An oral formulation of efavirenz‐loaded lactoferrin nanoparticles with improved biodistribution and pharmacokinetic profile

Kumar, Prashant; Lakshmi, Y. Jaya; Kondapi, AK

doi:10.1111/hiv.12475

Cited by 18 publications

(16 citation statements)

References 30 publications

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“…The incorneporation of EFV in NS increased the absorption of the drug in rat intestine in situ, and very important the oral bioavailability in the studies on Albino rabbits. Lactoferin used to prepare NPs loaded with ATZ [140], as described above, has been used also to encapsulate EFV [146], based on the same preparation technique: sol-oil chemistry. Compared with free EFV, the encapsulation of the drug in NPs showed a reduced toxicity to peripheral blood mononuclear cells, Jurkat T cells and B16-F10 cells, an increased anti-HIV-1 activity and improved oral bioavailability and pharmacokinetic profile in studies on rats.…”

Section: Nrtis and Nnrtismentioning

confidence: 99%

Nanomaterials Designed for Antiviral Drug Delivery Transport across Biological Barriers

et al. 2020

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Viral infections are a major global health problem, representing a significant cause of mortality with an unfavorable continuously amplified socio-economic impact. The increased drug resistance and constant viral replication have been the trigger for important studies regarding the use of nanotechnology in antiviral therapies. Nanomaterials offer unique physico-chemical properties that have linked benefits for drug delivery as ideal tools for viral treatment. Currently, different types of nanomaterials namely nanoparticles, liposomes, nanospheres, nanogels, nanosuspensions and nanoemulsions were studied either in vitro or in vivo for drug delivery of antiviral agents with prospects to be translated in clinical practice. This review highlights the drug delivery nanosystems incorporating the major antiviral classes and their transport across specific barriers at cellular and intracellular level. Important reflections on nanomedicines currently approved or undergoing investigations for the treatment of viral infections are also discussed. Finally, the authors present an overview on the requirements for the design of antiviral nanotherapeutics.

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Section: Nrtis and Nnrtismentioning

confidence: 99%

Nanomaterials Designed for Antiviral Drug Delivery Transport across Biological Barriers

et al. 2020

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“…Despite its high efficacy, its administration is usually associated with low bioavailability and high toxicity levels which may restrict its use. Consequently, efavirenz-loaded LF nanoparticles were fabricated by sol-oil method in order to enhance oral delivery of the drug [ 60 ]. Fabricated drug-loaded LF nanoparticles displayed particle size of about 45–60 nm with 59%EE.…”

Section: Lactoferrin In Nanotechnologymentioning

confidence: 99%

“…Fabricated drug-loaded LF nanoparticles displayed particle size of about 45–60 nm with 59%EE. Moreover, in vitro drug release studies revealed that maximum drug release was observed at pH 5, whereas drug release was minimal in both simulated gastric and intestinal fluids, which confirmed their stability in gastrointestinal environment, and hence their suitability for oral route of administration [ 60 ]. In vitro studies showed that the anti-HIV-1 activity of drug-loaded nanoparticles were 2 fold higher in comparison to free drug.…”

Section: Lactoferrin In Nanotechnologymentioning

confidence: 99%

“…In vitro studies showed that the anti-HIV-1 activity of drug-loaded nanoparticles were 2 fold higher in comparison to free drug. Furthermore, efavirenz-loaded LF nanoparticles displayed enhanced pharmacokinetic profiles associated with minimized toxicity in comparison to free drug [ 60 ]. In another interesting approach, efavirenz and curcumin were co-loaded in LF nanoparticles prepared by sol-oil chemistry to be utilized as a multiple prevention technology (MPT) agent.…”

Section: Lactoferrin In Nanotechnologymentioning

confidence: 99%

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Lactoferrin, a unique molecule with diverse therapeutical and nanotechnological applications

Sabra

Agwa

2020

International Journal of Biological Macromolecules

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Lactoferrin (LF) is a naturally glycoprotein with iron-binding properties and diverse biological applications including; antiviral, anti-inflammatory, antioxidant, anti-cancer and immune stimulating effects. In addition, LF was found to be an ideal nanocarrier for some hydrophobic therapeutics because of its active targeting potential due to overexpression of its receptor on the surface of many cells. Moreover, it was proven to be a good candidate for fabrication of nanocarriers to specifically deliver drugs in case of brain tumors owing to the capability of LF to cross the blood brain barrier (BBB). Consequently, it seems to be a promising molecule with multiple applications in the field of cancer therapy and nanomedicine.

