Development and Optimization of Erythromycin Loaded Transethosomes Cinnamon Oil Based Emulgel for Antimicrobial Efficiency

Abstract

Erythromycin (EM) is a macrolide antibiotic that is frequently used to treat skin bacterial infections. It has a short half-life (1–1.5 h), instability in stomach pH, and a low oral bioavailability. These foregoing factors limit its oral application; therefore, the development of topical formulations loaded with erythromycin is an essential point to maximize the drug’s concentration at the skin. Accordingly, the current study’s goal was to boost the antimicrobial activity of EM by utilizing the advantages of natural oils such as cinnamon oil. Erythromycin-loaded transethosomes (EM-TE) were generated and optimized using a Box–Behnken design employing, phospholipid concentration (A), surfactant concentration (B), and ethanol content (C) as independent variables. Their effects on entrapment efficiency, EE, (Y1) and the total amount of erythromycin that penetrated the skin after 6 h, Q6h (Y2), were assessed. The optimized transethosome showed a particle size of 256.2 nm, EE of 67.96 ± 0.59%, and Q6h of 665.96 ± 5.87 (µg/cm2) after 6 h. The TEM analysis revealed that, the vesicles are well-known packed structures with a spherical shape. The optimized transethosomes formulation was further transformed into a cinnamon oil-based emulgel system using HPMC as a gelling agent. The generated EM-TE-emulgel was characterized by its physical features, in vitro, ex vivo studies, and antimicrobial activities. The formulation showed sufficient characteristics for effective topical application, and demonstrated a great stability. Additionally, EM-TE-Emulgel had the highest transdermal flux (120.19 μg/cm2·h), and showed considerably (p < 0.05) greater antimicrobial activity, than EM-TE-gel and placebo TE-Emulgel. The action of EM was subsequently augmented with cinnamon oil, which eventually showed a notable effect against bacterial growth. Finally, these results demonstrate that the transethosomes-loaded cinnamon oil-based emulgel is an alternative way to deliver erythromycin for the treatment of topical bacterial infections.

Development of Tea Tree Oil Based Nanoemulgel Loaded with Azithromycin for Enhancing the Antibacterial Activity

“…On the other hand, as was previously noted, a gelling agent was used to prepare the gel base. A homogeneous emulgel was developed by adding the previously prepared emulsion that was loaded with AZ to the gel base and thoroughly mixing it for five minutes [21].…”

“…One gram of the developed preparations was sandwiched between two glass slides under a standard load. The spreadability value was determined by calculating the formulations' spreading areas diameter [21].…”

“…One milliliter of distilled water was employed to dilute ten-milligram samples, and then, a sample of one drop was coated with gold after being dried at room temperature and checked using a scanning electron microscopy [21].…”

“…Actually, the AZ flux from emulgel and nanoemulgel might be improved by the addition of the penetration enhance (oil) and surfactant. Additionally, the external water phase may hydrate the stratum corneum, cause cell swelling, and facilitate the drug transport [21]. Moreover, the im proved permeation of nanoemulgel containing AZ could related to the nano-scaled parti cles, which provide a greater surface area for AZ penetration and facilitate the release o a large portion of the drug [36].…”

The Effectiveness of The Use of Macrolide Antibiotic in Infectious Diseases

“…When used in high doses, depending on the type of pathogen, it may exhibit a bactericidal effect. Sensitive microorganisms include those whose growth is delayed at an antibiotic concentration of less than 0.5 mg/l, moderately sensitive -1-6 mg/l, and resistant -6-8 mg/l [19,20].…”