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Objective: The aim of this study was to develop mupirocin topical spray using Eudragit E100 as a film-forming agent for the treatment of bacterial skin infections as well as to promote wound healing., Materials and Methods: Twenty-seven of mupirocin formulations were formulated containing Eudragit E100 and other excipients. Mupirocin spray was prepared by aerosol crimping and filling machine using HFA-134a as a propellant. The formulations were evaluated for their stability and physicochemical properties. The factorial study was applied to evaluate the effects of glycerol and PEG400 on mupirocin-loaded Eudragit E100 films. The optimized formulation was assessed of drug release, antibacterial activities and in vitro cell line studies in comparison to the ointment formulation., Results and Discussion: Mupirocin sprays were formulated and optimized to obtain the formulation with excellent physicochemical and mechanical properties of the dressing film. The formulation had an excellent stability up to a year with more than 80% of mupirocin content. Mupirocin was released from the film up to 90% within 2 h. The formulation had a potent antibacterial effect against S. aureus and S. epidermidis. The formulation was safe to use as a topical formulation that had no toxicity to keratinocytes, fibroblasts and monocytes. The formulation also had an antiendotoxin effect without stimulating the production of NO and inflammatory cytokines (IL-1β and TNF-α)., Conclusions: Mupirocin topical spray was successful developed as a topical formulation and can be used instead of the ointment formulation. Animal experiments are warranted to further emphasize the safe use in the human skin.

Objective: The aim of this study was to conduct in vitro studies of a dry powder formulation of ethambutol dihydrochloride (EDH) to determine if it was an acceptable candidate for further in vivo studies to target alveolar macrophages for the treatment of lung tuberculosis., Materials and Methods: Nanosized drug particles were prepared by optimizing the spray drying conditions. The cell toxicities were determined by interacting the formulations with respiratory cell lines (A549, calu-3 and NR8383 cell lines), and phagocytosis of the formulations was tested on a macrophage cell line. Permeations of the EDH formulations across a lipid bilayer were studied using the Ussing chamber and HPLC. Bioactivity tests of the formulations were carried out by using the resazurin method on M. bovis cells., Result and Discussion: Spray rate and inlet temperature were the two most important factors that affected the size and % yield of the product. The % cell viability of A549 cells with all EDH formulations, pure EDH and chitosan carrier was higher than 80%, the calu-3 cell line had % viabilities of between 85 and 99%, and the % viability of NR8383 cells was between 81 and 100%. The pure EDH had a minimum inhibitory concentration (MIC) of 2 µg/mL while the EDH formulations had MIC values of less than 1 µg/mL when tested against M. bovis. The formulation was completely phagocytized by the macrophage cells after 30 min. The permeability of pure EDH across lipid bilayer was 48.7% after 2 h while in the EDH formulations it was enhanced to 71%., Conclusion: The EDH formulations showed a lower toxicity, higher potency and better permeation than the pure EDH. Thus, EDH DPI formulations could help to minimize the duration of treatment and the risk of developing multidrug resistance tuberculosis compared to the non-formulated EDH.