Enhanced oral bioavailability and brain uptake of Darunavir using lipid nanoemulsion formulation

Desai, Jagruti; Thakkar, Hetal

doi:10.1016/j.colsurfb.2018.11.057

Cited by 57 publications

(21 citation statements)

References 31 publications

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“…Here, the mucoadhesive and absorption enhancement properties of chitosan-oleate can finally amplify the geraniol absorption in the bloodstream in comparison with the coarse and unstable emulsion obtained in the presence of glycerol. An analogous result, as obtained in the present study, with nanoemulsions [41] was explained considering the high contact surface of the disperse phase with the absorption mucosa but also supposing an inhibition of efflux transporters like the P-gp pump. In the present case, although dimensions of the dispersed phase were found slightly below the micrometer, the surface area is in any case quite large with respect to coarse emulsions.…”

Section: Discussionsupporting

confidence: 87%

“…This hypothesis is supported by the evidence that, due to is chemical characteristics, geraniol requires specific formulations to be orally administered [7]. Moreover, the CS-OA 2.0% sample probably induces an increased geraniol contact area with the gastrointestinal mucosa than the coarse emulsion [41,42]. Here, the mucoadhesive and absorption enhancement properties of chitosan-oleate can finally amplify the geraniol absorption in the bloodstream in comparison with the coarse and unstable emulsion obtained in the presence of glycerol.…”

Section: Discussionmentioning

confidence: 89%

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Uptake in the Central Nervous System of Geraniol Oil Encapsulated in Chitosan Oleate Following Nasal and Oral Administration

et al. 2019

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The pharmacological activities of geraniol include anticancer and neuroprotective properties. However, its insolubility in water easily induces separation from aqueous formulations, causing administration difficulties. Here we propose new emulsified formulations of geraniol by using the amphiphilic polymer chitosan-oleate (CS-OA) as surfactant to combine mucoadhesive and absorption enhancer properties with stabilization effects on the oil dispersion. The formulation based on CS-OA 2% (w/w) (G-CS-OA-2.0%) showed viscosity values compatible with oral and nasal administration to rats, and mean diameter of the dispersed phase of 819 ± 104 nm. G-CS-OA-2.0% oral administration sensibly increases the geraniol bioavailability with respect to coarse emulsions obtained without CS-OA (AUC values in the bloodstream were 42,713 ± 1553 µg∙mL−1∙min and 2158 ± 82 µg∙mL−1∙min following administration of 50 mg/kg or 1 mg/kg, respectively), and enhances the aptitude of geraniol to reach the central nervous system from the bloodstream (AUC values in the cerebrospinal fluid were 7293 ± 408 µg∙mL−1∙min and 399 ± 25 µg∙mL−1∙min after oral administration of 50 mg/kg or 1 mg/kg, respectively). Moreover, relevant geraniol amounts were detected in the cerebrospinal fluid following the G-CS-OA-2% nasal administration (AUC values in the cerebrospinal fluid were 10,778 ± 477 µg∙mL−1∙min and 5571 ± 290 µg∙mL−1∙min after nasal administration of 4 mg/kg or 1 mg/kg, respectively).

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Section: Discussionsupporting

confidence: 87%

Section: Discussionmentioning

confidence: 89%

Uptake in the Central Nervous System of Geraniol Oil Encapsulated in Chitosan Oleate Following Nasal and Oral Administration

et al. 2019

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“…The different preparation methods to obtain nanoemulsions can be classified into high-energy or low-energy approaches. High-energy methods, such as ultrasonic homogenisation or microfluidisation, usually entail high formulation temperatures, what may limit their use of thermo labile molecules like peptides [73,74,77,[88][89][90][91][92][93][94]. Low-energy methods, including solvent displacement technique and phase inversion, are performed in milder conditions [74].…”

Section: Nanoemulsionsmentioning

confidence: 99%

Current approaches in lipid-based nanocarriers for oral drug delivery

Plaza-Oliver

Santander-Ortega

Lozano

2021

Drug Deliv. and Transl. Res.

