Solid lipid nanoparticles of stearic acid for the drug delivery of paliperidone

Abstract

ABSTRARTPaliperidone is an antipsychotic drug having poor water solubility and bioavailability. Solid lipid nanoparticles of stearic acid loaded with paliperidone was prepared to enhance the bioavailability. Spherical nanoparticles of stearic acid containing paliperidone was prepared with the surfactant, biz. Gelucire® 50/13 forming a stabilizing layer over the nanoparticles. Particle size of the SLNs was found to exponentially decrease with the increase in the surfactant concentration. Dynamic light scattering (DLS), transmission electron 10 microscopy (TEM) and atomic force microscopy (AFM) imaging revealed that the average particle size of SLNs was 230±30 nm. Fourier transform infra-red spectroscopy (FTIR), X-ray diffraction (XRD) and differential scanning calorimetry (DSC) analysis revealed that there was no chemical interaction between the ingredients of the SLNs. However, molecular dispersion of the paliperidone in the stearic acid matrix led to the reduction in crystallinity of stearic acid. The entrapment efficiency of paliperidone in the lipid was calculated as 42.4 (% w/w). The corresponding % drug loading was calculated as 4.1 (% w/w) of the total lipid content. Controlled 15 release pattern was observed in the invitro release kinetics studies. Invitro cell culture studies against RAW 264.7 murine macrophages revealed that the paliperidone loaded SLNs have some cytotoxicity. But the observed toxicity was not concentration dependent as there was at least 60 % viability of the cells in the concentration range of 30 -120 µg/ml.

Preparation and investigation of solid lipid nanoparticles for drug delivery

“…The reason for this may be that as the formulations were different to the other formulations that were used, lithocholic acid and Pluronic F127 covered the surface of the particle rather than being introduced into the lipid matrix. Similar results have been seen in the literature where the surfactant shell and lipid core are melting at two different melting points by revealing two peaks[57,58]. Although, there is an individual melting peak attributed to Pluronic F127 (54 o C) which is compatible with literature[56], the presence of Pluronic F127 clearly reduces the melting point (Tmax) of the particle to 68 o C and 67 o C for SLNP1 and SLN11, respectively.…”

Computational Modeling of the Interaction of Silver Nanoparticles with the Lipid Layer of the Skin

“…is was favorable because it improved bioavailability, as previously demonstrated by Kumar and Randhawa [23].…”

A Eutectic Mixture of Natural Fatty Acids Can Serve as the Gating Material for Near‐Infrared‐Triggered Drug Release

“…Considering the limited types of natural fatty acids, it is difficult to obtain PCMs with melting points close to the physiological temperature of human bodies (37 °C). [14] In addition, pure saturated fatty acids tend to crystallize upon cooling from a melt; the encapsulated drugs are thus prone to exclusion from the hydrophobic core, generating a drug-rich outer layer and thus undesired burst release. [15] To circumvent these drawbacks, a eutectic mixture of two (or even more) fatty acids, with a melting point lower than that of either of its components, can be used to extend the available melting points and, at the same time, alter the crystallization behavior of single-component fatty acids to increase the drug loading capacity.…”