sinking effect of blood, dropping 4.5 folds. Additionally, when loaded in MLV, BNZ had higher volume distribution (160 +/- 20 vs 102 +/- 15 ml/kg) and total clearance (35.23 +/- 2.3 vs 21.9 +/- 1.4 ml/h.kg), and lower concentration-time curve (7.23 +/- 0.2 vs 9.16 +/- 0.5 microg.h/ml) than BNZ. Hence, these studies showed that for MLV-BNZ, the amount of BNZ can be substantially increased, from 25 to 70%, being this formulation more rapidly cleared from circulation than free drug; also due to the lower interaction with blood components, lower side effects can be expected.
Related Concept Videos
Bioavailability Enhancement: Drug Permeability Enhancement
Drug Binding to Blood Components
HSA is the most abundant plasma protein and is vital in drug binding. It contains distinct drug-binding sites, with different drugs exhibiting affinity for specific sites. There are three main drug-binding domains for HSA: sites I, II, and III. These domains are further...
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
Bioavailability: Influencing Factors
Modified-Release Drug Delivery Systems: Bioavailability
Drug Biotransformation: Overview

