Characterization and Evaluation of 5-Fluorouracil-Loaded Solid Lipid Nanoparticles Prepared via a Temperature-Modulated Solidification Technique

Abstract

The aim of this research was to advance solid lipid nanoparticle (SLN) preparation methodology by preparing glyceryl monostearate (GMS) nanoparticles using a temperature-modulated solidification process. The technique was reproducible and prepared nanoparticles without the need of organic solvents. An anticancer agent, 5-fluorouracil (5-FU), was incorporated in the SLNs. The SLNs were characterized by particle size analysis, zeta potential analysis, differential scanning calorimetry (DSC), infrared spectroscopy, atomic force microscopy (AFM), transmission electron microscopy (TEM), drug encapsulation efficiency, in vitro drug release, and in vitro cell viability studies. Particle size of the SLN dispersion was below 100 nm, and that of redispersed lyophilizates was ~500 nm. DSC and infrared spectroscopy suggested that the degree of crystallinity did not decrease appreciably when compared to GMS. TEM and AFM images showed well-defined spherical to oval particles. The drug encapsulation efficiency was found to be approximately 46%. In vitro drug release studies showed that 80% of the encapsulated drug was released within 1 h. In vitro cell cultures were biocompatible with blank SLNs but demonstrated concentration-dependent changes in cell viability to 5-FU-loaded SLNs. The 5-FU-loaded SLNs can potentially be utilized in an anticancer drug delivery system.

Modified solid lipid nanoparticles encapsulated with Amphotericin B and Paromomycin: an effective oral combination against experimental murine visceral leishmaniasis

“…C-H stretching bands (718 & 1,457 cm −1 ) denoted the aliphatic side chain. No considerable differences in position, shape as well as the intensity of peaks related to GMS, was detected in comparison with PSLNs, DDSLNs spectra, indicating the solidification of lipid in the nanoparticles as a matrix having a similar arrangement to that of the original components 49 . The FTIR spectra of AmB showed distinctive peaks such as -OH stretch (3,438 cm −1 ), C=C bond (1558 cm −1 ) and NH 2 in-plane band (1634 cm −1 ) shown in Fig.…”

Effective use of nanocarriers as drug delivery systems for the treatment of selected tumors

“…All of these aspects of SLNs as anticancer drug carriers have been excellently reviewed by Wong et al 5 Few examples where SLN systems have been utilized for the delivery of anticancer drugs are docetaxel, 13 doxorubicin, 14 paclitaxel, 15 methotrexate 16 and 5-fluorouracil (5-FU). 17 …”

Influence of Various Process Variables and Formulation Excipients on the Engineering of Sertaconazole Solid Lipid Nanoparticles

“…Excess use of surfactant can interfere with loading properties of SLN [21]. As the concentration of OLMS increases from 2, 4 and 6 % w/v the particle size first decreases but remains stable for further rise in surfactant concentration.…”