In a “novel” formulation approach, a study has shown that anhydrous self-emulsifying oils (SEO) can be used in the development of eye drops containing antibiotics that are typically unstable in water.
This is according to a study published in the Drug Delivery Journal.
The innovation could significantly benefit antibacterial agents prone to hydrolysis in aqueous media, such as cephalosporins, penicillin, carbapenems, and tetracyclines.
In the paper, Katarzyna Krzeminska and her co-authors show that cefuroxime and vancomycin can be formulated with SEO carriers (also called self-emulsifying drug delivery systems) for ocular delivery without compromising on microbiological activity.
To formulate the SEO carriers, surfactants (polyoxyethylene sorbitan monolaurate or sorbitan monooleate) were dissolved in either fractionated coconut oil, castor oil, or olive oil. This was then added to micronized cefuroxime or vancomycin and mixed until the suspension was deemed homogeneous.
The stability of the formulations was assessed using high-performance liquid chromatography (HPLC) to analyze cefuroxime and vancomycin content in both aqueous and SEO-containing mixtures.
The study showed that within a day, aqueous cefuroxime solution demonstrated a significant decrease in antibiotic content, with complete degradation observed after 7 days.
All formulations containing self-emulsifying oils showed stability across the year, with only those containing castor oil and sorbitan monooleate experiencing 36% degradation after one month.
In the case of aqueous vancomycin, there was an observed 55% degradation of the original antibiotic content after one month of storage at 40oC. This was in sharp contrast to SEO-containing vancomycin formulations that had no more than 10% degradation after a full year.
In addition, microbiological assays conducted on SEO-containing cefuroxime and vancomycin products showed that the SEO component did not reduce the microbiological activity of both antibiotics. Thereby confirming the retained potency of the drugs despite the novel formulation approach.
The authors admit further research may need to be conducted to examine aspects such as eye tolerance the formulation as well as seek complete confirmation of in-vivo effectiveness through a clinical trial.
Source: Drug Delivery Journal
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