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Optimizing surfactant content to improve oral bioavailability of ibuprofen in microemulsions: just enough or more than enough?
Int J Pharm. 2014 Aug 25; 471(1-2):276-84.IJ

Abstract

Microemulsions show excellent potential as drug delivery systems, but the surfactants used to prepare them can cause side effects. Researchers have explored various strategies to expand microemulsion area and thereby reduce the surfactant content necessary, but how these strategies affect drug oral bioavailability has not been investigated in detail. Microemulsions were prepared using 16% or 24% mixed surfactant Tween 80-Cremophor EL-PEG400 (1:1:2) and either 6% caprylic/capric triglyceride oil (GTCC) or 6% or 15% mixed oil (Maisine™ 35-1 with GTCC). Some microemulsions contained just enough surfactant based on ternary phase diagrams, while others had excess surfactant. All empty and ibuprofen-loaded microemulsions were clear or translucent with a slight blue color, and they remained stable after dilution and centrifugation. In experiments with rats, oral bioavailability (AUC0⟶t) of ibuprofen in the microemulsions was similar for the different formulations (6779.0-7413.3 min μg/mL) and significantly higher than that of an ibuprofen suspension (4830.9 min μg/mL). The different formulations behaved similarly in a cellular uptake assay with Caco-2 cells. These results suggest that excess surfactant does not increase oral bioavailability or cellular uptake of ibuprofen. Therefore, to minimize side effects, using just enough surfactant to ensure microemulsion stability and drug solubility may be an appropriate strategy.

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.School of Pharmaceutical Sciences, Sun Yat-sen University, University Town, Guangzhou 510006, PR China.Pharmacy Department of Guangdong General Hospital, Guangdong Academy of Medical Sciences, Guangzhou 510080, PR China. Electronic address: zhaozengying@163.com.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

24858390

Citation

You, Xiuhua, et al. "Optimizing Surfactant Content to Improve Oral Bioavailability of Ibuprofen in Microemulsions: Just Enough or More Than Enough?" International Journal of Pharmaceutics, vol. 471, no. 1-2, 2014, pp. 276-84.
You X, Xing Q, Tuo J, et al. Optimizing surfactant content to improve oral bioavailability of ibuprofen in microemulsions: just enough or more than enough? Int J Pharm. 2014;471(1-2):276-84.
You, X., Xing, Q., Tuo, J., Song, W., Zeng, Y., & Hu, H. (2014). Optimizing surfactant content to improve oral bioavailability of ibuprofen in microemulsions: just enough or more than enough? International Journal of Pharmaceutics, 471(1-2), 276-84. https://doi.org/10.1016/j.ijpharm.2014.05.031
You X, et al. Optimizing Surfactant Content to Improve Oral Bioavailability of Ibuprofen in Microemulsions: Just Enough or More Than Enough. Int J Pharm. 2014 Aug 25;471(1-2):276-84. PubMed PMID: 24858390.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Optimizing surfactant content to improve oral bioavailability of ibuprofen in microemulsions: just enough or more than enough? AU - You,Xiuhua, AU - Xing,Qiao, AU - Tuo,Jue, AU - Song,Weijuan, AU - Zeng,Ying, AU - Hu,Haiyan, Y1 - 2014/05/22/ PY - 2014/03/11/received PY - 2014/04/22/revised PY - 2014/05/19/accepted PY - 2014/5/27/entrez PY - 2014/5/27/pubmed PY - 2015/2/20/medline KW - Cellular uptake KW - Microemulsions KW - Mixed oil KW - Oral bioavailability KW - Surfactant content SP - 276 EP - 84 JF - International journal of pharmaceutics JO - Int J Pharm VL - 471 IS - 1-2 N2 - Microemulsions show excellent potential as drug delivery systems, but the surfactants used to prepare them can cause side effects. Researchers have explored various strategies to expand microemulsion area and thereby reduce the surfactant content necessary, but how these strategies affect drug oral bioavailability has not been investigated in detail. Microemulsions were prepared using 16% or 24% mixed surfactant Tween 80-Cremophor EL-PEG400 (1:1:2) and either 6% caprylic/capric triglyceride oil (GTCC) or 6% or 15% mixed oil (Maisine™ 35-1 with GTCC). Some microemulsions contained just enough surfactant based on ternary phase diagrams, while others had excess surfactant. All empty and ibuprofen-loaded microemulsions were clear or translucent with a slight blue color, and they remained stable after dilution and centrifugation. In experiments with rats, oral bioavailability (AUC0⟶t) of ibuprofen in the microemulsions was similar for the different formulations (6779.0-7413.3 min μg/mL) and significantly higher than that of an ibuprofen suspension (4830.9 min μg/mL). The different formulations behaved similarly in a cellular uptake assay with Caco-2 cells. These results suggest that excess surfactant does not increase oral bioavailability or cellular uptake of ibuprofen. Therefore, to minimize side effects, using just enough surfactant to ensure microemulsion stability and drug solubility may be an appropriate strategy. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/24858390/Optimizing_surfactant_content_to_improve_oral_bioavailability_of_ibuprofen_in_microemulsions:_just_enough_or_more_than_enough L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(14)00371-8 DB - PRIME DP - Unbound Medicine ER -