Topical formulations for disease treatment
Israel, Bridg'ette Beatrice
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Purpose: Develop a bioadhesive formulation for the treatment of aquatic life with skin lesions or abrasions. The purpose of the second research project is to develop novel mutual prodrugs (MP) which couple n-acetyl-glucosamine with NSAID, either ketoprofen or ibuprofen. These mutual prodrugs are designed to aid in the treatment of osteoarthritis. Lastly, the transdermal permeability of N-Acetyl-D-Glucosamine is evaluated for the development of the mutual prodrug. Methods: For research project one, oleaginous gels were prepared and their viscosity measurements were taken with a rheometer to gain information pertaining to the bioadhesive forces present in each formulation. The mutual prodrugs are synthesized for project two. One mutual prodrug links n-acetyl-glucosamine to ketoprofen and the other links n-acetyl-glucosamine to ibuprofen. N-Acetyl-D-Glucosamine solutions were prepared at different concentrations for the third project. Enhancing agents were also incorporated to evaluate their influence on permeability of N-Acetyl-D-Glucosamine. The Franz cell apparatus and High Performance Liquid Chromatography were utilized to collect and analyze samples, respectively. Results: The findings of project one are as follows, gels prepared with safflower oil and wheat germ oil demonstrated the greatest viscosity and perceived bioadhesion when compared to the other gels and all controls. The gel prepared with both safflower oil and wheat germ oil provided the largest inhibition zone. The structure of the oil may be important since both safflower oil and wheat germ oil contain linoleic and linolenic acids, whereas olive oil contains mostly oleic acid. Permeability studies, of project two, show that the ketoprofen mutual prodrug permeates shed snakeskin more than three times greater than either ibuprofen derivative, while ethanol markedly increases the permeation for all three. It was determined, for project three, that the permeability coefficients of the phosphate buffer/ethanol solutions at 5%, 10%, and 25% were about threefold larger in value as those for saturated DMSO solution, whereas the 2% and 50% solution values were lower. Conclusion: The bioadhesive gel prepared with safflower oil showed greatest stickiness to chicken breast, greatest viscosity, and best antimicrobial release (for project one). It was concluded, from the results of project two, that the ketoprofen mutual prodrug appears the most likely candidate for transdermal administration; the ibuprofen mutual prodrugs for oral delivery; all three mutual prodrugs may be candidates for oral delivery or subcutaneous injection. The permeability coefficients calculated, during project three, supports the idea that phosphate buffer/ethanol solutions at 5%, 10%, and 25% are the optimal candidates for formulation while phosphate buffer/ethanol solutions at 2%, 50% contains too little ethanol and saturation has been reached, respectively.