ABSTRACT
This study establishes a quantitative analysis of multi-components by single marker (QAMS) method for the simultaneous determination of gallic acid, sodium danshensu, protocatechuic acid, protocatechuic aldehyde, vanillin, rosmarinic acid, salvianolic acid B, eugenol, cryptotanshinone and tanshinone IIA in Guanxinshutong capsules (Bambusae Concretio Silicea, Salvia miltiorrhiza, clove, borneol, Bambusae Concretio Silicea) by HPLC. Sample was loaded onto an Agilent C18 (ZORBAX Extend-RP C18, 250 mm × 4.6 mm, 5 µm) column and eluted with methanol-0.4% aqueous formic acid solution as a flow phase gradient, flow speed 1.0 mL·min-1, detection wavelength 280 nm, column temperature 35 ℃ and sample intake of 5 µL. Using protocatechuic acid as the internal reference, a relative correction factor was calculated and the durability was investigated, and the content of 10 components was calculated by QAMS and external standard method (ESM). The results show that the specificity, linear relationship, precision, repeatability, and stability of the 10 components were good. The average recovery was 98.20%-103.47% and RSD was 1.26%-2.84%. The relative positive factors and contents of the other nine components were calculated as gallic acid (0.759, 227.381), sodium tanshinol (3.630, 3.283), protocatechualdehyde (0.185, 0.150), vanillin (0.532, 65.213), rosmarinic acid (4.240, 1.035), salvianolic acid B (3.245, 18.204), eugenol (1.729, 9.265), cryptotanshinone (0.691, 1.449), and tanshinone ⅡA (0.702, 1.939). The results of QAMS were consistent with ESM analysis, and the relative error was between -3% and 3%. This method is stable and reliable, and can be used for the determination of 10 components in Guanxinshutong capsules.
ABSTRACT
OBJECTIVE: To prepare hyaluronic acid(HA)-modified breast cancer microenvironment respond nanoparticles and investigate their physicochemical properties as well as in vitro function. METHODS: The polymer HA-PASP was prepared by linking HA with polyaspartic acid (PASP) through a hydrazone bond. Polyethylene glycol (PEG) was used as contrast material for PEG-PASP. Using Doxorubicin(DOX) as a model drug, HA-PASP-NPs@DOX and PEG-PASP-NPs@DOX were prepared by dialysis method. Particle size, morphology and Zeta potential of nanoparticles were observed by particle size tester and transmission electron microscope (TEM). The physical and chemical properties of nanoparticles were evaluated including encapsulation efficiency, drug loading, stability and drug release ability. In vitro function was evaluated including breast cancer cell targeting and tumor microenvironmental response. RESULTS: HA-PASP-NPs@DOX was spherical and uniform, size was (143±21) nm and Zeta potential was (-27.8±3.8) mV, encapsulation efficiency was 28.3% and drug loading was 5.2%. Under pH 7.4, the structure of nanoparticles was stable for more than 30 d, but under pH 6.5 the drug release up to 96%. HA-PASP-NPs@DOX was targeted to MDA-MB-231 cells, which increased DOX uptake by tumor cells. CONCLUSION: The HA-PASP-NPs@DOX could be successfully prepared by dialysis method, which target breast cancer cells and release drugs efficiently in an acidic environment, what′s more, increase cytotoxicity activity.
ABSTRACT
Objective To optimize the formulation of paeonol nanostructured lipid carrier (NLC) thermosensitive in situ gel through Box-Behnken response surface method; To investigate its release properties in vitro to provide references for the study of transdermal drug delivery system. Methods Taking mass fraction of poloxamer 407 and poloxamer 188 as the factors, the gelling temperature as the index, the mathematical relationship between the gelling temperature and two factors was established by binomial model and multivariate linear regression model. The Box-Behnken response surface method was used to optimize the formulation of paeonol NLC thermosensitive in situ gel, and the in vitro release characteristics of the preparation was investigated. Results There was a credible quantitative relationship between the gelling temperature and the 2 factors, and the binomial model was more reliable than the multivariate linear model. The best prescriptions of paeonol NLC thermosensitive in situ gel were 22.90% poloxamer 407 and 3.34% poloxamer 188; gelling temperature was (33.4±0.1)℃, and the cumulative release amount of paeonol in situ gel in 24 h was 51.19%. Conclusion This method is suitable for the formulation optimization of paeonol NLC thermosensitive in-situ gel, and the established mathematical model has good predictability. The optimized formulation can provide references for the development of paeonol transdermal preparation.