Topical Delivery of Erythromycin from Various Formulations: An in Vivo Hairless Mouse Study

Abstract

Topical products containing erythromycin, a macrolide antibiotic with poor aqueous solubility, are usually formulated as high alcohol content solutions or gels. In this study, we evaluated the deposition of erythromycin base into various strata of hairless mouse skin following topical in vivo application from various low- and nonalcoholic formulations. The formulations tested included nonionic liposomal formulation composed of glyceryl dilaurate, cholesterol, and polyoxyethylene-10-stearyl either at a weight ratio of 57:15:28, two nonionic oil-in-water (o/w) liposomal emulsions containing isopropyl myristate or light mineral oil as the oil phase, a conventional o/w emulsion, a 40% hydroalcoholic solution, and two commercially available topical products. Eight hours after topical administration of these formulations, the efficiency of uptake of erythromycin into the living skin strata was in the order: liposomal isopropyl myristate emulsion > > liposomal mineral oil emulsion > > nonionic liposomes approximately Emgel approximately Theramycin-Z > > conventional emulsion > > hydroalcoholic solution. Alcohol-free liposomal systems are shown to be as efficient as high alcohol content products in facilitating permeation of erythromycin through the stratum corneum into living skin tissue.

Niosomes: a review of their structure, properties, methods of preparation, and medical applications

“…The multiple membrane extrusion method uses surfactant, cholesterol, and dicetyl phosphate in chloroform, and the mixture is evaporated to produce a thin film. The film is then hydrated with aqueous drug solution, and the suspension produced is extruded through polycarbonate membranes, which are placed in series for up to 8 passages [20,27,31].…”

Niosomes as Carrier in Dermal Drug Delivery

“…Slow penetration of drug through skin is the main disadvantage of transdermal route of delivery. An increase in the penetration rate has been achieved by transdermal delivery of erythromycin incorporated in niosomes for acne therapy (Jayaraman et al, 1996).…”

Cyclodextrin-erythromycin complexes as a drug delivery device for orthopedic application

“…Both samples were incubated in a 37°C water bath for various time periods. A fraction of samples (100 µL) was collected at different time points (0, 3,5,7,9,12,14,16,18, and 20 hours). These samples were filtered through syringe filters (Minisart, Sartorius Stedim North America Inc, Bohemia, NY) with a pore size of 0.45 µm.…”

“…16 We propose that the efficiency of erythromycin delivered to a periprosthetic site can be increased by improving the chemical stability and water solubility of the drug. 17,18 Cyclodextrins are cyclic oligomers of glucose that are molecular "carriers" with a hydrophilic exterior and a hydrophobic cavity. Cyclodextrins are biocompatible and do not elicit an immune response in humans.…”