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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.
Int J Pharm. 2015 Jun 20; 487(1-2):17-24.IJ

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+Show Affiliations

School of Pharmaceutical Sciences, Sun Yat-sen University, University Town, Guangzhou 510006, PR China.School of Pharmaceutical Sciences, Sun Yat-sen University, University Town, Guangzhou 510006, PR China.School of Pharmaceutical Sciences, Sun Yat-sen University, University Town, Guangzhou 510006, PR China.Guangzhou Cellprotek Pharmaceutical Co., Ltd., Science Park, Guangzhou 510663, PR China.School of Pharmacy, Fujian Medical University, Fuzhou 350108, PR China.Department of Pharmacology, Zhongshan School of Medicine, Sun Yat-sen University, 74 Zhongshan II Road, Guangzhou 510080, PR China.School of Pharmaceutical Sciences, Sun Yat-sen University, University Town, Guangzhou 510006, PR China.School of Pharmaceutical Sciences, Sun Yat-sen University, University Town, Guangzhou 510006, PR China.School of Pharmaceutical Sciences, Sun Yat-sen University, University Town, Guangzhou 510006, PR China.School of Pharmaceutical Sciences, Sun Yat-sen University, University Town, Guangzhou 510006, PR China. Electronic address: lsshhy@mail.sysu.edu.cn.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

25841571

Citation

Chen, Yizhen, et al. "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." International Journal of Pharmaceutics, vol. 487, no. 1-2, 2015, pp. 17-24.
Chen Y, Tuo J, Huang H, et al. 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. Int J Pharm. 2015;487(1-2):17-24.
Chen, Y., Tuo, J., Huang, H., Liu, D., You, X., Mai, J., Song, J., Xie, Y., Wu, C., & Hu, H. (2015). 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. International Journal of Pharmaceutics, 487(1-2), 17-24. https://doi.org/10.1016/j.ijpharm.2015.03.075
Chen Y, et al. 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. Int J Pharm. 2015 Jun 20;487(1-2):17-24. PubMed PMID: 25841571.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - 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. AU - Chen,Yizhen, AU - Tuo,Jue, AU - Huang,Huizhi, AU - Liu,Dan, AU - You,Xiuhua, AU - Mai,Jialuo, AU - Song,Jiaqi, AU - Xie,Yanqi, AU - Wu,Chuanbin, AU - Hu,Haiyan, Y1 - 2015/04/01/ PY - 2014/11/27/received PY - 2015/02/26/revised PY - 2015/03/26/accepted PY - 2015/4/6/entrez PY - 2015/4/7/pubmed PY - 2016/2/18/medline KW - Chain length KW - Drug solubility KW - Microemulsion areas KW - Mixed oils KW - Oral bioavailability KW - Unsaturated degrees SP - 17 EP - 24 JF - International journal of pharmaceutics JO - Int J Pharm VL - 487 IS - 1-2 N2 - 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. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/25841571/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_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(15)00302-6 DB - PRIME DP - Unbound Medicine ER -