Preparation and pharmacodynamic assessment of ezetimibe nanocrystals: Effect of P-gp inhibitory stabilizer on particle size and oral absorption

Colloids and Surfaces. B, Biointerfaces
Kale Mohana Raghava Srivalli, Brahmeshwar Mishra

Abstract

Drug nanocrystals have been widely accepted as potent formulations to overcome poor solubility, dissolution and bioavailability problems of hydrophobic drugs. The present study aimed to develop drug nanocrystals of ezetimibe (Eze), a model BCS class II and hypocholesterolemic drug using bottom up precipitation methods. D-α-Tocopheryl polyethylene glycol 1000 succinate (TPGS), and L-ascorbic acid-2-glucoside (AA2G), were the two stabilizers whose potential in developing Eze nanocrystals was investigated. Particle size and zeta potential portrayed the potential of both the stabilizers in producing Eze nanocrystals. The optimized nanocrystal formulations were evaluated for in-vitro solubility, dissolution, solid state characters and in-vivo pharmacodynamic performance. The nanocrystal formulations remarkably increased the solubility of the drug (p<0.05 compared to pure drug). Pure drug could not dissolve more than 28.9% during the 60 min dissolution study whereas the drug nanocrystals prepared with AA2G and TPGS presented t90% at 41.33 ± 2.58 and 16.07 ± 2.32 min, respectively. The PXRD and DSC studies confirmed the retention of crystallinity and the SEM images indicated lack of aggregation in dried nanocrystals. The TPGS nanocrys...Continue Reading

References

Feb 13, 2001·International Journal of Pharmaceutics·S L RaghavanJ Hadgraft
May 14, 2005·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Manthena V S Varma, Ramesh Panchagnula
Jun 2, 2005·Proceedings of the National Academy of Sciences of the United States of America·Margarita Garcia-CalvoNancy A Thornberry
Jan 20, 2007·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·D Douroumis, A Fahr
Jul 16, 2008·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Anne ZimmermannLars Hovgaard
Jul 26, 2008·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·R P Dixit, M S Nagarsenker
Aug 30, 2008·International Journal of Pharmaceutics·Bernard Van EerdenbrughPatrick Augustijns
Sep 23, 2008·Journal of Pharmaceutical Sciences·Bernard Van EerdenbrughGuy Van den Mooter
Nov 11, 2008·International Journal of Pharmaceutics·Ravindra S DhumalPeter York
Jan 24, 2009·International Journal of Pharmaceutics·Prabhat R MishraCornelia M Keck
Mar 11, 2010·International Journal of Pharmaceutics·Jana Pardeike, Rainer H Müller
Apr 27, 2010·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Dengning XiaFude Cui
Apr 28, 2010·Molecular Pharmaceutics·Yang LiuFeng Liu
Oct 12, 2010·International Journal of Pharmaceutics·Dhananjay S SingareParchuri Srinivasa Rao
Jan 8, 2011·Chemical & Pharmaceutical Bulletin·Tugba GulsunLevent Oner
Oct 31, 2012·Colloids and Surfaces. B, Biointerfaces·Guangpu LiuHongxiang Lou
Jan 12, 2013·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Jianjun ZhangShuai Qian
Mar 15, 2013·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Yuanyuan GuoZhiping Zhang
Apr 23, 2013·Colloids and Surfaces. B, Biointerfaces·Pradum Pundlikrao IgeSurendra G Gattani
Nov 21, 2014·Current Drug Targets·Kale Mohana Raghava Srivalli, Brahmeshwar Mishra
Jun 23, 2016·Saudi Pharmaceutical Journal : SPJ : the Official Publication of the Saudi Pharmaceutical Society·Kale Mohana Raghava Srivalli, Brahmeshwar Mishra

❮ 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.