Abstract
Perillyl alcohol has been studied in the treatment of cancer disease. However, its high toxicity is a drawback, which can be overcome by its incorporation in nanostructured systems. The aim of this work was to develop and validate a chromatographic method for determination of perillyl alcohol encapsulation efficiency in a polymeric nanoparticles formulation and evaluation of the presence of related degradation products. Perillyl alcohol was subjected to forced conditions of hydrolysis (acidic, alkaline and neutral), oxidation, photolysis and thermal stress, as suggested in the International Conference of Harmonization (ICH) guidelines. The drug showed significant degradation under acidic conditions. The degradation products could be adequately separated on an XBridge C18 column (100 × 2.1 mm, 3.5 µm) using isocratic elution (350 µL min−1) of water/acetonitrile (65 : 35, v/v) at 210 nm. Data from validation studies demonstrated that the method is selective, linear (coefficient of determination (R2) > 0.999) over the range of 20.0-80.0 µg mL−1, precise (relative standard deviation (RSD) < 2.0%), accurate (98.07 to 101.99%) and robust for minor changes. The method was successfully applied to determine the encapsulation efficiency of perillyl alcohol in polymeric nanoparticles, both for product development and for quality control purposes. After nanoparticles production, the presence of degradation products was not observed indicating that the single-emulsion solvent-evaporation technique used does not favor chemical degradation of the drug.
Highlights
One alternative to overcome these problems is the use of polymeric nanoparticles, which are defined as particulate dispersions or solid particles with a size in the range of 10-1000 nm
A suitable stability-indicating method was developed for both determination of Perillyl alcohol (POH) encapsulation efficiency in polymeric nanoparticles formulation and evaluating the presence of related degradation products
The results of the validation study suggest that the method is selective, linear, precise, accurate and robust
Summary
Chemotherapeutic agents harm healthy tissues, leading to systemic toxicity and adverse effects that greatly limit the maximum tolerated dose of anti-cancer drugs and restrict their therapeutic efficacy.[11] One alternative to overcome these problems is the use of polymeric nanoparticles, which are defined as particulate dispersions or solid particles with a size in the range of 10-1000 nm. Poly(lactic-co-glycolic acid) (PLGA) is one of the most successfully developed biodegradable polymers and has attracted considerable attention due to its attractive properties, such as its low risk of toxicity, high biodegradability and biocompatibility, protection of molecules from premature degradation, improvement
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