ABSTRACT
Emodin nanostructured lipid carriers(ED-NLC) were prepared and their quality was evaluated in vitro. Based on the results of single-factor experiments, the ED-NLC formulation was optimized by Box-Behnken response surface method with the dosages of emodin, isopropyl myristate and poloxamer 188 as factors and the nanoparticle size, encapsulation efficiency and drug loading as evaluation indexes. Then the evaluation was performed on the morphology, size and in vitro release of the nanoparticles prepared by emulsification-ultrasonic dispersion method in line with the optimal formulation, i.e., 3.27 mg emodin, 148.68 mg isopropyl myristate and 173.48 mg poloxamer 188. Under a transmission electron microscope(TEM), ED-NLC were spherical and their particle size distribution was uniform. The particle size of ED-NLC was(97.02±1.55) nm, the polymer dispersion index 0.21±0.01, the zeta potential(-38.96±0.65) mV, the encapsulation efficiency 90.41%±0.56% and the drug loading 1.55%±0.01%. The results of differential scanning calorimeter(DSC) indicated that emodin may be encapsulated into the nanostructured lipid carriers in molecular or amorphous form. In vitro drug release had obvious characteristics of slow release, which accorded with the first-order drug release equation. The fitting model of Box-Behnken response surface methodology was proved accurate and reliable. The optimal formulation-based ED-NLC featured concentrated particle size distribution and high encapsulation efficiency, which laid a foundation for the follow-up study of ED-NLC in vivo.
Subject(s)
Drug Carriers , Emodin , Follow-Up Studies , Lipids , NanostructuresABSTRACT
Objective: A method for simultaneous determination of 10 active ingredients in Dahuang Lidan Tablets (DLP) by HPLC wavelength switching method was established, and its quality was evaluated by statistical analysis. Methods: A Phenomenex Kinetex C18 column was used with a column temperature of 30 ℃ and a mobile phase gradient of methanol-0.15% phosphoric acid. The flow rate was 1 mL/min and the detection wavelengths were 265.0 nm (0-5.8 min, gallic acid), 283.9 nm (5.8-7 min, 5-hydroxymethyl furfural), 222.2 nm (7-18 min, corilagin, p-hydroxybenzaldehyde), 256.7 nm (18-74 min, ellagic acid, aloe-emodin, rhein, emodin, chrysophanol, emodin methyl ether), respectively. Statistical analysis of the content of components in 10 batches of drugs was performed using SPSS 21 Software. Results: The linearity of 10 components in the respective mass concentration ranges was good (r > 0.998 0), the average sample recovery was in the range of 98.45%-100.12%, and the RSD was in the range of 0.80%-2.51%. The content of 10 components was as follow: gallic acid (8.371-11.438 mg/tablet), 5-hydroxymethylfurfural (0.046-0.087 mg/tablet), corilagin (0.721-2.094 mg/tablet), p-hydroxybenzaldehyde (0.034-0.065 mg/tablet), ellagic acid (1.736-1.996 mg/tablet), aloe-emodin (0.337-0.440 mg/tablet), rhein (1.636-2.562 mg/tablet), emodin (0.602-0.846 mg/tablet), chrysophanol (0.388-0.566 mg/tablet) and emodin methyl ether (0.621-0.781 mg/tablet). The quality of the 10 batches of samples was basically the same. Conclusion: This method is simple and accurate and can be used for the quality control of DLP.