International Journal of Drug Delivery Technology
Volume 14, Issue 3

Preparation, Characterization and Evaluation of Monosaccharide Tagged Nanostructured Lipid Carriers for Targeting of Etravirine to Macrophagic AIDS Viral Reservoirs

Bala Tripura Sundari1*, CVS Subramanyam2

1Faculty of Pharmacy, College of Technology, Osmania University, Hyderabad, Telangana, India.

2Department of Pharmaceutics Gokaraju Rangaraju College of Pharmacy, Hyderabad, Telangana, India. 

Received: 12 th March, 2024; Revised: 03rd May, 2024; Accepted: 2nd August, 2024; Available Online: 25th September, 2024

ABSTRACT

Purpose of the study: The present study aimed to develop and examine monosaccharide-decorated nanoparticles specifically designed for macrophage targeting of etravirine.

Methods: Nanostructured lipid carriers (NLC) were prepared with stearylamine as such or after tagging with mannose and galactose as one of the lipid components of NLC. Prior to synthesis, a docking study was used to analyze the potential for interaction of the stearylamine- sugar conjugates with respective lectin receptors. Mannose and galactose-conjugated stearylamine were separately synthesized. Fourier-transform infrared spectroscopy (FTIR), mass spectrometry (MS) and nuclear magnetic resonance (NMR) studies were used to assess successful reactions. Etravirine-loaded non-targeted nanostructured lipid carriers (NLCs) were synthesized with the emulsification solvent evaporation method and characterized for parameters such as zeta potential, in-vitro release, entrapment efficiency and particle size.

To create targeted nanoparticles, stearylamine was replaced with either of the conjugated lipids in the formulation. For stability, all NLC dispersions were lyophilized. In-vitro investigations included cellular uptake and cytotoxicity assessments in the RAW 264.7 macrophage cell line. Following intravenous administration of the NLCs in Wistar rats, in-vivo biodistribution was evaluated.

Results: The docking studies showed good binding potential of both conjugated lipids for respective receptors. Evaluation of synthesized products showed successful conjugation of sugars to stearylamine. The synthesized nanoparticles demonstrated impressive etravirine loading capabilities and exhibited a circular shape with a mean size of approximately 260 nm. Drug release from all NLC formulations persisted for over 24 hours and remained stable after lyophilization. In-vitro evaluations in the RAW 264.7 macrophage cell line revealed that mannosylated nanoparticles had enhanced uptake when compared to non-targeted and galactosylated counterparts. In-vivo plasma and tissue distribution studies corroborated the in-vitro findings, as the mannosylated NLCs displayed a higher distribution into organs with a rich presence of macrophages.

Conclusion: The studies indicate that while sugar tagging of nanoparticles can prove to be an effective strategy for targeting drugs to macrophagic tissue for tackling latent AIDS virus, the choice of sugar is critical.

Keywords: Mannose, Galactose, Mannosylated stearylamine conjugate, Galactosylated stearylamine conjugate, Etravirine,

Macrophage targeting.

International Journal of Drug Delivery Technology (2024); DOI: 10.25258/ijddt.14.3.05

How to cite this article: Sundari BT, Subramanyam CVS. Preparation, Characterization and Evaluation of Monosaccharide Tagged Nanostructured Lipid Carriers for Targeting of Etravirine to Macrophagic AIDS Viral Reservoirs. International Journal of Drug Delivery Technology. 2024;14(3):1278-1291.

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