Preparation and modification of capsaicin solid lipid nanoparticles / 中国药学杂志

OBJECTIVE: To prepare capsaicin-solid lipid nanoparticles (CAP-SLNs) and study their physical and chemical properties. Then, the CAP-SLNs were modified with chitosan (CTS) and the pharmacokinetics across colon of rats was studied in vivo. METHODS: CAP-SLNs were prepared by emulsion-solvent evaporation method. The mean size, encapsulation efficiency and drug loading of the nanoparticles were investigated. RESULTS: The average diameter of CAP-SLNs was (118.89 ±25.0) nm, the encapsulation efficiency was (38.56 ±2.6)%, and the drug-loading was (6.17 ±0.21)%. After colon-specific delivery in rats, the AUC0.360 min(243. 63 ±61.46) mg · min · L-1 and ρmax(1.23 ±0.18) mg · L-1 of CTS-CAP-SLNs were 1.81-fold and 1.95-fold higher than CAP. CONCLUSION: It is simple and feasible to prepare CAP-SLNs by emulsion-solvent evaporation method. The pharmacokinetic parameters in rats are improved remarkably compared with CAP.

Preparation of lappaconitine-loaded nanoparticles with polylactic acid and its release properties in vitro / 中国药学杂志

OBJECTIVE: To prepare lappaconitine (LA)-loaded polylactic acid (PLA) nanoparticles (LA/PLA NPs) and investigate its release properties in vitro. METHODS: LA/PLA NPs were prepared by optimized emulsion-solvent evaporation method with biodegradable PLA as carrier material and polyvinyl alcohol (PVA) as emulsifier. The entrapment efficiency and drug loading rate of LA were used as the main evaluation indexes to optimize the preparation process by orthogonal design method. The mean particle size was measured by laser particle size analyzer; the morphology of LA/PLA NPs was observed by atomic force microscope; the in vitro release behavior was studied by dynamic dialysis. RESULTS: The optimized LA/PLA NPs were spherical. The mean particle size was (429±9.19) nm, the entrapment efficiency and drug loading rate were (86.34±2.15)% and (45.85±1.34)%, respectively. The in vitro release study showed that the LA/PLA NPs could provide a continuous release of LA for 15 d. CONCLUSION: LA/PLA NPs with high entrapment efficiency and drug loading rate are prepared successfully, and show sustained release effect for LA in vitro.

Prepraration of PLGA-PLL-PEG Nanoparticles Simultaneously Loaded with Daunorubicin and Tetrandrine / 中国药学杂志

OBJECTIVE: To prepare PLGA-PLL-PEG nanoparticles simultaneously loaded with daunorubicin (DNR) and tetrandrine (Tet).

Preparation,optimization and characterization of NC-1900 loaded MePEG-PLA nanoparticles / 复旦学报（医学版）

Purpose To optimize the preparation of NC-1900 loaded MePEG-PLA nanoparticles (NPs). Methods MePEG-PLA copolymers of different molecular weight synthesized by solvent poly-merization method were used to prepare NC-1900 loaded MePEG-PLA NPs by double emulsion/solvent evaporation method.Orthogonal experimental design and multiple regressions were used to optimize the preparation method with nanoparticle size and NC-1900 encapsulation efficiency (EE) as res-ponse variables.NPs were characterized by particle size and Zeta potential detector and transmission electron microscope.The leakage of NC-1900 from NPs was evaluated by high-performance liquid chromatography (HPLC) detection. Results MePEG3000-PLA44800 NPs prepared according to the optimized conditions had a mean diameter of (77 ± 11) nm and EE of (21.4 ± 0.1) %.Only 5% and 15% of NC-1900 were leaked in pH 7.4 PBS and blank plasma at the end of 48 h,respectively. Conc-lusions The optimized MePEG3000-PLA44800 NPs is a favorable carrier for NC-1900.