Preparation, characterization, and optimization of primaquine-loaded solid lipid nanoparticles

Abstract

Primaquine (PQ) is one of the most widely used antimalarial drugs and is the only available drug that combats the relapsing form of malaria. PQ use in higher doses is limited by severe tissue toxicity including hematological- and gastrointestinal-related side effects. Nanoformulation of drugs in an appropriate drug carrier system has been extensively studied and shown to have the potential to improve bioavailability, thereby enhancing activity, reducing dose frequency, and subsequently reducing toxicity. The aim of this work was to design, synthesize, and characterize PQ-loaded solid lipid nanoparticles (SLNs) (PQ-SLNs) as a potential drug-delivery system. SLNs were prepared by a modified solvent emulsification evaporation method based on a water-in-oil-in-water (w/o/w) double emulsion. The mean particle size, zeta potential, drug loading, and encapsulation efficiency of the PQ-SLNs were 236 nm, +23 mV, 14%, and 75%, respectively. The zeta potential of the SLNs changed dramatically, from −6.54 mV to +23.0 mV, by binding positively charged chitosan as surface modifier. A spherical morphology of PQ-SLNs was seen by scanning electron microscope. In vitro, release profile depicted a steady drug release over 72 hours. Differential scanning calorimeter thermograms demonstrated presence of drug in drug-loaded nanoparticles along with disappearance of decomposition exotherms, suggesting increased physical stability of drug in prepared formulations. Negligible changes in characteristic peaks of drug in Fourier transform infrared spectra indicated absence of any interaction among the various components entrapped in the nanoparticle formulation. The nanoformulated PQ was 20% more effective as compared with conventional oral dose when tested in Plasmodium berghei -infected Swiss albino mice. This study demonstrated an efficient method of forming a nanomedicine delivery system for antimalarial drugs.

Spanish olive leaf extract‐loaded nanostructured lipid carriers: Production and physicochemical characterization by Zetasizer, FT‐IR, DTA/TGA, FE‐SEM and XRD

“…Also, at the end of the test, about 4%-5% of the ash was remained and the rest of the ingredients were completely decomposed. These results are consistent with the results reported in the literature (Ismail et al, 2014;Omwoyo et al, 2014;Prabhu et al, 2015;Rafi Shaik et al, 2017).…”

Comparative Study of Glyceryl Behenate or Polyoxyethylene 40 Stearate-Based Lipid Carriers for Trans-Resveratrol Delivery: Development, Characterization and Evaluation of the In Vitro Tyrosinase Inhibition

“…TGA analysis is used for nanoparticle characterization and indicates degradation behavior of formulations [38]. Herein, we found that RSV has undergone thermal degradation after approximately 250°C, similarly to previous observations [39].…”

General Perception of Liposomes: Formation, Manufacturing and Applications

“…DSC and XRD are complementary techniques that evaluate the thermal behavior and crystallinity, respectively, and provide valuable information for characterization of loaded liposomes [46,51,52]. DSC evaluates the differences in heat flow (electric power) between a sample and a reference.…”

“…The heat flow curve provides the respective transition temperature and enthalpy, which allows to identify the nature of thermal events: endo-or exothermic [53][54][55]. DSC represents the most useful thermal analysis technique in the study of lipid-based materials [46,52,[54][55][56].…”

“…Functionalized liposomes labeled with radioisotopes can also be used as molecular probes in nuclear imaging. For instance, liposomes labeled with 64 Cu, 18 F, 89 Zr or 52 Mn have been reported in positron emission tomography while 99m TC, 111 In or 67 Ga labeled liposomes were applied in single photon emission computed tomography. Acoustic liposomes which are liposomes made of perfluoropropane gas can be used as contrast agents in ultrasound imaging technique.…”