Impact of mucoadhesive polymeric nanoparticulate systems on oral bioavailability of a macromolecular model drug

European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V
Angela FabianoYlenia Zambito

Abstract

Nanoparticles (NP) only different in mucoadhesivity are compared for impact on drug oral bioavailability. Two polymeric NP types based on quaternary ammonium-chitosan (NP QA-Ch) and S-protected thiolated derivative thereof (NP QA-Ch-S-pro), respectively, containing the macromolecular drug model, FD4, were prepared by crosslinking each polymer with reduced MW hyaluronic acid. The structure of basic polymers was determined by H1NMR analysis. NP were similar in size (371 ± 38 vs. 376 ± 82 nm); polydispersity index (0.39 ± 0.08 vs. 0.41 ± 0.10); zeta potential (13.4 ± 0.9 vs. 11.9 ± 1.2 mV); reversible interactions with drug (bound drug, 67 vs. 66%); encapsulation efficiency (23 ± 5 vs. 23 ± 8%); release properties (15% released in 15 h in both cases); and apparent permeation across excised rat intestine (Papp, 8.8 ± 0.8 vs. 10 ± 1 cm/s). Then the differences in NP transport ratio through mucus (TR, 0.75 vs. 0.37) and adhesion to excised rat intestinal mucosa (adsorbed fraction, 23 ± 3 vs. 45 ± 2%) were ascribed to higher mucoadhesivity of NP QA-Ch-S-pro compared to NP QA-Ch. This directly influenced drug oral bioavailability in rats (Tmax, 1 vs. 2 h; AUC, 1.7 ± 0.3 vs. 2.9 ± 0.4 μg/mL min, for NP QA-Ch and NP QA-Ch-S-pro, respecti...Continue Reading

Citations

Dec 19, 2019·International Journal of Molecular Sciences·Anna Maria PirasGiovanna Batoni
Jul 28, 2020·Pharmaceutics·Anastasia DetsiPanagiotis Zoumpoulakis
Sep 16, 2020·International Journal of Molecular Sciences·Angela FabianoYlenia Zambito
Jan 7, 2021·Drug Delivery and Translational Research·Supratim DasVineet Kumar Rai
Jun 23, 2020·Biomacromolecules·Christoph FedererAndreas Bernkop-Schnürch
Nov 12, 2020·International Journal of Pharmaceutics·Eva Sanchez Armengol, Flavia Laffleur

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.