Systemic delivery of alpha-asarone with Kolliphor HS 15 improves its safety and therapeutic effect on asthma

作者：Lu, Hua; Li, Jianbo; Li, Man; Gong, Tao^*; Zhang, Zhirong

来源：Drug Delivery, 2015, 22(3): 266-275.

DOI：10.3109/10717544.2014.889776

• Alpha-asarone
• anaphylaxis
• ARE solubilizing efficiency
• asthma
• Kolliphor HS 15
• pharmacokinetics
• polysorbate 80
• tissue distributions

The commercially available alpha-asarone injections (CA-ARE) were frequently found to cause severe anaphylactic reactions by the solubilizer contained in the formulation such as polysorbate 80 and propylene glycol. This study aimed to develop a new ARE injection using Kolliphor HS 15 as solubilizing agent (HS 15-ARE) by the dissolution method to resolve its poor solubility problem and reduce the anaphylaxis of CA-AREs caused by Polysorbate 80. The HS 15-ARE micelle showed a homogeneous round shape with the mean particle size of around 13.73 +/- 0.02 nm, polydisperse index (PDI) of 0.19 +/- 0.01 and solubilizing efficiency of 95.7% +/- 2.4%. In vitro and in vivo studies showed that HS 15-ARE is a stable injection presenting the same pharmacokinetic profile with CA-ARE. Moreover, improved therapeutic effect was observed for HS 15-ARE in treating asthma compared to CA-ARE (p<0.05) with no anaphylactic reactions observed. These results demonstrate that the new formulation of ARE (HS 15-ARE) has a great potential for replacing CA-AREs injections.

• 出版日期2015-5
• 单位四川大学