Preparation of Oxcarbazepine Nanostructured Lipid Carriers and Their Physicochemical Properties / 中国药学杂志

OBJECTIVE: To prepare oxcarbazepine nanostructured lipid carriers (OXC-NLC), and investigate their physicochemical properties. METHODS: OXC-NLC was prepared by emulsification solvent evaporation method, and the optimum prescription was screened by orthogonal design. Scanning electron microscope was used to observe the morphology of OXC-NLC. Granulometer was applied to determine the particle size and distribution. DSC was adopted for phase analysis. RESULTS: OXC-NLC prepared under the optimum conditions was mostly spherical grains, with an average particle size of (63.04 ± 2.05) nm, which were distributed evenly, and the Zeta potential was (-33.52 ± 0.34) mV. DSC results indicated that the drug was dispersed in nanoparticles in an amorphous state, with entrapment efficiency of (98.16 ± 1.59)% and drug-loading capacity of (4.27 ± 0.70)%. The in vitro drug release was 27.31% in 8 h, which was followed by a sustained release. CONCLUSION: The prepared OXC-NLC has uniform particle size distribution, high encapsulation efficiency, and sustained release effect. This processing technology is simple, reliable, and highly reproducible.

Preparation and transdermal permeation of ropivacaine ethosomal gel in vitro / 中国药学杂志

OBJECTIVE: To prepare ropivacaine ethosomal gel and study its transdermal permeation. METHODS: The ropivacaine ethosomes were prepared by ethanol injection method. The formulation and the preparation method of ethosomes were optimized by orthogonal experiment. The particle size, morphology and encapsulation efficiency were evaluated, and the carbomer was added as the base for the preparation of the ethosomal gel. The penetration experiments of ropivacaine ethosomal gel through mouse skin were performed by Franz's cell. The cumulative penetration amount was calculated. RESULTS: The obtained ethosomes were approximately spherical, the size were (127.6±4.8) nm. The entrapment efficiency of ropivacaine in ethosomes was (77.58±1.07)%. Accumulative permeation amount of ropivacaine ethosomal gel within 24 h was 73.07 μg·cm-2, which was about 1.56 times of normal gel. CONCLUSION: The gel is feasible in preparation technique, controllable in quality and can significantly promote transdermal penetration of ropivacaine.