Abo Bibliothek: Guest
Digitales Portal Digitale Bibliothek eBooks Zeitschriften Referenzen und Berichte Forschungssammlungen
Critical Reviews™ in Therapeutic Drug Carrier Systems
Impact-faktor: 2.9 5-jähriger Impact-Faktor: 3.72 SJR: 0.736 SNIP: 0.551 CiteScore™: 2.43

ISSN Druckformat: 0743-4863
ISSN Online: 2162-660X

Volumen 36, 2019 Volumen 35, 2018 Volumen 34, 2017 Volumen 33, 2016 Volumen 32, 2015 Volumen 31, 2014 Volumen 30, 2013 Volumen 29, 2012 Volumen 28, 2011 Volumen 27, 2010 Volumen 26, 2009 Volumen 25, 2008 Volumen 24, 2007 Volumen 23, 2006 Volumen 22, 2005 Volumen 21, 2004 Volumen 20, 2003 Volumen 19, 2002 Volumen 18, 2001 Volumen 17, 2000 Volumen 16, 1999 Volumen 15, 1998 Volumen 14, 1997 Volumen 13, 1996 Volumen 12, 1995

Critical Reviews™ in Therapeutic Drug Carrier Systems

DOI: 10.1615/CritRevTherDrugCarrierSyst.v17.i4.10
41 pages

Chirality and Its Implications in Transdermal Drug Development

Indra Reddy
Texas A&M Health Science Center Irma Lerma Rangel College of Pharmacy
Thirumala R. Kommuru
Research and Development, Eurand America, Inc., Vandalia, OH 45377
Abdel-Azim A. Zaghloul
Department of Pharmaceutical Sciences, Texas Tech School of Pharmacy, 1300 Coulter, Amarillo, TX 79106
Mansoor A. Khan
Department of Pharmaceutical Sciences, School of Pharmacy, Texas Tech University Health Science Center, Amarillo, TX 79106


Today more than 50% of marketed drugs are chiral. It has been well recognized that the stereochemistry of chiral drugs has a major influence on their pharmacological, pharmacokinetic, and toxicological actions. Studies on enantiomeric differences in the percutaneous permeation of chiral compounds have been actively pursued in recent years. Stratum corneum, the rate-limiting barrier in transdermal permeation, is made up of keratin and ceramide, which could potentially provide chiral environment. Transdermal delivery is often facilitated by the presence of penetration enhancers, which act primarily by altering die diffusion by disrupting the highly ordered membrane structure or by affecting the partitioning behavior of the diffusant molecules. Enantioselective permeation was observed with some chiral excipients including terpene enhancers. While studies on crystalline structures of pure enantiomers and racemates are helpful in understanding the basis for differentiation of physicochemical properties, prediction and control of permeability of enantiomers and racemates based on the physicochemical characteristics would be highly beneficial. The flux characteristics of enantiomers and racemates appear to be dependent upon their thermodynamic properties. Such analyses have a predictive value and are useful in the transdermal drug product development of chiral molecules. While the decision to market either an individual enantiomer or racemate lies strictly under the control of the sponsors, the guidance of the Food and Drug Administration is very helpful. This review presents an overview of the skin structure and transport and a concise review of enantioselective permeation with or without chiral enhancers. Regulatory perspectives on chiral drug product development are also discussed.

Articles with similar content:

Polymeric and Lipid-Based Materials for Topical Nanoparticle Delivery Systems
Critical Reviews™ in Therapeutic Drug Carrier Systems, Vol.27, 2010, issue 5
R. Jayachandra Babu, Kasturi R. Pawar
Modulation of Intracellular Signaling Using Protein-Transduction Technology
Critical Reviews™ in Immunology, Vol.30, 2010, issue 5
Nao Jounai, Akihide Ryo, Toshihiro Horii, Ken J. Ishii, Koichi Suzuki, Kouji Kobiyama, Fumihiko Takeshita
Mucosal Drug Delivery: Membranes, Methodologies, and Applications
Critical Reviews™ in Therapeutic Drug Carrier Systems, Vol.21, 2004, issue 3
Bozena Michniak, Yifan Song, Rashmi Thakur, Victor M. Meidan, Yiping Wang
Drug Carrier Systems for Solubility Enhancement of BCS Class II Drugs: A Critical Review
Critical Reviews™ in Therapeutic Drug Carrier Systems, Vol.30, 2013, issue 3
Sumit Kumar, Saahil Arora , Deepak Bhargava, Arti Thakkar
What Is Involved in a Regulatory Trial Investigating a New Medical Device?
Journal of Long-Term Effects of Medical Implants, Vol.17, 2007, issue 2
Mohit Bhandari, Sarah Resendes, Emil Schemitsch, Paula J. McKay