Study of pharmacokinetics and tissue distribution of liposomal brucine for dermal administration

Abstract

Bai-Can Yang1, Zhi-Feng Chu1, Sha Zhu1, Li-Jun Wang1, Yu-Hong Feng1, Feng-Hua Li1, Chang-Sheng Liu2, Yuan Yuan21Pharmacy Department of Traditional Chinese Medicine, Shanghai University of Traditional Chinese Medicine, Shanghai, People’s Republic of China; 2Key Laboratory for Ultrafine Materials of Ministry of Education, and Engineering Research Center for Biomedical Materials of Ministry of Education, East China University of Science and Technology, Shanghai, People’s Republic of ChinaObjective: To evaluate the pharmacokinetics and tissue distribution of liposomal brucine (LB) for dermal application.Methods: Pharmacokinetics and tissue distribution were studied by in vivo animal testing. High performance liquid chromatography (HPLC) was used to detect the concentration of brucine in rats’ skin, plasma and various tissues.Results: After dermal administration, LB was absorbed rapidly in the skin and could be detected after 0.5 hours. After 36 hours, levels were too low to be detected. In plasma, levels were also too low to be detected after 36 hours. The concentration of LB reached 50% of the maximum in all tissues except the brain, peaking after 1.5 hours but still detectable after 12 hours.Conclusion: The concentration of LB was high in skin at the application site. LB was quickly absorbed into tissues through the blood circulation and widely distributed throughout the whole body. There was no obvious toxicity and LB did not readily accumulate in tissues and organs. It showed local potency but low overall systemic toxicity.Keywords: liposomal brucine, dermal administration, pharmacokinetics, tissue distribution