Development and characterization of lecithin stabilized glibenclamide nanocrystals for enhanced solubility and drug delivery

Abstract

Novel LNCs (lipid nanocrystals) were developed with an aim to improve the solubility, stability and targeting efficiency of the model drug glibenclamide (GLB). PEG 20000, Tween 80 and soybean lecithin were used as polymer, surfactant and complexing agent, respectively. GLB nanocrystals (NCs) were prepared by precipitation process and complexed using hot and cold melt technique. The LNCs were evaluated by drug loading, saturation solubility (SL), optical clarity, in vitro dissolution, solid state characterization, in vivo and stability analysis. LNCs exhibited a threefold increase in SL and a higher dissolution rate than GLB. The percentage dissolution efficiency was found to decrease with increase in PEG 20000. The average particle size was in the range of 155-842 nm and zeta potential values tend to increase after complexation. X-ray powder diffractometry and differential scanning calorimetry results proved the crystallinity prevailed in the samples. Spherical shaped particles (51000 nm) with a lipid coat on the surface were observed in scanning electron microscopy analysis. Fourier transform infrared results proved the absence of interaction between drug and polymer and stability study findings proved that LNCs were stable. In vivo study findings showed a decrease in drug concentration to pancreas in male Wistar rats. It can be concluded that LNCs are could offer enhanced solubility, dissolution rate and stability for poorly water soluble drugs. The targeting efficiency of LNCs was decreased and further membrane permeability studies ought to be carried out.

Enhancing efficacy of gemcitabine in pancreatic patient-derived xenograft mouse models

“…The mixture was vortexed intermittently until soy lecithin was dissolved completely followed by addition of 240 mg 4NSG to soy lecithin solution. The mixture was sonicated until 4NSG dispersed completely in the solution ( Kumar et al, 2014 ; Zhang et al, 2018 ). Soybean lecithin is a basic substance of life, and it is a safe natural mixture of phospholipids ( Kumar et al, 2014 ).…”

“…The mixture was sonicated until 4NSG dispersed completely in the solution ( Kumar et al, 2014 ; Zhang et al, 2018 ). Soybean lecithin is a basic substance of life, and it is a safe natural mixture of phospholipids ( Kumar et al, 2014 ). It exhibits an amphiphilic structure which may be used as an inactive ingredient and its FDA approved.…”

In vivo synergistic anti-tumor effect of paclitaxel nanoparticles combined with radiotherapy on human cervical carcinoma

“…The most important aspect of these results was that the obtained size prevents nanoparticles renal filtration during circulation in the human body, thus increasing the blood circulation time and facilitating an effective and powerful targeting of the tumor through the EPR effect (Xu et al, 2015 ). In addition, although it was kept stable for a much shorter time (48 h) without any stabilizing agent compared to the study using soybean LEC for stabilization (Kumar et al, 2014 ), the lyophilized nanoparticles could be homogeneously and stably dissolved, as previously reported (Wu et al, 2014 ), ensuring the best solubility into the blood and on the same time, and they were more suitable for storage and large-scale production.…”

Stabilizing Agents for Drug Nanocrystals: Effect on Bioavailability

“…Poloxamers are synthetic polymers consisting of a series of closely related block copolymers of ethylene oxide and propylene oxide [ 18 , 25 , 26 ]. Poloxamers have been explored and applied in the field of pharmacy and biomedicine as thermo-sensitive hydrogels, nanoparticle and micelle carriers, particle surface coatings, and tissue scaffolds [ 27 , 28 ].…”