Nimodipine-loaded mixed micelles: formulation, compatibility, pharmacokinetics, and vascular irritability study

Abstract

Background:The clinical application of nimodipine (NIM) is limited by several unfavorable properties, which are induced by its low aqueous solubility. In the present study, nimodipineloaded egg phosphatidylcholine-sodium glycocholate mixed micelles (NIM-EPC-SGC-MMs) were prepared to improve the water solubility of NIM, thus allowing it to be more applicable for clinical use. Methods: NIM-EPC-SGC-MMs were prepared using the coprecipitation method and the factors influencing formulation quality were optimized. After formulation, water solubility, solubilizing efficiency, drug loading, particle size, physical compatibility, pharmacokinetics, and vascular irritability were determined. Results: The mean size of the NIM-EPC-SGC-MMs was 6.099 ± 0.048 nm under optimized conditions. The water solubility of NIM in EPC-SGC-MMs was enhanced 250-fold compared with free NIM. The physical compatibility, pharmacokinetic, and vascular irritability studies showed that, in comparison to the commercially available NIM injections, NIM-EPC-SGCMMs presented better physical compatibility, the same pharmacokinetic profile, and less risk of local vascular irritation and phlebitis. Conclusion: EPC-SGC-MMs represent a promising new formulation suitable for the intravenous delivery of NIM.

Mesoporous drug carrier systems for enhanced delivery rate of poorly water-soluble drug: nimodipine

“…In the recent decades, nanospheres [8-12, 15, 16, 18] or microspheres [11,13,14,17] were widely used as drug carriers. A few reports have been published on the use of liquid and solid microemulsions [19,20], solid dispersions [21][22][23] or drug-loaded type systems based on cyclodextrins [24][25][26] and lipid [27][28][29] or phospholipid micelles [30,31]. Nevertheless, all these systems have organic character, so are potentially sensitive to external factors such as temperature or pH, and can drastically change their properties under the effect of these factors [32].…”

Self-assembled nanoparticles based on chondroitin sulfate-deoxycholic acid conjugates for docetaxel delivery: Effect of degree of substitution of deoxycholic acid

“…Subsequently, the final solutions were centrifuged at 4000 rpm for 20 min, before being filtered through a 0.8 μm membrane to remove insoluble DTX. [34,35]. All experiments were repeated in triplicate.…”

Subcutaneously injected ivermectin-loaded mixed micelles: formulation, pharmacokinetics and local irritation study

“…On Day 14, the rest of the six animals were sacrificed. The obtained samples were washed immediately with saline and fixed in 4% paraformaldehyde for 48 h (Song et al, 2011). After dehydration, the samples were embedded in paraffin, cut into tissue sections and stained using hematoxylin and eosin.…”