Back to Search Start Over

Solid lipid nanoparticles loaded with lipoyl–memantine codrug: Preparation and characterization

Solid lipid nanoparticles loaded with lipoyl–memantine codrug: Preparation and characterization

Authors :
Fatime Geyikoglu
Erika Fornasari
Ivana Cacciatore
Sara Laserra
Piera Sozio
Antonio Di Stefano
Michele Ciulla
Lisa Marinelli
Abdul Basit
Hasan Turkez
Source :
International Journal of Pharmaceutics. 485:183-191
Publication Year :
2015
Publisher :
Elsevier BV, 2015.

Abstract

Solid lipid nanoparticles (SLNs) are considered very attractive drug-delivery systems (DDS) able to enhance the efficacy of some therapeutic agents in several pathologies difficult to treat in a conventional way. Starting from these evidences, this study describes the preparation, physicochemical characterization, release, and in vitro cytotoxicity of stealth SLNs as innovative approach to improve solubility and absorption through the gastrointestinal tract of lipoyl-memantine (LA-MEM), a potential anti-Alzheimer codrug. Physico-chemical properties of LA-MEM loaded SLNs have been intensively investigated. Differential scanning calorimetry (DSC) was used to clarify the state and crystalline structure of the formulation. The results obtained from particles size analysis, polydispersity (PDI), and zeta potential measurements allowed the identification of the optimized formulation, which was characterized by a drug-lipid ratio 1:5, an average intensity diameter of 170nm, a PDI of 0.072, a zeta potential of -33.8mV, and an entrapment efficiency of 88%. Moreover, in vitro stability and release studies in both simulated gastric fluid (SGF) and simulated intestinal fluid (SIF), and preliminary in vitro cytotoxicity studies revealed that LA-MEM loaded SLNs could represent potential candidate for an in vivo investigation as DDS for the brain since it resulted devoid of citotoxicity and able to release the free codrug.

Details

ISSN :
03785173
Volume :
485
Database :
OpenAIRE
Journal :
International Journal of Pharmaceutics
Accession number :
edsair.doi.dedup.....70eda9fe442b3ca5bacc11bbbe846f38
Full Text :
https://doi.org/10.1016/j.ijpharm.2015.03.001