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Formulations, hemolytic and pharmacokinetic studies on saikosaponin a and saikosaponin d compound liposomes. | LitMetric

AI Article Synopsis

  • - The study focused on creating a liposome formulation for saikosaponin A (SSa) and saikosaponin D (SSd) that minimizes hemolysis and improves bioavailability.
  • - Researchers used a combination of experimental designs to optimize the liposome's size, encapsulation efficiency, and hemolysis reduction, determining the best conditions for their formulation.
  • - Results showed that under optimal conditions, the liposome significantly enhanced the pharmacokinetic properties of both compounds, leading to better circulation time and overall effectiveness after intravenous administration.

Article Abstract

The aim of this study was to develop and optimise a saikosaponin a and saikosaponin d compound liposome (SSa-SSd-Lip) formulation with reduced hemolysis and enhanced bioavailability. A screening experiment was done with Plackett-Burman design, and response surface methodology of five factors (EPC/SSa-SSd ratio, EPC/Chol ratio, water temperature, pH of PBS, and ultrasound time) was employed to optimise the mean diameter, entrapment efficiency of SSa and SSd, and the reduction of hemolysis for SSa-SSd-Lip. Under the optimal process conditions (EPC/SSa-SSd ratio, EPC/Chol ratio, water temperature and pH of PBS were 26.71, 4, 50 °C and 7.4, respectively), the mean diameter, the entrapment efficiency of SSa, the entrapment efficiency of SSd and the hemolysis were 203 nm, 79.87%, 86.19%, 25.16% (SSa/SSd 12.5 mg/mL), respectively. The pharmacokinetic studies showed that the SSa-SSd-Lip had increased circulation time, decreased Cl, and increased AUC, MRT and T1/2β (p < 0.05) for both SSa and SSd after intravenous administration in comparison with solution.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272718PMC
http://dx.doi.org/10.3390/molecules20045889DOI Listing

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