Phospholipon 90H (P90H)-based PEGylated microscopic lipospheres delivery system for gentamicin: an antibiotic evaluation

ABSTRACT

<p><b>OBJECTIVE</b>To formulate gentamicin liposphere by solvent-melting method using lipids and polyethylene glycol 4 000 (PEG-4 000) for oral administration.</p><p><b>METHODS</b>Gentamicin lipospheres were prepared by melt-emulsification using 30% w/w Phospholipon® 90H in Beeswax as the lipid matrix containing PEG-4 000. These lipospheres were characterized by evaluating on encapsulation efficiency, loading capacity, change in pH and the release profile. Antimicrobial activities were evaluated against Escherichia coli, Pseudomonas aeruginosa, Salmonella paratyphii and Staphylococcus aureus using the agar diffusion method.</p><p><b>RESULTS</b>Photomicrographs revealed spherical particles within a micrometer range with minimal growth after 1 month. The release of gentamicin in vitro varied widely with the PEG-4 000 contents. Moreover, significant (P>0.05) amount of gentamicin was released in vivo from the formulation. The encapsulation and loading capacity were all high, indicating the ability of the lipids to take up the drug. The antimicrobial activities were very high especially against Pseudomonas compare to other test organisms. This strongly suggested that the formulation retain its bioactive characteristics.</p><p><b>CONCLUSIONS</b>This study strongly suggest that the issue of gentamicin stability and poor absorption in oral formulation could be adequately addressed by tactical engineering of lipid drug delivery systems such as lipospheres.</p>