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Preparation and evaluation of ibuprofen-loaded microemulsion for improvement of oral bioavailability.
Drug Deliv. 2011 Jan; 18(1):90-5.DD

Abstract

The purpose of the current study was to improve the solubility of ibuprofen, a poorly water-soluble drug, in a microemulsion system that is suitable for oral administration. Microemulsion was prepared using different sorts of oils, surfactants, and co-surfactants. Pseudo-ternary phase diagrams were used to evaluate the microemulsion domain. The formulations were characterized by solubility of the drug in the vehicle, droplet size, and drug release. The optimal formulation consists of 17% Labrafil M 1944CS, 28% Cremophor RH40/Transcutol P (3:1, w/w), and 55% water, with a maximum solubility of ibuprofen up to 60.3 mg/ml. The mean droplet size of microemulsion was 57 nm. The pharmacokinetic study of microemulsion was performed in rats and compared with granule formulation. The microemulsion has significantly increased the C(max) and area under the curve (AUC) compared to that of the granule (p < 0.05). The relative bioavailability of ibuprofen in microemulsions was 1.9-fold higher than that of the granule. These results indicated that this novel microemulsion is a useful formulation for enhancing the oral bioavailability of ibuprofen.

Authors+Show Affiliations

School of Pharmaceutical Sciences, Hebei University, Baoding 071002, PR China. hbupharm@126.comNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

20942639

Citation

Hu, Liandong, et al. "Preparation and Evaluation of Ibuprofen-loaded Microemulsion for Improvement of Oral Bioavailability." Drug Delivery, vol. 18, no. 1, 2011, pp. 90-5.
Hu L, Yang J, Liu W, et al. Preparation and evaluation of ibuprofen-loaded microemulsion for improvement of oral bioavailability. Drug Deliv. 2011;18(1):90-5.
Hu, L., Yang, J., Liu, W., & Li, L. (2011). Preparation and evaluation of ibuprofen-loaded microemulsion for improvement of oral bioavailability. Drug Delivery, 18(1), 90-5. https://doi.org/10.3109/10717544.2010.522613
Hu L, et al. Preparation and Evaluation of Ibuprofen-loaded Microemulsion for Improvement of Oral Bioavailability. Drug Deliv. 2011;18(1):90-5. PubMed PMID: 20942639.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Preparation and evaluation of ibuprofen-loaded microemulsion for improvement of oral bioavailability. AU - Hu,Liandong, AU - Yang,Jianxue, AU - Liu,Wei, AU - Li,Li, Y1 - 2010/10/13/ PY - 2010/10/15/entrez PY - 2010/10/15/pubmed PY - 2011/3/18/medline SP - 90 EP - 5 JF - Drug delivery JO - Drug Deliv VL - 18 IS - 1 N2 - The purpose of the current study was to improve the solubility of ibuprofen, a poorly water-soluble drug, in a microemulsion system that is suitable for oral administration. Microemulsion was prepared using different sorts of oils, surfactants, and co-surfactants. Pseudo-ternary phase diagrams were used to evaluate the microemulsion domain. The formulations were characterized by solubility of the drug in the vehicle, droplet size, and drug release. The optimal formulation consists of 17% Labrafil M 1944CS, 28% Cremophor RH40/Transcutol P (3:1, w/w), and 55% water, with a maximum solubility of ibuprofen up to 60.3 mg/ml. The mean droplet size of microemulsion was 57 nm. The pharmacokinetic study of microemulsion was performed in rats and compared with granule formulation. The microemulsion has significantly increased the C(max) and area under the curve (AUC) compared to that of the granule (p < 0.05). The relative bioavailability of ibuprofen in microemulsions was 1.9-fold higher than that of the granule. These results indicated that this novel microemulsion is a useful formulation for enhancing the oral bioavailability of ibuprofen. SN - 1521-0464 UR - https://www.unboundmedicine.com/medline/citation/20942639/Preparation_and_evaluation_of_ibuprofen_loaded_microemulsion_for_improvement_of_oral_bioavailability_ L2 - https://www.tandfonline.com/doi/full/10.3109/10717544.2010.522613 DB - PRIME DP - Unbound Medicine ER -