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

Abstract	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.
Authors	Hua Lu, Jianbo Li, Man Li, Tao Gong, Zhirong Zhang
Journal	Drug delivery (Drug Deliv) Vol. 22 Issue 3 Pg. 266-75 (May 2015) ISSN: 1521-0464 [Electronic] England
PMID	24580506 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	Allylbenzene Derivatives Anisoles Anti-Asthmatic Agents Kolliphor HS 15 Solvents Stearates asarone Polyethylene Glycols Histamine
Topics	Allylbenzene Derivatives Anaphylaxis (blood, chemically induced) Animals Anisoles (administration & dosage, adverse effects, blood, therapeutic use) Anti-Asthmatic Agents (administration & dosage, adverse effects, blood, therapeutic use) Asthma (blood, drug therapy) Biological Availability Cells, Cultured Chemistry, Pharmaceutical Disease Models, Animal Drug Stability Erythrocytes (drug effects) Guinea Pigs Hemolysis (drug effects) Histamine (blood) Injections, Intravenous Male Molecular Structure Particle Size Polyethylene Glycols (chemistry) Rats, Wistar Sheep Solvents (chemistry) Stearates (chemistry) Surface Properties Tissue Distribution

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