title: Preparation, characterization and cytotoxicity evaluation of tanshinone IIA nanoemulsions.
abstract: Tanshinone IIA (TA) is a major active component of Danshen (Salvia miltiorrhiza bunge), a well-known traditional Chinese medicine. In this paper, we describe an optimal method for preparing TA nanoemulsions (TA-NEs) to solve the problems of TA's poor solubility in water and insufficient dissolution rate. Optimization of the method for preparing nanoemulsions of lipid soluble TA by emulsification/high pressure homogenization was carried out with a 2(3) factorial design, using Tween 80, lecithin and water content as independent variables. The particle size, entrapment efficiency and polydispersity index of eight formulations were then evaluated. Two optimal formulations, TA-NE-F2 and TA-NE-F4, were developed and both exhibited markedly enhanced in vitro release ability, as compared to TA. However, only TA-NE-F4 remained stable for over 3 months. TA-NE-F4 particles were spherical and intact, with a mean particle size of 95.6 nm and a high entrapment efficiency of 99.3%, TA-NE-F4 showed a fast dissolution rate of 80% in 10 min and 100% in 20 min. The cytotoxicity of TA-NE-F4 against T24 human bladder cancer cells was 103.4-fold greater than TA alone in both a time- and a dose-dependent manner. Overall, we describe a feasible method for preparing TA-NEs that exhibit potent cytotoxicity.
authors.affiliation: Department of Occupational Therapy, I-Shou University, Kaohsiung 82445, Taiwan.
authors.forename: Li-Ching
authors.initials: LC
authors.lastname: Chang
authors.forename: Chi-Lien
authors.initials: CL
authors.lastname: Wu
authors.forename: Ching-Wen
authors.initials: CW
authors.lastname: Liu
authors.forename: Wen-Ho
authors.initials: WH
authors.lastname: Chuo
authors.forename: Ping-Chia
authors.initials: PC
authors.lastname: Li
authors.forename: Tong-Rong
authors.initials: TR
authors.lastname: Tsai
mesh_terms: D045784:Abietanes / Q000008:administration & dosage* / Q000302:isolation & purification / Q000494:pharmacology; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D004355:Drug Stability; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage / Q000302:isolation & purification / Q000494:pharmacology; D004655:Emulsions; D005079:Excipients; D006801:Humans; D053758:Nanoparticles / Q000008:administration & dosage / Q000648:ultrastructure; D036103:Nanotechnology; D010316:Particle Size; D012995:Solubility; D013501:Surface-Active Agents; D001749:Urinary Bladder Neoplasms / Q000188:drug therapy / Q000473:pathology
chemical_list: D045784:Abietanes; D004365:Drugs, Chinese Herbal; D004655:Emulsions; D005079:Excipients; D013501:Surface-Active Agents; C021751:tanshinone