Synthesis and characterization of tenofovir disoproxil fumarate loaded nanoparticles for HIV‐1 treatment

Abstract

The remarkable ability of the human immunodeficiency virus (HIV) to evade the host's immune system and conventional antiretroviral therapy, has posed significant challenges in achieving complete eradication of the virus in people living with HIV (PLWHIV). However, nanotechnology has emerged as promising avenue for addressing some of the obstacles associated with the use of antiretroviral drugs by modifying drug molecules in nanoscale dimensions. Hence, the present study explores the utilization of poly(epsilon‐caprolactone) (PCL) as a carrier for encapsulating tenofovir disoproxil fumarate (TDF), offering an alternative treatment approach for HIV infection. TDF‐loaded polymeric nanoparticles were successfully prepared using double emulsion solvent evaporation technique and characterized. The characterization of TDF‐loaded polymeric nanoparticles at varied drug to polymer ratios showed that TDF was loaded in PCL with an encapsulation efficiency and drug loading capacity in the range of 23–46% and 4.8–19.9%, respectively. Of note, the neutralization efficacy of TDF‐loaded polymeric nanoparticles was more improved compared to free TDF. Encapsulation of TDF with PCL did not hinder the antiviral activity of TDF against HIV‐1 infection but rather enhanced its potency.

Histomorphometric changes in testis following administration of tenofovir nanoparticles in an animal model

“…Growing body of evidence implicating nano-delivery particles needs urgent attention as there is increasing interest in the delivery of nanoformulated antiretroviral drugs to overcome the adverse complications. Notably, recent in-vivo and in-vitro studies have demonstrated advances and promising results have been noted when TDF-loaded nanoparticles were studied on various cell lines and rat organs for their potential application to manage HIV and associated complications [ 21 – 23 ]. Although, the current HIV treatment regimen in South Africa containing the preferred first-line ART combination of tenofovir disoproxil fumarate, lamivudine, and dolutegravir (TLD) has produced better treatment outcomes such as viral load suppression, enhanced immune response, and improved clinical indices [ 24 – 26 ].…”