title: Development, optimization and in vitro evaluation of norcantharidin loadedself-nanoemulsifying drug delivery systems (NCTD-SNEDDS).
abstract: This study focused on developing a self-nanoemulsifying drug delivery system (SNEDDS) containing bioactive surfactants under an efficient screening approach for overcoming problems associated with the delivery of norcantharidin (NCTD), a high dose chemotherapy agent having pH dependent solubility. Preliminary screening was implemented to select proper components combination. Besides the solubility of NCTD in the oil phase, emulsifying efficiency, droplet size and size distribution were also employed to select components of the SNEDDS. Moreover, the influence of surfactant and co-surfactant on the interfacial tension and droplets of nanoemulsions were investigated to further understand the mechanism of spontaneous emulsification. Co-surfactant addition promoted the emulsification via reducing the water/oil interfacial tension and viscosity. Ternary phase diagrams were constructed to investigate the phase behavior and designate the optimum systems. The alternative formulations were characterized for cloud point, dilution robustness, droplet size, polydispersity index (PDI) and transmission electron microscopy (TEM). In vitro dissolution study showed that the dissolution rate of optimized formulation (NCTD 10 mg/g, EO 50 wt.%, Cremophor EL 35 wt.%, ethylene glycol 15 wt.%) was slower than drug suspension under the same conditions, confirming that the developed SNEDDS formulation would exhibit sustained release potential.
authors.affiliation: a Key Laboratory of Plant Protection Resources and Pest Management, Ministry of Education , College of Plant Protection, Northwest A&F University , Yangling , China.
authors.forename: Liya
authors.initials: L
authors.lastname: Zeng
authors.affiliation: a Key Laboratory of Plant Protection Resources and Pest Management, Ministry of Education , College of Plant Protection, Northwest A&F University , Yangling , China.
authors.forename: Yalin
authors.initials: Y
authors.lastname: Zhang
mesh_terms: D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000008:administration & dosage* / Q000737:chemistry; D004339:Drug Compounding / Q000379:methods*; D016503:Drug Delivery Systems / Q000379:methods*; D065546:Drug Liberation; D004355:Drug Stability; D004655:Emulsions; D006863:Hydrogen-Ion Concentration; D053758:Nanoparticles / Q000737:chemistry*; D010316:Particle Size; D012995:Solubility; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry*; D013816:Thermodynamics
chemical_list: D019086:Bridged Bicyclo Compounds, Heterocyclic; D004655:Emulsions; D013501:Surface-Active Agents; C069741:norcantharidin
keywords: Nanoemulsion; interfacial tension; oral bioavailability; spontaneous emulsification; sustained release