Liposomes have been considered the most suitable drug delivery system for a range of pharmaceutical and biomedical applications. The drugs encapsulated have several advantages such as the protection of drugs by degradation caused by the organism environment and the minimization of the potential side effects in the body. The ethanol injection method is an interesting technique for scaling-up liposomes production, due to their simplicity, fast implementation, and reproducibility. However, only a very small percentage of a water-soluble drug can be passively encapsulated inside the formed vesicles. This problem led us to optimize the production of liposomes encapsulating methotrexate disodium salt, a hydrophilic drug, based on the principles of the ethanol injection method. After several optimizations, our results showed that it was possible to establish a new pre-concentration method for liposomes production, observing an increase in the encapsulation efficiency of methotrexate more than 10 times. Furthermore, we established a rapid and easy method for quantification of drugs encapsulated in liposomes, exploiting the advantages of 1H Nuclear Magnetic Resonance (NMR) spectrometry. Comparing the assay results obtained by quantitative NMR with conventional techniques Ultraviolet-Visible spectrophotometry and High-Performance Liquid Chromatography no significant differences in drug concentration were observed. In summary, the present study offerings a promising liposomal production method for liposomes encapsulating methotrexate and even a simple quantitative NMR analysis method for quantification of drugs encapsulated in liposomes.

Liposomes encapsulating methotrexate: Methods for production and quantification

Macromolecular Chemistry: The Second Century

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ACS Spring 2020 National Meeting & Expo

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.