OBJECTIVE:To prepare and characterize Fluorescent dye 1,1′-octacosyl-3,3,3′,3′-tetramethylindocarbocyanine iodide(DiR)-loading polyethylene glycol-poly lactic-co-glycolic acid(DiR-PEG-PLGA)nanocapsules,and to evaluate its biocompatibility in vitro. METHODS:Using PLGA and PEG-PLGA as carrier,DiR-PEG-PLGA nanocapsules were prepared by modified ultrasonic emulsification method. The particle size,Zeta potential,morphology,stability and fluorescence in vitro of nanocapsules were detected respectively. MTT assay was used to evaluate cytotoxicity in vitro of nanocapsules to human-derived HL7702 hepatocytes,and hemolysis test was carried out to investigate its hemolysis effects. RESULTS:Prepared DiR-PEG-PLGA nanocapsules were spherical with a clear core-shell structure. The average particle size was(507.53 ± 7.87)nm,polydispersity coetficient of particle size was 0.306 1±0.001 5 and Zeta potential was(-35.20±0.92)mV with good stability within 6 months under 4℃. Fluorescence signal intensity(y)of nanocapsules was increased linearly with DiR mass concentration(x)in vitro. The linear eguation was y=0.345 2x+0.433 4(R2=0.997 3).The toxicity of nanocapsules to HL7702 cells was between 0-1 degree,and no hemolytic effect was observed. CONCLUSIONS:The study successfully prepare fluorescent DiR-PEG-PLGA nanocapsules with high biocompatibility in vitro,which is further expected to become a safe optical drug carrier.

Swertia patens Burk. is a commonly used herbal medicine of the Yi nationality in Yunnan, China. It is widely used in the treatment of children with spastic abdominal pain, cholecystitis, and other diseases, mainly containing iridoid glycosides and ketone compounds. The highest and most significant pharmacological activity, with antispasmodic, analgesic, sedative, anti-inflammatory, liver-protecting, stomach-protecting, and other effects, is closely related to its effects of soothing the liver, clearing heat, and relieving stomach pain. As a very distinctive pediatric folk medicine, the related quality standards of Swertia patens Burk. have not been perfected, and the development of preparations is relatively lagging.

Objective To optimize the preparation process of Swertia patens,Burk.standard decoction and establish its quality standard by using the quality by design(QbD)concept.Methods Critical Quality Attributes(CQAs)were predicted and analyzed according to the quality marker(Q-marker)theory of traditional Chinese medicine;Failure mode and effects analysis(FMEA)was used to screen critical process parameters(CPPs);The measurement method of key quality attributes was established;The extraction process was optimized by Box Behnken test after the preliminary range was determined according to the single factor test;The entropy method was used for comprehensive scoring;The design space was established and the optimal operation space for process validation was selected;Standard decoction of Swertia patens Burk in fifteen batches with different habitats were prepared with the best technology,and the quality standards for the extraction rate,extract,thin layer chromatography,fingerprint,content,and the content transfer rate were established finally.Results The key quality attributes were swertiamarin content,gentiopicrin content,and paste yield;The key process parameters were soaking time,water amount,and decocting time;The established model had statistical significance;The optimum conditions were as follows:soaking time 90 min,adding water 15 times,decocting time 30 min(second decocting 20 min);The paste yield was 21.13％-30.73％;The extract was 82.00％-88.00％;The spot of swertiamarin was clear in TLC;The similarity between each samples in 15 batches and reference atlas were＞0.85％;The content of swertiamarin was 250.64-385.21 mg·g-1,and the transfer rate was 43.76％-77.73％;The content of gentiopicrin was 0.69-2.70 mg·g-1,and the transfer rate was 56.02％-105.29％.Conclusion Based on the above methods and techniques,the preparation process of Swertia patens Burk.The standard decoction was screened,which provides a reference for the preparation development and quality control of its formula granules.