ABSTRACT
OBJECTIVE:To establish a method for the determination of drug loading and encapsulation efficiency of Epirubi-cin hydrochloride-sorafenib-loaded Polylactic Acid-glycolic Acid Polymer(PLGA)embolic microspheres. METHODS:HPLC meth-od was adopted to determine the contents of epirubicin hydrochloride and sorafenib in the preparation,and then drug loading and encapsulation efficiency were calculated by formula. The determination was performed on Phenomenex Luna 5u C8(2) 100A col-umn with mobile phase consisted of methanol-water(containing 0.05% trifluoroacetic acid and 0.14% dium dodecyl sulfate)(75:25,V/V)at the flow rate of 1.0 mL/min. The detection wavelength was set at 252 nm,and the column temperature was maintained at 25℃. The injection volume was 10μL. RESULTS:The linear ranges were 2.020-101.00μg/mL for epirubicin hydrochloride(r=0.9998)and 2.048-102.40 μg/mL for sorafenib(r=0.9997),respectively. The limits of quantification were 3.2970,2.5468 μg/mL, respectively. The detection limits were 0.9891,0.7641 μg/mL,respectively. RSDs of precision,stability and repeatability tests were all less than 2.0%. The recoveries were 96.41%-101.80%(RSD=1.64%,n=9),99.46%-101.45%(RSD=0.70%,n=9),re-spectively. Drug loading of two components in 3 batches of samples were no lower than 1.17%,encapsulation efficiency no lower than 58%. CONCLUSIONS:The method is simple,accurate,can be used to determine drug loading and encapsulation efficiency of Epirubicin hydrochloride-sorafenib PLGA embolic microspheres.
ABSTRACT
OBJECTIVE: To evaluate the stability of epirubicin hydrochloride solutions for clinical use prepared from three different formulations (one concentrated solution and two powders for injection). METHODS: Epirubicin hydrochloride in three formulations was dissolved or diluted in 0.9% sodium chloride to prepare the test solutions with concentration of 0.4mg · mL-1. These solutions were stored at different temperatures and under different shading circumstances, and samples were collected periodically during the storage to evaluate the stability, including visual inspection, pH value and content of epirubicin. RESULTS: All epirubicin solutions were stable when stored at 2-8°C under dark condition for 40 d with average content of greater than 93.76%. When stored atroom temperature with or without light exposure for 40 d, only the solution diluted from the concentrated water solution for injection was stable, as the average content remained above 92.57%. While the solutions prepared from the other two powders for injection were not stable, as the average content fell below 90% at room temperature after 2-7 d. CONCLUSION: Epirubicin solutions prepared from three different formulations are stable when stored either at 2-8°C under dark condition for 40 d or at room temperature for 24 h. The solution prepared from the concentrated water solution for injection is more stable than the solutions prepared from the two powders for injections when stored at room temperature for a long period (40 d).
ABSTRACT
OBJECTIVE:To prepare epirubicin hydrochloride solid lipid nanoparticle(EPI-SLN) and investigate its physicochemical property. METHODS: EPI-SLN was prepared by ultrasonic dispersion technique with glyceryl behenate as matrix,and the appearance,particle size,? electric potential,and entrapment efficiency of the SLN were evaluated and its stability at 3 month storing at 4 ℃ was investigated. RESULTS: EPI-SLN assumed spherical shape with a particle diameter of (212.8?6.2) nm,? electric potential of (-24.7?0.3) mV and entrapment efficiency of 82 %. The EPI-SLN at 4 ℃ was stable after storing for 3 months,showing no marked change in mean diameter,? electric potential or entrapment efficiency. CONCLUSION: The prepared EPI-SLN is up to the standard.