Abstract

An in-depth analysis of nanotechnology applications for the improvement of solubility, distribution, bioavailability and stability of reverse transcriptase inhibitors is reported. Current clinically used nucleoside and non-nucleoside agents, included in combination therapies, were examined in the present survey, as drugs belonging to these classes are the major component of highly active antiretroviral treatments. The inclusion of such agents into supramolecular vesicular systems, such as liposomes, niosomes and lipid solid NPs, overcomes several drawbacks related to the action of these drugs, including drug instability and unfavorable pharmacokinetics. Overall results reported in the literature show that the performances of these drugs could be significantly improved by inclusion into nanosystems.

Highlights

  • The human immunodeficiency virus (HIV), belonging to the lentivirus genus of the large family of retroviridae, is the etiological agent of AIDS

  • This approach known as HAART nowadays represents the most useful therapeutic treatment, even though it is affected by many drawbacks such as lifetime administration with a consequent reduced patients’ compliance, severe side effects, and quick viral outbreak after drug resistance emergence

  • A large number of diversely assembled nanocarriers loaded with different classes of antiviral drugs were developed and deeply investigated to improve both pharmacokinetic characteristics and stability behavior

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Summary

Introduction

The human immunodeficiency virus (HIV), belonging to the lentivirus genus of the large family of retroviridae, is the etiological agent of AIDS. The targets of conventional drugs are proteins involved in the viral entry or specific enzymes necessary for the virus replication such as protease (PR), reverse transcriptase (RT) and integrase (IN) This approach known as HAART (highly active antiretroviral therapy) nowadays represents the most useful therapeutic treatment, even though it is affected by many drawbacks such as lifetime administration with a consequent reduced patients’ compliance, severe side effects, and quick viral outbreak after drug resistance emergence. In the light of these findings, the incorporation of new or customary anti-HIV drugs into supramolecular carriers could be effective in suppressing viral replication This strategy is corroborated by the possibility of encapsulating drugs or genes to be delivered next to the infected cells and to target reservoir tissues to eradicate latent HIV [14].

Drug Protection Nanosystems
Lamivudine
Abacavir
Emtricitabine
Tenofovir
Tenofovir SLN
Chitosan based TDF Nanoparticles
Alternative Polymeric TDF NPs
Non-Nucleoside Reverse Transcriptase Inhibitors Nanosystems
Nevirapine
Efavirenz
Efavirenz SLN
Polymeric EFV NPs
Alternative Supramolecular EFV NPs
Dapivirine
Etravirine
Rilpivirine
Findings
Conclusions
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