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Abstract
Objective: Saquinavir (SQV) is a US-FDA approved HIV protease inhibitor (HPI) for HIV cure. The purpose of the present investigation was to develop and characterize the anticancer potential of the SQV-loaded folic acid (FA) conjugated PEGylated and non-PEGylated poly(d,l-lactide-co-glycolide) (PLGA) nanoparticles (NPs) (SQV–Fol–PEG–PLGA and SQV–Fol–PLGA) employing PC-3 (human prostate) and MCF-7 (human breast) cancer cell lines.
Materials and methods: Developed NPs were characterized by IR, NMR, DSC, XRD, size, charge and further tested for drug loading and cellular uptake properties.
Result: The entrapment efficiency was found to be 56 ± 0.60 and 58 ± 0.80 w/v for SQV–Fol–PEG–PLGA and SQV–PLGA NPs, respectively. The obtained results of SQV–Fol–PEG–PLGA showed enhanced cytotoxicity and cellular uptake and were most preferentially taken up by the cancerous cells via folate receptor-mediated endocytosis (RME) mechanism. At 260 µM concentration, SQV–PLGA NPs and SQV–Fol–PEG–PLGA NPs showed 20%, 20% and 23% cell growth inhibition in PC-3 cells, respectively whereas in MCF-7 cells it was 12%, 15% and 14% cell growth inhibition, respectively.
Conclusions: Developed targeted SQV–Fol–PEG–PLGA NPs were superior anticancer potential as compared to non-targeted SQV–PLGA NPs. Thus, these targeted NPs provide another option for anticancer drug delivery scientists.
Declaration of interest
The authors report no conflicts of interest. The authors alone are responsible for the content and writing of this article.
The authors (Ruchi Singh) would like to acknowledge Department of Science and Technology (DST), New Delhi, India for providing the Fellowship to carry out this research work. Additionally, authors would also like to acknowledge F. Hoffman-La Roche, Mannheim (Germany) for providing the gift sample of Saquinavir.