Pharm Sci. 2021;27(3): 418-432.
doi: 10.34172/PS.2020.96
  Abstract View: 173
  PDF Download: 33

Research Article

Efavirenz Loaded Nanostructured Lipid Carriers for Efficient and Prolonged Viral Inhibition in HIV-Infected Macrophages

Ketan Mahajan 1 ORCID logo, Satish Rojekar 1, Dipen Desai 2, Smita Kulkarni 2 ORCID logo, Pradeep Vavia 1* ORCID logo

1 Centre for Novel Drug Delivery Systems, Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, N. P. Marg, Matunga (E), Mumbai – 400 019, India.
2 Department of Virology, National AIDS Research Institute, Plot No 73, G-block, M I D C, Bhosari, Pune, Maharashtra 411 026, India.


Background: The clinical outcome of anti-HIV therapy is poor due to the inherent fallouts ofanti-HIV therapy. It is further worsened due to the presence of viral reservoirs in immune cellslike the macrophages. An ideal anti-HIV therapy must reach, deliver the drug and exert itsaction inside macrophages. To address this, we developed novel cationic nanostructured lipidcarriers of efavirenz (cationic EFV-NLC).

Methods: The developed cationic EFV NLCs were evaluated for particle size, zeta potential,encapsulation efficiency, in-vitro drug release, DSC, XRD, TEM, cytotoxicity, cellular uptakestudies and anti-HIV efficacy in a monocyte-derived macrophage cell line (THP-1).

Results: Cationic EFV-NLCs showed high encapsulation efficiency (90.54 ± 1.7%), uniformparticle size distribution (PDI 0.3-0.5 range) and high colloidal stability with positive zetapotential (+23.86 ± 0.49 mV). DSC and XRD studies confirmed the encapsulation of EFVwithin NLCs. Cytotoxicity studies (MTT assay) revealed excellent cytocompatibility (CC5013.23 ± 0.54 μg/mL). Fluorescence microscopy confirmed the efficient uptake of cationic EFVNLCs,while flow cytometry revealed time and concentration dependant uptake within THP-1cells. Cationic EFV-NLCs showed higher retention and sustained release with 2.32-fold higherpercent inhibition of HIV-1 in infected macrophages as compared to EFV solution at equimolarconcentrations. Interestingly, they demonstrated 1.23-fold superior anti-HIV efficacy over EFVloadedNLCs at equimolar concentrations.

Conclusion: Cationic NLCs were capable of inhibiting the viral replication at higher limitsconsistently for 6 days suggesting successful prevention of HIV-1 replication in infectedmacrophages and thus can prove to be an attractive tool for promising anti-HIV therapy.

Keywords: Anti-HIV efficacy, Efavirenz, HIV-AIDS infection, Nanostructured lipid carriers, Macrophages, Viral reservoirs
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Submitted: 23 Sep 2020
Revision: 23 Nov 2020
Accepted: 24 Nov 2020
ePublished: 24 Nov 2020
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