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“…Polymeric nanoparticles have also been used to entrap ARV drugs to improve their PK profiles. Compared with free EFV, EFVloaded lactoferrin nanoparticles (lacto-EFV-nano) exhibited improved oral bioavailability and improved PK, with a > 3-4-fold increase in the area under the plasma concentrationtime curve (AUC), a > 30% increase in the peak plasma concentration of the drug after oral administration (C max ), and a 2-fold increase in the time to reach C max (t max ) and t 1/2 [113]. In another study, using methacrylate co-polymer (Eudragit-E100) to engineer nanoparticles of EFV, EFV bioavailability and biodistribution were improved, which resulted in higher drug concentrations in serum and major organs, especially in the brain, compared to the free drug formulation [114].…”

Section: Extended Plasma Drug Levels-mentioning

confidence: 99%

Recent developments of nanotherapeutics for targeted and long-acting, combination HIV chemotherapy

Gao

Kraft

et al. 2019

European Journal of Pharmaceutics and Biopharmaceutics

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Combination antiretroviral therapy (cART) given orally has transformed HIV from a terminal illness to a manageable chronic disease. Yet despite the recent development of newer and more potent drugs for cART and suppression of virus in blood to undetectable levels, residual virus remains in tissues. Upon stopping cART, virus rebounds and progresses to AIDS. Current oral cART regimens have several drawbacks including (1) challenges in patient adherence due to pill fatigue or side-effects, (2) the requirement of life-long daily drug intake, and (3) limited penetration and retention in cells within lymph nodes. Appropriately designed injectable nano-drug combinations that are long-acting and retained in HIV susceptible cells within lymph nodes may address these challenges. While a number of nanomaterials have been investigated for delivery of HIV drugs and drug combinations, key challenges involve developing and scaling delivery systems that provide a drug combination targeted to HIV host cells and tissues where residual virus persists. With validation of the drug-insufficiency hypothesis in lymph nodes, progress has been made in the development of drug combination nanoparticles that are long-acting and targeted to lymph nodes and cells. Unique drug combination nanoparticles (DcNPs) composed of three HIV drugs-lopinavir, ritonavir, and tenofovir-have been shown to provide enhanced drug levels in lymph nodes; and elevated drug-combination levels in HIV-host cells in the blood and plasma for two weeks. This review summarizes the progress in the development of nanoparticle-based drug delivery systems for HIV therapy. It discusses how injectable nanocarriers may be designed to enable delivery of drug combinations that are long-lasting and target-selective in physiological contexts (in vivo) to provide safe and effective use. Consistent drug combination exposure in the sites of residual HIV in tissues and cells may overcome drug insufficiency observed in patients on oral cART.

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An oral formulation of efavirenz‐loaded lactoferrin nanoparticles with improved biodistribution and pharmacokinetic profile

Abstract: Compared with free EFV, lacto-EFV-nano is a promising oral nanoformulation with enhanced bioavailability and efficacy of EFV and improved safety.

Cited by 18 publications

References 30 publications

Nanomaterials Designed for Antiviral Drug Delivery Transport across Biological Barriers

Nanomaterials Designed for Antiviral Drug Delivery Transport across Biological Barriers

Lactoferrin, a unique molecule with diverse therapeutical and nanotechnological applications

Recent developments of nanotherapeutics for targeted and long-acting, combination HIV chemotherapy

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