Nanostructured lipid carriers for oral bioavailability enhancement of raloxifene: Design and in vivo study

Abstract

The objective of present work was to utilize potential of nanostructured lipid carriers (NLCs) for improvement in oral bioavailability of raloxifene hydrochloride (RLX). RLX loaded NLCs were prepared by solvent diffusion method using glyceryl monostearate and Capmul MCM C8 as solid lipid and liquid lipid, respectively. A full 3(2) factorial design was utilized to study the effect of two independent parameters namely solid lipid to liquid lipid ratio and concentration of stabilizer on the entrapment efficiency of prepared NLCs. The statistical evaluation confirmed pronounced improvement in entrapment efficiency when liquid lipid content in the formulation increased from 5% w/w to 15% w/w. Solid-state characterization studies (DSC and XRD) in optimized formulation NLC-8 revealed transformation of RLX from crystalline to amorphous form. Optimized formulation showed 32.50 ± 5.12 nm average particle size and -12.8 ± 3.2 mV zeta potential that impart good stability of NLCs dispersion. In vitro release study showed burst release for initial 8 h followed by sustained release up to 36 h. TEM study confirmed smooth surface discrete spherical nano sized particles. To draw final conclusion, in vivo pharmacokinetic study was carried out that showed 3.75-fold enhancements in bioavailability with optimized NLCs formulation than plain drug suspension. These results showed potential of NLCs for significant improvement in oral bioavailability of poorly soluble RLX.

Enhanced Lymphatic Uptake of Leflunomide Loaded Nanolipid Carrier via Chylomicron Formation for the Treatment of Rheumatoid Arthritis

“…Figure shows a complete solubilization of leflunomide in lipid matrix or transformation of leflunomide crystal to amorphous form that has been dispersed in the lipid matrix. 20 …”

Lymph cancer chemotherapy: delivery of doxorubicin-gemcitabine prodrug and vincristine by nanostructured lipid carriers

“…33 Drug (1 g of DOX-GEM and 0.5 g of VCR), Precirol ATO 5 (5 g), and injectable soya lecithin (10 g) were mixed in a 50 mL solvent mixture of ethanol and acetone (1:1, v/v) followed by bath sonication for 10 min. The obtained mixture was kept on a water bath maintained at 60°C to make a clear solution of lipids and drug in an organic solvent system.…”

Enhancing biopharmaceutical attributes of phospholipid complex-loaded nanostructured lipidic carriers of mangiferin: Systematic development, characterization and evaluation

“…Indeed, nanocarriers such as lipid micelles (Neuberg et al, 2015), solid lipid nanoparticles (Mukherjee et al, 2009;Bunjes, 2010), nanostructured lipidic carriers (NLCs) (Khan et al, 2015) and lipid nanocapsules (Sánchez-Moreno et al, 2012) have already been reported to hold immense promise for oral delivery of poorly water-soluble bioactives. Amongst these nanocarriers, the NLCs are considered to be of wider interest owing to their high drug-loading efficiency and drug stability (Naseri et al, 2015;Shah et al, 2016). Accordingly, the current work on the proposed novel technology was undertaken, wherein the PLCs of Mgf were incorporated into NLCs, for further enhancing the biopharmaceutical attributes.…”