HIV/AIDS is a global pandemic and the deleterious effects of human immunodeficiency virus in the brain cannot be overlooked. Though the current anti-retro viral therapy is able to reduce the virus load in the peripheral tissues of the body, the inability of the anti-retro viral drugs to cross the blood brain barrier, as such, limits its therapeutic effect in the brain. The development of newer, successful nanoparticulate drug delivery systems to enhance the feasibility of the anti-retro viral drugs to the brain, offers a novel strategy to treat the AIDS-related neuronal degradation. This review summarised the neuropathogenesis of neuroAIDS, the challenges and achievements made in the delivery of therapeutics across the BBB and the use of nanocarriers as a safe and effective way for delivering anti-retro viral drugs to the brain.
Objective:
A simple, accurate and economical reverse phase- high performance liquid chromatographic
method has been developed for the simultaneous quantitative estimation of two anti-retro
viral drugs, Etravirine and Elvitegravir in nanoparticulate formulations for the first time. This method is
a novel analytical technique for the detection of the both the drugs concurrently, as there is no method
available for their simultaneous quantification, to the best of our knowledge.
Methods:
Optimization and validation of the chromatographic conditions were completed according to
the standard ICH guidelines. The separation was done on a C18 column (250 mm x 4.6mm, 5μm) using
methanol and phosphate buffer of pH (5.6) as the mobile phase in the ratio 78:22 v/v at a flow rate of
1ml/min for a short run time of 13 min. The detection wavelength was 285nm and the column temperature
was maintained at 32oC.
Results:
The developed method was linear over 10 to 160 μg/ml with a regression coefficient of 0.999
for each. The LOD values were 4.83 and 9.25 µg/ml while LOQ values were 14.63 and 28.01 µg/ml for
etravirine and elvitegravir respectively. The recovery values obtained by etravirine and elvitegravir
were between 97.6% and 100.8%.
Conclusion:
The method was specific, precise, fast and accurate with good inter and intra day precision.
The method was also effectively employed for the characterization and simultaneous quantification
of both drugs in nanoparticulate formulation.
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