Design, Optimization and Characterization of Ibuprofen Microemulsions and Microemulsion-based Gels

Download or read book Design, Optimization and Characterization of Ibuprofen Microemulsions and Microemulsion-based Gels written by Sujata Pandey and published by . This book was released on 2020 with total page 54 pages. Available in PDF, EPUB and Kindle. Book excerpt: Transdermal and topical drug delivery has been used as an alternative approach to oral drug delivery due to the various benefits it offers, including avoidance of the hepatic first pass metabolism, improved patient compliance, sustained or controlled drug release, and enhanced delivery to local target tissues. However, the barrier function of the skin, especially the stratum corneum, is a major challenge of drug permeation. Many different formulation techniques and approaches have been studied for enhancing drug permeation into the skin. The use of chemical permeation enhancers and formulations approaches, such as microemulsions, are some of the effective techniques to increase drug permeation. This thesis work focused on the composition and microstructures of microemulsions for enhancing the dermal delivery of ibuprofen. The effect of the type and composition of microemulsions, and the type of permeation enhancers incorporated into the microemulsions on the permeation and release profile of ibuprofen were studied. Four microemulsions were formulated, which were selected based on the pseudo-ternary phase diagrams. Among the four microemulsions, in two microemulsions (F2 and F4), 2% Carbopol 940 was incorporated as a gelling agent to form a gel base. Although the water content of F1 and F2 - both containing oleyl alcohol as the penetration enhancer - was low compared to formulations containing Transcutol® (i.e., F3 and F4), a higher permeation was observed for F1 and F2. The results suggest that water content played an important role in the better permeation of F1 and F2. Specifically, the findings suggest that the role of water content in the formulation could be more crucial than other parameters depending upon the permeation enhancer used in the formulation. It could be that the performance of the permeation enhancer, Transcutol®, depended more upon the water content of the formulation compared to formulations rich in fatty acid derivatives. However, a detailed study with varying concentrations of water in the formulations is required to validate the findings. Transcutol® is an effective permeation enhancer but the water content of the formulation containing Transcutol® needs to be optimal to increase drug permeation. These results suggest that based on the type of permeation enhancer used, the water content in the formulation must be considered differently and optimized accordingly. It further suggests that although Transcutol® is an effective permeation enhancer, the optimization of the formulation is an important parameter affecting its action in the formulation. The high permeation from formulations containing oleic acid and oleyl alcohol could be due to the amount of fatty acid derivatives in the formulation. Fatty acids, such as oleic acid, and fatty alcohols, such as oleyl alcohol can interact with the lipids in the stratum corneum (SC) leading to a synergistic increase in the SC's fluidity, which also increases drug mobility. When comparing the DSC profiles of F1 and F2, two exothermic peaks were observed in the cooling thermogram while no exothermic peaks were obtained in F3 and F4.