The Synthesis of Tamoxifen-Loaded Albumin Nanoparticles by Homogenizers: Optimization and In Vitro Characterization Publisher



Safavi MS¹ ; Shojaosadati SA¹ ; Dorkoosh FA² ; Jo HJ³ ; Kwon Y³ ; Lee KC⁴ ; Yang HG⁵ ; Park EJ⁵ ; Na DH⁵
Source: Journal of Drug Delivery Science and Technology Published:2017

Abstract

The aim of this study was to develop mechanical homogenization processes to fabricate protein-based nanoparticles. The high-pressure homogenizer (HPH) and high-speed homogenizer (HSH); were used to encapsulate the hydrophobic drug, tamoxifen, in albumin nanoparticles. The results revealed that the rotational speed with HSH and the pressure with HPH were the main factors affecting the size, while increasing the residence time led to more homogenous nanoparticles. Seven homogenization cycles at 14917 psi and 8.24 min of mixing at 17360 rpm ensured a drug loading of 14.2 ± 1.9% and 11.6 ± 2.3% for HPH and HSH, respectively. We found a direct correlation between the obtained size and energy input and retention time with both homogenizing devices. The characteristics of the optimized nanoparticles were within the desired range to meet the requirements of intravenous injection. The surface morphology of the nanoparticles determined by transmission electron microscopy showed semi-spherical nanoparticle shapes. Further, the secondary structure of albumin in nanoparticles was determined via circular dichroism, which showed only slight structural changes versus native albumin, making it a promising, self-targeted drug delivery system. Finally, BT474 viability assays and western blot analysis showed the effectiveness of the tamoxifen-loaded albumin nanoparticles prepared via homogenization. © 2017 Elsevier B.V.