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Preparation and Evaluation of Oil-in-Water Self-Nanoemulsifying Systems with Potential for Pulmonary Delivery

Kalra, Ashish
http://rave.ohiolink.edu/etdc/view?acc_num=mco1364764383

Abstract Details

2013, Master of Science in Pharmaceutical Science (MSP), University of Toledo, College of Pharmacy.
Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) are mixtures of oil, surfactant and cosolvent/cosurfactant, which emulsify under conditions of gentle agitation. SNEDDS can drastically improve absorption of poorly water soluble drugs by keeping it in solubilized form at the site of absorption. The objective of the study was to develop a formulation to increase the solubility of poorly water soluble drugs and carbamazepine was selected as a model drug. The solubility of carbamazepine was tested in the formulation components. Formulation development and screening of oil-in-water nanoemulsions was done based on results obtained from an evaluation of self-emulsification time, phase diagram domains, and characteristics of resultant nanoemulsions. The optimized formulation was found to contain Cremophor RH 40 as the surfactant, PEG 400 as the co-surfactant and Labrafil M 2125 CS as the oil. Oil-in-water nanoemulsions were evaluated for clarity, precipitation, zeta potential, and droplet size distribution. Nanoemulsions were characterized using dynamic light scattering, electrophoretic light scattering, transmission electron microscopy and differential scanning calorimetry. The droplet size analysis was done using Dynamic Light Scattering (DLS) and Transmission Electron Microscopy (TEM). Nanoemulsions were nebulized into a mist using a commercial pediatric nebulizer and characterized using laser diffraction and transmission electron microscopy (TEM). An aseptic method was developed and validated for preparing sterile SNEDDS. The biocompatibility of the formulation was evaluated on NIH3T3 cell lines using MTT assay. SNEDDS were also loaded with a fluorescent dye (Sudan IV) in order to study its permeation characteristic through porcine lung tissue using histological analysis. Nanoemulsions showed a droplet size of less than 20 nm with a neutral zeta potential. Nebulized SNEDDS were able to retain the physiochemical properties of liquid SNEDDS. The mist showed a droplet size of less than 5 µm. Sterility testing and cell toxicity results validated that the method is capable of formulating microorganism free nanoemulsion that was biocompatible. In vitro permeability tests indicated penetration of oil droplets intracellularly through biological membranes. Thus SNEDDS developed in this study demonstrated good stability and has the potential to deliver poorly water soluble drugs.
Jerrry Nesamony, PhD (Committee Chair)
Sai Hanuman Sagar Boddu, PhD (Committee Member)
Surya M. Nauli, PhD (Committee Member)
140 p.
Pharmaceuticals; Pharmacy Sciences

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Citations

  • Kalra, A. (2013). Preparation and Evaluation of Oil-in-Water Self-Nanoemulsifying Systems with Potential for Pulmonary Delivery [Master's thesis, University of Toledo]. OhioLINK Electronic Theses and Dissertations Center. http://rave.ohiolink.edu/etdc/view?acc_num=mco1364764383

    APA Style (7th edition)

  • Kalra, Ashish. Preparation and Evaluation of Oil-in-Water Self-Nanoemulsifying Systems with Potential for Pulmonary Delivery. 2013. University of Toledo, Master's thesis. OhioLINK Electronic Theses and Dissertations Center, http://rave.ohiolink.edu/etdc/view?acc_num=mco1364764383.

    MLA Style (8th edition)

  • Kalra, Ashish. "Preparation and Evaluation of Oil-in-Water Self-Nanoemulsifying Systems with Potential for Pulmonary Delivery." Master's thesis, University of Toledo, 2013. http://rave.ohiolink.edu/etdc/view?acc_num=mco1364764383

    Chicago Manual of Style (17th edition)

mco1364764383
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This open access ETD is published by University of Toledo Health Science Campus and OhioLINK.