title: Optimized mixed oils remarkably reduce the amount of surfactants in microemulsions without affecting oral bioavailability of ibuprofen by simultaneously enlarging microemulsion areas and enhancing drug solubility.
abstract: The toxicity and irritation associated with high amounts of surfactants restrict the extensive utilization of microemulsions. To address these shortcomings, employing mixed oils to enlarge microemulsion areas therefore reducing surfactant contents is a promising strategy. However, what kinds of mixed oils are more efficient in enlarging microemulsion areas still remains unclear. In this research, we found that the chain length and degree of unsaturation of oils play a key role in enlarging microemulsion areas. The combination of moderate chain saturated oil caprylic/capric triglyceride (GTCC) with long chain unsaturated oil glycerol trioleate significantly increased the microemulsion areas. Solubility of ibuprofen in the mixed oils was unexpectedly and remarkably increased (almost 300mg/mL) compared with that (around 100mg/mL) of the single oil (GTCC), which also resulted in greatly increased solubility of ibuprofen in mixed oils-containing microemulsions. By optimizing the mixed oil formulation, the absolute amount of surfactant in drug-loaded microemulsions was reduced but increased drug oral bioavailability in rats was maintained. It could be concluded that the combined use of moderate chain oils and long chain unsaturated oils could not only acquire enlarged microemulsion areas but also enhanced drug solubility, therefore doubly reducing surfactant amount, which is extremely beneficial for developing safe microemulsions.
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, University Town, Guangzhou 510006, PR China.
authors.forename: Yizhen
authors.initials: Y
authors.lastname: Chen
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, University Town, Guangzhou 510006, PR China.
authors.forename: Jue
authors.initials: J
authors.lastname: Tuo
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, University Town, Guangzhou 510006, PR China.
authors.forename: Huizhi
authors.initials: H
authors.lastname: Huang
authors.affiliation: Guangzhou Cellprotek Pharmaceutical Co., Ltd., Science Park, Guangzhou 510663, PR China.
authors.forename: Dan
authors.initials: D
authors.lastname: Liu
authors.affiliation: School of Pharmacy, Fujian Medical University, Fuzhou 350108, PR China.
authors.forename: Xiuhua
authors.initials: X
authors.lastname: You
authors.affiliation: Department of Pharmacology, Zhongshan School of Medicine, Sun Yat-sen University, 74 Zhongshan II Road, Guangzhou 510080, PR China.
authors.forename: Jialuo
authors.initials: J
authors.lastname: Mai
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, University Town, Guangzhou 510006, PR China.
authors.forename: Jiaqi
authors.initials: J
authors.lastname: Song
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, University Town, Guangzhou 510006, PR China.
authors.forename: Yanqi
authors.initials: Y
authors.lastname: Xie
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, University Town, Guangzhou 510006, PR China.
authors.forename: Chuanbin
authors.initials: C
authors.lastname: Wu
authors.affiliation: School of Pharmaceutical Sciences, Sun Yat-sen University, University Town, Guangzhou 510006, PR China. Electronic address: lsshhy@mail.sysu.edu.cn.
authors.forename: Haiyan
authors.initials: H
authors.lastname: Hu
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D001682:Biological Availability; D002210:Caprylates / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D003652:Decanoic Acids / Q000737:chemistry; D004355:Drug Stability; D004553:Electric Conductivity; D004655:Emulsions / Q000737:chemistry*; D007052:Ibuprofen / Q000008:administration & dosage* / Q000493:pharmacokinetics*; D009821:Oils / Q000737:chemistry*; D010316:Particle Size; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013501:Surface-Active Agents / Q000737:chemistry*; D013535:Suspensions; D014280:Triglycerides / Q000737:chemistry
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D002210:Caprylates; D003652:Decanoic Acids; D004655:Emulsions; D009821:Oils; D013501:Surface-Active Agents; D013535:Suspensions; D014280:Triglycerides; C031071:decanoic acid; C031492:octanoic acid; D007052:Ibuprofen
keywords: Chain length; Drug solubility; Microemulsion areas; Mixed oils; Oral bioavailability; Unsaturated degrees