Preparation and acute toxicity test of Bruceae Fructus oil and β-cyclodextrin polymer inclusion complexes / 中草药

ABSTRACT

Objective: To prepare Bruceae Fructus oil (BFO) β-cyclodextrin polymer (CDP) inclusion complexes (BFO-CDP-IC), and investigate its safety by acute toxicity test. Methods: BFO was extracted and CDP was prepared according to the literature, the IC of BFO with CDP (BFO-CDP) was prepared by homogenizing method and characterized by SEM, 1H-NMR, and FT-IR. The optimum preparation process was determined by single factor test and L9(34) orthogonal test. Entrapment efficiency (EE) was determined by HPLC. Acute toxicity of BFO-CDP-IC was assessed by determining the number of deaths of ICR mice over gavage treatment for 2 weeks. The commercial emulsion of BFO (BFOE) was used as a reference. Results: The extraction rate of BFO was 17.3%, the yield of CDP was 49.26%, and the degree of crosslinking was 8.47. The optimal conditions for preparation were as follows, ratio of BFO and CDP was 110, preparation temperature and time was 20℃ and 6 min, the amount of ether was 0.5 g. Additionally, the HPLC data showed that drug loading of complexes was 7.1%, and EE was 80%. In the acute toxicity test, the median lethal dose (LD50) of BFOE was 9.78 g/kg. In contrast, all mice treated with IC survived even at the highest dosage (15.36 g/kg). Conclusion: The prepared BFO-IC has high EE compared with commercially available BFOE, BFO-CDP polymer significantly decreased toxicity of BFO.