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Simvastatin- cyclodextrin complexes in aqueous solutions; challenges and solutions.

Ismael Abo Horan and Hákon Hrafn Sigurðsson

Age-related macular degeneration (AMD) is a leading cause of vision loss and blindness in the elderly population. Recently, topical statins showed promising results in tackling posterior segment diseases. The initial aim was to formulate stable simvastatin- cyclodextrin inclusion complexes as eye drops. However, the preliminary studies showed that RMβCD, HPβCD, γ CD, or SBEβCD catalyze the hydrolysis of simvastatin lactone to simvastatin hydroxy acid. To address this stability issue, simvastatin lactone is formulated into an oil-in-water nano-emulsion (O/W NE). All NEs were transparent with bluish color. The mean average size for the blank NE was around 263.3 ± 4 nm and zeta potential of -35.3 ± 0.2 mV, whereas the 0.25 mg/ml simvastatin NE exhibited an average size of 257.4 ± 1.3 nm, and zeta potential of -34.7 ± 0.1mV.Loading simvastatin lactone doesn’t seem to influence the NE size and charge. Estimating the loading efficiency is ongoing.

 

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