111

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Graphical abstract Lipid-based nanocarriers have gained much interest as carriers of drugs with poor oral bioavailability because of their remarkable advantages like low toxicity, affordable scale-up manufacture, strong biocompatibility or high drug loading efficiency. The potential of these nanocarriers lies in their ability to improve the gastrointestinal stability, solubility and permeability of their cargo drugs. However, achieving efficient oral drug delivery through lipid-based nanocarriers is a challenging task, since they encounter multiple physicochemical barriers along the gastrointestinal tract, e.g. the gastric acidic content, the intestinal mucus layer or the enzymatic degradation, that they must surmount to reach their target. These limitations may be turned into opportunities through a rational design of lipid-based nanocarriers. For that purpose, this review focuses on the main challenges of the oral route indicating the strategies undertaken for lipid-based nanocarriers in order to overcome them. Understanding their shortcomings and identifying their strengths will determine the future clinical success of lipid-based nanocarriers.

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“…Using this formulation a 2.3-fold higher oral bioavailability of DRV with respect to both the unprocessed and the nanonized DRV/RTV combinations was estimated in albino Sprague-Dawley rats (Augustine et al 2018). Enhanced bioavailability of darunavirloaded lipid nanoemulsion in the brain after oral administration was described by Desai and Thakkar (2019).…”

Section: Human Immunodeficiency Virusmentioning

confidence: 99%

Nanoformulations: A Valuable Tool in the Therapy of Viral Diseases Attacking Humans and Animals

Jampílek

Kráľová

2019

Nanotheranostics

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Various viruses can be considered as one of the most frequent causes of human diseases, from mild illnesses to really serious sicknesses that end fatally. Numerous viruses are also pathogenic to animals and plants, and many of them, mutating, become pathogenic also to humans. Several cases of affecting humans by originally animal viruses have been confirmed. Viral infections cause significant morbidity and mortality in humans, the increase of which is caused by general immunosuppression of the world population, changes in climate, and overall globalization. In spite of the fact that the pharmaceutical industry pays great attention to human viral infections, many of clinically used antivirals demonstrate also increased toxicity against human cells, limited bioavailability, and thus, not entirely suitable therapeutic profile. In addition, due to resistance, a combination of antivirals is needed for life-threatening infections. Thus, the development of new antiviral agents is of great importance for the control of virus spread. On the other hand, the discovery and development of structurally new antivirals represent risks. Therefore, another strategy is being developed, namely the reformulation of existing antivirals into nanoformulations and investigation of various metal and metalloid nanoparticles with respect to their diagnostic, prophylactic, and therapeutic antiviral applications. This chapter is focused on nanoscale materials/formulations with the potential to be used for the treatment or inhibition of the spread of viral diseases caused by human immunodeficiency virus, influenza A viruses (subtypes H3N2 and H1N1), avian influenza and swine influenza viruses, respiratory syncytial virus, herpes simplex virus, hepatitis B and C viruses, Ebola and Marburg viruses, Newcastle disease virus, dengue and Zika viruses, and pseudorabies virus. Effective antiviral long-lasting and target-selective nanoformulations developed for oral, intravenous, intramuscular, intranasal, intrarectal, intravaginal, and intradermal applications are discussed.

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Enhanced oral bioavailability and brain uptake of Darunavir using lipid nanoemulsion formulation

Cited by 57 publications

References 31 publications

Uptake in the Central Nervous System of Geraniol Oil Encapsulated in Chitosan Oleate Following Nasal and Oral Administration

Uptake in the Central Nervous System of Geraniol Oil Encapsulated in Chitosan Oleate Following Nasal and Oral Administration

Current approaches in lipid-based nanocarriers for oral drug delivery

Nanoformulations: A Valuable Tool in the Therapy of Viral Diseases Attacking Humans and Animals

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