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Development and Characterization of Oil-in-Water Nanoemulsions from Self-Microemulsifying Mixtures

Shah, Ishan
http://rave.ohiolink.edu/etdc/view?acc_num=mco1302134022

Abstract Details

2011, Master of Science in Pharmaceutical Science (MSP), University of Toledo, College of Pharmacy.
Self-Microemulsifying Drug Delivery Systems (SMEDDS) are isotropic mixtures of oil, surfactant and/or cosurfactants, and a drug that spontaneously forms an oil-in-water nanoemulsion upon gentle agitation with water. When dispersed in the gastrointestinal (GI) tract, the motility of stomach provides necessary agitation for emulsification. SMEDDS incorporated with a poorly water soluble drug demonstrates improved drug absorption since it maintains the drug in a solubilized state in the GIT tract. The purpose of this research was to screen lipid excipients for their self-microemulsification efficiency and to develop SMEDDS based formulation in liquid and solid forms using ibuprofen as a model drug. Excipients evaluated for SMEDDS were Tween 80 and Cremophor RH 40 as surfactants, Transcutol P, Capyrol 90 and PEG 400 as cosurfactants and Labrafac Lipophile WL 1349 (a medium chain triglyceride) as the oil. Self Microemulsifying (SME) mixtures containing various proportions of these components were tested for their self-microemulsification ability and were characterized by ternary phase diagrams. Based on these results, a particular mixture containing Tween 80-PEG 400-LL WL 1349 was selected and optimized for drug delivery purpose. Liquid SMEDDS was formulated by dissolving ibuprofen in the SME mixture. Solid SMEDDS was formulated by adsorbing Liquid SMEDDS onto an inert carrier Neusilin US2 by physical mixing. SMEDDS were analyzed for their droplet size and zeta potential. Solid state characterization of Solid SMEDDS was performed using scanning electron microscopy, differential scanning calorimetry and powder x-ray diffractometry. Finally, in vitro drug release studies were performed on Liquid and Solid SMEDDS and the results compared to plain ibuprofen dissolution. Ibuprofen was found to be physically and chemically stable in the SMEDDS and did not precipitate upon aqueous dilution. Solid and Liquid SMEDDS showed a droplet size of less than 50 nm and possessed a neutral zeta potential. Solid state characterization of Solid SMEDDS confirmed the presence of ibuprofen in a molecularly dissolved state in the formulation. In vitro drug release studies showed that 75 % of drug was released from Solid and Liquid SMEDDS within first five minutes of the dissolution time. A SMEDDS based dosage form was successfully developed and shows potential for application in the delivery of poorly water soluble drugs.
Jerry Nesamony, Ph.D. (Committee Chair)
Kenneth Alexander, Ph.D. (Committee Member)
Black Curtis, Pharm.D (Committee Member)
Sai Hanuman Sagar Boddu, Ph.D. (Committee Member)
113 p.
Pharmaceuticals
Lipids; Nanoemulsion; Oral delivery

Recommended Citations

Citations

  • Shah, I. (2011). Development and Characterization of Oil-in-Water Nanoemulsions from Self-Microemulsifying Mixtures [Master's thesis, University of Toledo]. OhioLINK Electronic Theses and Dissertations Center. http://rave.ohiolink.edu/etdc/view?acc_num=mco1302134022

    APA Style (7th edition)

  • Shah, Ishan. Development and Characterization of Oil-in-Water Nanoemulsions from Self-Microemulsifying Mixtures. 2011. University of Toledo, Master's thesis. OhioLINK Electronic Theses and Dissertations Center, http://rave.ohiolink.edu/etdc/view?acc_num=mco1302134022.

    MLA Style (8th edition)

  • Shah, Ishan. "Development and Characterization of Oil-in-Water Nanoemulsions from Self-Microemulsifying Mixtures." Master's thesis, University of Toledo, 2011. http://rave.ohiolink.edu/etdc/view?acc_num=mco1302134022

    Chicago Manual of Style (17th edition)

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This open access ETD is published by University of Toledo Health Science Campus and OhioLINK.