Approaches to increase mechanistic understanding and aid in the selection of precipitation inhibitors for supersaturating formulations - a PEARRL review

The Journal of Pharmacy and Pharmacology
Daniel J PriceChristoph Saal

Abstract

Supersaturating formulations hold great promise for delivery of poorly soluble active pharmaceutical ingredients (APIs). To profit from supersaturating formulations, precipitation is hindered with precipitation inhibitors (PIs), maintaining drug concentrations for as long as possible. This review provides a brief overview of supersaturation and precipitation, focusing on precipitation inhibition. Trial-and-error PI selection will be examined alongside established PI screening techniques. Primarily, however, this review will focus on recent advances that utilise advanced analytical techniques to increase mechanistic understanding of PI action and systematic PI selection. Advances in mechanistic understanding have been made possible by the use of analytical tools such as spectroscopy, microscopy and mathematical and molecular modelling, which have been reviewed herein. Using these techniques, PI selection can be guided by molecular rationale. However, more work is required to see widespread application of such an approach for PI selection. Precipitation inhibitors are becoming increasingly important in enabling formulations. Trial-and-error approaches have seen success thus far. However, it is essential to learn more about the mo...Continue Reading

References

Feb 27, 1975·Nature·M Levitt, A Warshel
Sep 1, 1984·Hepatology : Official Journal of the American Association for the Study of Liver Diseases·R T Holzbach
Jan 1, 1994·Journal of Applied Biomaterials : an Official Journal of the Society for Biomaterials·T ChandyC P Sharma
Jul 7, 1999·Journal of Pharmaceutical Sciences·N Rodríguez-Hornedo, D Murphy
Apr 18, 2000·International Journal of Pharmaceutics·M IervolinoJ Hadgraft
Jun 28, 2000·Pharmaceutical Research·B C Hancock, M Parks
Oct 18, 2000·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·C W Pouton
Dec 6, 2000·Advanced Drug Delivery Reviews·M Nakano
Feb 13, 2001·Journal of Colloid and Interface Science·Kouji MaedaShouji Hirota
Mar 29, 2001·Journal of Pharmacological and Toxicological Methods·C A Lipinski
Jul 13, 2002·Journal of Pharmaceutical Sciences·Jef PeetersMarcus E Brewster
Apr 22, 2003·Chemical Communications : Chem Comm·P E BonnettR J Davey
Feb 26, 2004·The Journal of Pharmacy and Pharmacology·Edmund S KostewiczJennifer B Dressman
Apr 15, 2004·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·R Neslihan Gursoy, Simon Benita
Nov 3, 2004·Nature Reviews. Drug Discovery·Colin R GardnerOrn Almarsson
Mar 12, 2005·Journal of Pharmaceutical Sciences·Goran Westerberg, Lars Wiklund
Sep 13, 2005·Journal of Colloid and Interface Science·Hong WenKinam Park
Jul 15, 2006·International Journal of Pharmaceutics·Vimon TantishaiyakulWibul Wongpoowarak
Mar 3, 2007·Nature Reviews. Drug Discovery·Christopher J H PorterWilliam N Charman
Jun 19, 2007·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Markus VogtJennifer B Dressman
Jul 10, 2007·Advanced Drug Delivery Reviews·Abu T M Serajuddin
Jul 17, 2007·Journal of Pharmaceutical Sciences·Thorsteinn LoftssonFífa Konrádsdóttir
Sep 12, 2007·Journal of Pharmaceutical Sciences·Sandrien JanssensGuy Van den Mooter
Sep 25, 2007·Journal of Controlled Release : Official Journal of the Controlled Release Society·Rebecca L CarrierImran Ahmed
Jan 26, 2008·Nature Reviews. Drug Discovery·Jarkko RautioJouko Savolainen
Feb 27, 2008·International Journal of Pharmaceutics·Wei-Guo DaiZhengyu Deng
Apr 19, 2008·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Marcus E BrewsterThorsteinn Loftsson
May 2, 2008·Journal of Pharmaceutical Sciences·Alan D GiftLynne S Taylor
Jun 20, 2008·Journal of Colloid and Interface Science·Lennart LindforsUlf Olsson
Apr 18, 2009·Journal of Pharmaceutical Sciences·Joachim BrouwersPatrick Augustijns
May 13, 2009·Molecular Pharmaceutics·James C DiNunzioRobert O Williams
Aug 19, 2010·Pharmaceutical Research·Sara CarlertBertil Abrahamsson
Sep 3, 2010·Current Topics in Medicinal Chemistry·Ayako OhnoMasahiro Shirakawa

❮ Previous
Next ❯

Citations

Dec 29, 2020·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Alexandra-Roxana IlieRené Holm
Mar 11, 2020·International Journal of Pharmaceutics: X·Deanna M MudieDavid T Vodak
Feb 22, 2021·Advanced Drug Delivery Reviews·Zahari VinarovPatrick Augustijns
May 21, 2021·International Journal of Pharmaceutics·Martin MüllerJörg Breitkreutz
May 15, 2021·International Journal of Pharmaceutics·Tanja PotrčPetra Kocbek
Sep 6, 2019·Molecular Pharmaceutics·Ralm G RicarteMarc A Hillmyer

❮ 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.

Related Papers

Journal of Child Language
K PlunkettE Bates
Advanced Drug Delivery Reviews
Jennifer WalshEuropean Formulation Initiative
Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Leena Peltonen, Clare Strachan
Journal of Pharmacy & Pharmaceutical Sciences : a Publication of the Canadian Society for Pharmaceutical Sciences, Société Canadienne Des Sciences Pharmaceutiques
Meiyan YangChunsheng Gao
© 2022 Meta ULC. All rights reserved