RESUMO
Background: Recently, applications of albumin nanoparticles as drug delivery carriers have increased. Most toxicology studies have shown that surface chemistry and size of nanoparticles play an important role in biocompatibility and toxicity
Objectives: The effect of desolvating agents with different chemical properties on the size of synthesized HSA NPs was investigated
Materials and Methods: Acetone, ethanol, methanol, and acetonitrile were used to synthesize HSA NPs with controllable size by desolvation method. Scanning electron microscopy [SEM], dynamic light scattering [DLS], and circular dichroism [CD] were employed to characterize produced particles. Finally, the toxicity of HSA NPs synthesized under different conditions was evaluated on PC-12 cells
Results: The sizes of synthesized particles differed according to the different solvents used. The sizes were 275.3 nm, 155.3 nm, 100.11 nm, and 66.2 nm for acetonitrile, ethanol, acetone, and methanol, respectively. CD showed that larger NPs had more changes in the secondary structures. Finally, the toxicity monitored on the cultured PC-12 cells showed no significant toxic effect through treating with these NPs at different concentrations [0-500 micro g.mL[-1]]
Conclusions: The size of HSA NPs has a strong dependency on the desolvating agent. The mechanism in which the desolvating agent affects the size of HSA NPs is complex. Various factors such as dielectric constant, polarity, functional groups, and hydrogen bonding of the solvents have the potential to affect the size and structure of HSA NPs. CD analysis suggested that the solvent denaturing capability had a critical effect on the HSA particle size. The stronger denaturing capability of the solvent resulted in the larger HSA particle size
RESUMO
Background: Eptifibatide [Integrilin] is an intravenous [IV] peptide drug that selectively inhibits ligand binding to the platelet GP IIb/IIIa receptor. It is an efficient peptide drug, however has a short half-life. Therefore, antithrombotic agents like eptifibatide are required to become improved with a protected and targeted delivery system such as using nano-liposomes to the site of thrombus
Objectives: The goal in the present report was to optimize encapsulation efficiency of the eptifibatide into Arg-Gly-Asp [RGD]-modified nano-liposomes [RMNL]. As well, it was intended to evaluate the effect of sodium lauryl sulfate [SLS] on drug release
Materials and Methods: The effect of five independent variables including number of freeze/thawing cycles, concentration of eptifibatide, 1,2-distearoyl-sn-glycero-3-phosphocholine [DSPC], cholesterol, and dipalmitoyl-GRGDSPA peptide on drug entrapment efficiency [DEE] was investigated using response surface methodology [RSM]. The effect of different concentrations of SLS on encapsulation and drug release from RMNL was also investigated. The size and morphology of RMNL were characterized using transmission electron microscopy [TEM]
Results: The maximum DEE [38%] was obtained with 7 freeze/thawing cycles, 3.65 micro moL eptifibatide, 7 mM DSPC, 3 mM cholesterol, and 1 mM dipalmitoyl- GRGDSPApeptide. SLS has significantly increased the drug release from RMNL, although its effect on encapsulation efficiency was not significant
Conclusions: The optimization of the formulations for valuable and expensive peptide drugs is essential to have the maximum encapsulation efficiency and the minimum experiments