Encapsulation of drugs in intact erythrocytes, because of the profound characteristics of these natural microspheres, has gained considerable attention in recent years. In this study, the inhibition time courses of serum angiotensin-converting enzyme (ACE) activity after intravenous administration of enalaprilat encapsulated in intact erythrocytes was evaluated and compared with free drug, in a rabbit model. Three groups of animals each received free drug, drug-loaded erythrocytes or sham-encapsulated erythrocytes. Serum ACE activity was determined in each case using the synthetic substrate hippuryl-histidyl-leucine and quantitation of the hippuric acid released by a developed and validated HPLC method. The serum ACE inhibition profiles in the three groups showed that the encapsulated drug inhibited the serum ACE more slowly, more efficiently, over a considerably longer time and in a more reproducible manner, than the free drug or sham-encapsulated erythrocytes. We conclude that the erythrocytes can serve as efficacious slow-release drug carriers for enalaprilat in circulation.

Download full-text PDF

Source
http://dx.doi.org/10.1111/j.2042-7158.2001.tb01796.xDOI Listing

Publication Analysis

Top Keywords

intact erythrocytes
12
free drug
12
serum ace
12
serum angiotensin-converting
8
angiotensin-converting enzyme
8
intravenous administration
8
ace activity
8
three groups
8
sham-encapsulated erythrocytes
8
erythrocytes
7

Similar Publications

Kingella kingae, an emerging pediatric pathogen, secretes the pore-forming toxin RtxA, which has been implicated in the development of various invasive infections. RtxA is synthesized as a protoxin (proRtxA), which gains its biological activity by fatty acylation of two lysine residues (K558 and K689) by the acyltransferase RtxC. The low acylation level of RtxA at K558 (2-23 %) suggests that the complete acylation at K689 is crucial for toxin activity.

View Article and Find Full Text PDF

Leucinostatins target Plasmodium mitochondria to block malaria transmission.

Parasit Vectors

December 2024

Department of Biological Sciences, Florida International University, 11200 SW 8th St, Miami, FL, 33199, USA.

Background: Malaria remains a critical disease. Leucinostatins from the fungus Purpureocillium lilacinum inhibited the transmission of Plasmodium falciparum to mosquitoes via contact.

Methods: Here, we modified the leucinostatin B (LB) C-terminus to make derivatives and examined their inhibition against malaria transmission to mosquitoes.

View Article and Find Full Text PDF

Red blood cells (RBCs) play a role in the regulation of vascular tone via release of adenosine triphosphate (ATP) into the vasculature in response to various stimuli. Interestingly, ApoE/LDLR double-deficient (ApoE/LDLR) mice, a murine model of atherosclerosis, display a higher exercise capacity compared to the age-matched controls. However, it is not known whether increased exercise capacity in ApoE/LDLR mice is linked to the altered ATP release from RBCs.

View Article and Find Full Text PDF

The Molecular Determinants of Erythrocyte Removal Impact the Development of Metabolic Dysfunction-Associated Steatohepatitis.

Endocr Metab Immune Disord Drug Targets

December 2024

Laboratory of Biochemistry, Department of Medicine, Democritus University of Thrace, Alexandroupolis, Greece.

Metabolic dysfunction-associated steatohepatitis (MASH) is a major cause of a worldwide clinical and financial burden. Despite the tremendous efforts for untangling the molecular mechanisms, there is still a need for defining specific therapeutic targets. In this editorial, the author will focus on the role of erythrocyte death and hepatic erythrophagocytosis in MASH.

View Article and Find Full Text PDF

In several physiopathological processes, phosphatidylserine (PS), normally sequestered to the inner leaflet of the plasma membrane, becomes exposed to the cell surface. In erythrocytes (RBC), PS externalization is a crucial event for the removal of aged/damaged cells but can also be associated with increased prothrombotic activity. Structurally related olive oil antioxidants, including hydroxytyrosol (HT), are able to significantly reduce the percentage of PS-exposing RBC, when cells are exposed to toxic compounds such as the heavy metal mercury (Hg).

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!