Determining the Effect of pH on the Partitioning of Neutral, Cationic and Anionic Chemicals to Artificial Sebum: New Physicochemical Insight and QSPR Model

Pharmaceutical Research
Senpei YangGuoping Lian

Abstract

Sebum is an important shunt pathway for transdermal permeation and targeted delivery, but there have been limited studies on its permeation properties. Here we report a measurement and modelling study of solute partition to artificial sebum. Equilibrium experiments were carried out for the sebum-water partition coefficients of 23 neutral, cationic and anionic compounds at different pH. Sebum-water partition coefficients not only depend on the hydrophobicity of the chemical but also on pH. As pH increases from 4.2 to 7.4, the partition of cationic chemicals to sebum increased rapidly. This appears to be due to increased electrostatic attraction between the cationic chemical and the fatty acids in sebum. Whereas for anionic chemicals, their sebum partition coefficients are negligibly small, which might result from their electrostatic repulsion to fatty acids. Increase in pH also resulted in a slight decrease of sebum partition of neutral chemicals. Based on the observed pH impact on the sebum-water partition of neutral, cationic and anionic compounds, a new quantitative structure-property relationship (QSPR) model has been proposed. This mathematical model considers the hydrophobic interaction and electrostatic interaction as the...Continue Reading

References

Jul 1, 1976·The Journal of Investigative Dermatology·J S StraussD T Downing
Jun 1, 1986·The Journal of Investigative Dermatology·K M NordstromJ J Leyden
Sep 1, 1984·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·D M SmallJ A Hamilton
Feb 1, 1995·Pharmaceutical Research·A C LauerN D Weiner
Jun 1, 1997·Pharmaceutical Research·S D KrämerH Wunderli-Allenspach
Jan 1, 1997·Critical Reviews in Therapeutic Drug Carrier Systems·B Illel
Oct 31, 1998·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·U Hagedorn-Leweke, B C Lippold
Feb 2, 2002·Nature·Laura J van 't VeerStephen H Friend
Oct 5, 2002·Journal of Controlled Release : Official Journal of the Controlled Release Society·Ylva Y Grams, Joke A Bouwstra
Feb 14, 2004·The Journal of Investigative Dermatology·Nina OtbergJürgen Lademann
Sep 1, 2005·Annals of Biomedical Engineering·Ana M Barbero, H F Frasch
Nov 2, 2005·International Journal of Pharmaceutics·Victor M MeidanBozena B Michniak
Dec 26, 2006·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Yakov FrumVictor M Meidan
Jun 26, 2007·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Steffi HansenUlrich F Schaefer
Jul 13, 2007·International Journal of Pharmaceutics·Satyanarayana Valiveti, Guang Wei Lu
Jul 27, 2007·International Journal of Pharmaceutics·Satyanarayana ValivetiGuang Wei Lu
Dec 12, 2007·British Journal of Clinical Pharmacology·Nina OtbergJürgen Lademann
Oct 22, 2008·International Journal of Pharmaceutics·Guang Wei LuMatt Mollan
Aug 3, 2010·International Journal of Pharmaceutics·Liming WangLujia Han
Mar 5, 2011·Journal of Pharmaceutical Sciences·Steffi HansenGerald B Kasting
Jun 27, 2012·Journal of Pharmaceutical Sciences·Salem Seif, Steffi Hansen

❮ Previous
Next ❯

Software Mentioned

SPSS
MarvinSketch
Origin
EPI Suite
SIMASTAT

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.