Potential Impact of Cyclodextrin-Containing Formulations in Toxicity Evaluation of Novel Compounds in Early Drug Discovery
Journal Title: Journal of Pharmaceutics & Pharmacology - Year 2014, Vol 2, Issue 1
Abstract
Cyclodextrins (CDs) are widely used as enabling excipients to improve in vivo drug delivery. The ability of CDs to form inclusion complexes with drugs and thereby improving solubility and stability of drugs is well established, and has been successfully used for several drugs on the market. Combined with well established preclinical and clinical safety profiles for selected CDs, they are of interest as excipients in preclinical and clinical stages of drug development. Another feature of CDs is their demonstrated ability to mitigate local toxicities of drugs. While this feature makes them attractive from a clinical drug delivery perspective, it may not be ideal from a preclinical toxicology evaluation perspective when the new chemical entities have intrinsic irritant or cytotoxic characteristics, which may be shielded by CDs. Herein, we review use of CDs in pharmaceuticals, focusing on their potential to mitigate toxicities of compounds, and suggest that, this very potential may undermine toxicity evaluation, especially by oral route, of novel compounds during early drug discovery.
Authors and Affiliations
Umesh M Hanumegowda
Prevention of Crystal Formation during Formulation of Acyclovir Powder for Solution for Infusion
Aims and objectives: The main objective of the present work is to develop acyclovir powder for solution for infusion with clear solution upon half sealing and formation of stable cake after freezing drying programme. Dur...
Development of Controlled- Release Solid Dispersion Granules Containing a Poorly Water-Soluble Drug, Porous Calcium Silicate, and the Water-Soluble Polymer Polyvinylpyrrolidone
Objectives: This study sought to develop controlled-release solid dispersion granules containing a poorly water-soluble drug, porous calcium silicate (PCS), and a water-soluble polymer. Methods: Nifedipine (NIF) and ind...
Phytochemical Analysis of Polygonum amplexicaule Essential Oil from Pithoragarh, Uttarakhand, India
Introduction: Polygonum amplexicaule (Polygonaceae) is an herbal drug used to treat fractures, rheumatism, osteoporosis, muscle injuries and pain. It has also been reported to be effective to treat atherosclerosis and it...
Current Medication Trends and Global Impact on Neurodegenerative Disorders
Neurodegenerative disorders are the medical condition characterized by destruction in neuronal cells, abruption of neuronal activity and distinct involvement of the functional movement. The main neuronal disorders like P...
Effect of Centruroides Antivenom on Reversal of Methamphetamine-Induced Hyperkinesis and Hyperthermia in Rats
Context: Methamphetamine (MA) toxicity is a major health concern causing agitation, hyperkinesia, hyperthermia, and even death, affecting 24.7 million people worldwide. It has been observed that MA generates movement dis...