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Solid lipid nanoparticles loaded with lipoyl–memantine codrug: Preparation and characterization
Solid lipid nanoparticles loaded with lipoyl–memantine codrug: Preparation and characterization
- 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.
- Subjects :
- Cell Survival
Chemistry, Pharmaceutical
Dispersity
Pharmaceutical Science
Nanotechnology
Mice
Differential scanning calorimetry
Drug Stability
Memantine
In vivo
Cell Line, Tumor
Solid lipid nanoparticle
Zeta potential
Animals
Humans
Technology, Pharmaceutical
Particle Size
Solubility
Drug Carriers
Gastric Juice
Calorimetry, Differential Scanning
Intestinal Secretions
Thioctic Acid
Codrug
Chemistry
Lipids
body regions
Kinetics
Oxidative Stress
Drug delivery
Biophysics
Nanoparticles
Crystallization
Excitatory Amino Acid Antagonists
Subjects
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