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1.
Life Sci ; 264: 118676, 2021 Jan 01.
Article in English | MEDLINE | ID: mdl-33129880

ABSTRACT

Angiotensin-converting enzyme 2 (ACE 2) is a membrane-bound enzyme that cleaves angiotensin II (Ang II) into angiotensin (1-7). It also serves as an important binding site for SARS-CoV-2, thereby, facilitating viral entry into target host cells. ACE 2 is abundantly present in the intestine, kidney, heart, lungs, and fetal tissues. Fetal ACE 2 is involved in myocardium growth, lungs and brain development. ACE 2 is highly expressed in pregnant women to compensate preeclampsia by modulating angiotensin (1-7) which binds to the Mas receptor, having vasodilator action and maintain fluid homeostasis. There are reports available on Zika, H1N1 and SARS-CoV where these viruses have shown to produce fetal defects but very little is known about SARS-CoV-2 involvement in pregnancy, but it might have the potential to interact with fetal ACE 2 and enhance COVID-19 transmission to the fetus, leading to fetal morbidity and mortality. This review sheds light on a path of SARS-CoV-2 transmission risk in pregnancy and its possible link with fetal ACE 2.


Subject(s)
Angiotensin-Converting Enzyme 2/genetics , COVID-19/epidemiology , Pandemics , Placenta/virology , Receptors, Virus/genetics , Spike Glycoprotein, Coronavirus/genetics , Adult , Angiotensin-Converting Enzyme 2/chemistry , Angiotensin-Converting Enzyme 2/metabolism , COVID-19/diagnosis , COVID-19/mortality , COVID-19/virology , Female , Fetal Mortality/trends , Fetus , Gene Expression Regulation , Host-Pathogen Interactions/genetics , Humans , Kidney/virology , Models, Molecular , Pregnancy , Protein Structure, Secondary , Receptors, Virus/chemistry , Receptors, Virus/metabolism , Renin-Angiotensin System/genetics , SARS-CoV-2/pathogenicity , Spike Glycoprotein, Coronavirus/chemistry , Spike Glycoprotein, Coronavirus/metabolism , Uterus/virology
2.
J Pharm Pharmacol ; 68(12): 1535-1550, 2016 Dec.
Article in English | MEDLINE | ID: mdl-27709612

ABSTRACT

OBJECTIVES: This study was designed to demonstrate the potential of novel α-lipoic acid-stearylamine (ALA-SA) conjugate-based solid lipid nanoparticles in modulating the pharmacokinetics and hepatotoxicity of tamoxifen (TMX). METHODS: α-lipoic acid-stearylamine bioconjugate was synthesized via carbodiimide chemistry and used as a lipid moiety for the generation of TMX-loaded solid lipid nanoparticles (TMX-SLNs). TMX-SLNs were prepared by solvent emulsification-diffusion method and optimized for maximum drug loading using rotatable central composite design. The optimized TMX-SLNs were stabilized using 10% w/w trehalose as cryoprotectant. In addition, pharmacokinetics and hepatotoxicity of freeze-dried TMX-SLNs were also evaluated in Sprague Dawley rats. KEY FINDINGS: Initial characterization with transmission electron microscopy revealed spherical morphology with smooth surface having an average particle size of 261.08 ± 2.13 nm. The observed entrapment efficiency was 40.73 ± 2.83%. In-vitro release study showed TMX release was slow and pH dependent. Pharmacokinetic study revealed a 1.59-fold increase in relative bioavailability as compared to TMX suspension. A decrease in hepatotoxicity of TMX is evidenced by the histopathological evaluation of liver tissues. CONCLUSIONS: α-lipoic acid-stearylamine conjugate-based SLNs have a great potential in enhancing the oral bioavailability of poorly soluble drugs like TMX. Moreover, this ALA-SA nanoparticulate system could be of significant value in long-term anticancer therapy with least side effects.


Subject(s)
Amines/chemistry , Chemical and Drug Induced Liver Injury/prevention & control , Drug Carriers , Estrogen Antagonists/pharmacokinetics , Nanoparticles , Tamoxifen/pharmacokinetics , Thioctic Acid/chemistry , Administration, Oral , Animals , Biological Availability , Chemical and Drug Induced Liver Injury/etiology , Chemical and Drug Induced Liver Injury/pathology , Cryoprotective Agents/chemistry , Drug Compounding , Drug Stability , Estrogen Antagonists/administration & dosage , Estrogen Antagonists/chemistry , Estrogen Antagonists/toxicity , Female , Freeze Drying , Hydrogen-Ion Concentration , Nanotechnology , Particle Size , Rats, Sprague-Dawley , Solubility , Solvents/chemistry , Surface Properties , Surface-Active Agents/chemistry , Tamoxifen/administration & dosage , Tamoxifen/chemistry , Tamoxifen/toxicity , Technology, Pharmaceutical/methods , Thioctic Acid/analogs & derivatives , Trehalose/chemistry
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