Preparation and In-Vitro Hematological Evaluation of Chlorambucil Loaded Lipid Nanoparticles Publisher



Sahib AS¹ ; Alhammid SNA² ; Akrami M³ ; Muhammed HA⁴ Show Affiliations
Source: International Journal of Drug Delivery Technology Published:2021

Abstract

Chlorambucil (CBL) is an orally administered anticancer drug currently utilized in the therapy of lymphomas, breast, and ovarian carcinomas. CBL was a candidate to be loaded inside lipid nanocarrier for parenteral administration to eliminate its serious adverse effects. Six formulas were prepared using the homogenization-ultrasonication method. Distearoyl phosphatidylethanolamine (DSPE) and soybean oil were the best lipids selected for CBL solubility and incorporation inside the nanoparticles. Poloxamer F68 ratio (1:2) relative to the total amount of lipids used and soy lecithin to surfactant ratio of 1:2 were the best ratios to get the best results of zeta potential (ZP), particle size (PS), and polydispersity index (PDI). Formula F5 was the best selected one with 85 ± 8 nm PS, 0.26 ± 0.01 PDI, and-35 ± 1.3 mV ZP. These results reveal an acceptable size for parenteral administration and good surface potential stability for colloidal dispersion. Drug entrapment efficiency (88.7 ± 3.7) and loading capacity (4.25 ± 0.03) were high concerning CBL solubility in the lipids. Particle morphology was studied by transmission electron microscopes (TEM), and appeared the spherical shape of the particle. Some erythrocyte hemolysis and high protein corona (34.59%) with plasma protein led to particle size enlargement to about 327 nm and decreased absolute ZP to about-28.5 mV. © 2021, Dr. Yashwant Research Labs Pvt. Ltd.. All rights reserved.