PMID- 19900521
OWN - NLM
STAT- MEDLINE
DCOM- 20100408
LR  - 20181201
IS  - 1873-3476 (Electronic)
IS  - 0378-5173 (Linking)
VI  - 386
IP  - 1-2
DP  - 2010 Feb 15
TI  - Percutaneous penetration modifiers and formulation effects.
PG  - 42-51
LID - 10.1016/j.ijpharm.2009.10.052 [doi]
AB  - The enhancement/retardation of percutaneous permeation of diethyl-m-toluamide 
      (DEET) in the presence of five percutaneous penetration modifiers (laurocapram, 
      3-dodecanoyloxazolidin-2-one (N-0915), S,S-dimethyl-N-(4-bromobenzoyl) 
      iminosulfurane (DMBIS), S,S-dimethyl-N-(2-methoxycarbonylbenzenesulfonyl) 
      iminosulfurane (DMMCBI) and tert-butyl 1-dodecyl-2-oxoazepan-3-yl-carbamate 
      (TBDOC)) was investigated. These permeation modifiers were formulated in either 
      water, propylene glycol (PG), ethanol or polyethylene glycol 400 (PEG 400). The 
      permeation studies indicated that laurocapram enhanced DEET permeation in PG, but 
      retarded in PEG 400. Likewise, N-0915 acted as a retardant with ethanol and PEG 
      400, but not with water. DMBIS decreased the permeation with ethanol as compared 
      to permeation with water, PEG 400 or PG. Similarly, DMMCB acted as a retardant 
      with ethanol and PEG 400, but not with water or PG. TBDOC formulations revealed 
      its activity as a retardant with ethanol, but behaved as enhancer with water, PG 
      and PEG 400. In addition, penetration modifier interactions with stratum corneum 
      ceramide were investigated using chemical modeling. This investigation is 
      significant since it confirms the role of pharmaceutical formulations and shows 
      for the first time that an enhancer can become a retardant or vice versa 
      depending upon the vehicle in which it is applied to the skin. Hence, we should 
      be using the term "penetration modifiers" for all such compounds.
CI  - Copyright 2009 Elsevier B.V. All rights reserved.
FAU - Kaushik, Diksha
AU  - Kaushik D
AD  - Ernest Mario School of Pharmacy, Rutgers-The State University of New Jersey, 
      Piscataway, NJ 08854, United States.
FAU - Costache, Aurora
AU  - Costache A
FAU - Michniak-Kohn, Bozena
AU  - Michniak-Kohn B
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20091110
PL  - Netherlands
TA  - Int J Pharm
JT  - International journal of pharmaceutics
JID - 7804127
RN  - 0 (Azepines)
RN  - 0 (Carbamates)
RN  - 0 (Ceramides)
RN  - 0 (Insect Repellents)
RN  - 0 (N-(4-bromobenzoyl)-S,S-dimethyliminosulfurane)
RN  - 0 (Oxazolidinones)
RN  - 0 (Pharmaceutic Aids)
RN  - 0 (Solvents)
RN  - 0 (Sulfur Compounds)
RN  - 059QF0KO0R (Water)
RN  - 134-62-3 (DEET)
RN  - 1F3X9DRV9X (laurocapram)
RN  - 3K9958V90M (Ethanol)
RN  - 3WJQ0SDW1A (Polyethylene Glycols)
RN  - 6DC9Q167V3 (Propylene Glycol)
RN  - F1X8L2B00J (N-(alpha-hydroxyoctadecanoyl)phytosphingosine)
SB  - IM
MH  - Administration, Cutaneous
MH  - Azepines/administration & dosage
MH  - Cadaver
MH  - Carbamates/pharmacology
MH  - Ceramides/chemistry
MH  - Chemistry, Pharmaceutical
MH  - DEET/administration & dosage/chemistry/*metabolism
MH  - Drug Compounding
MH  - Ethanol/chemistry
MH  - Humans
MH  - Hydrogen Bonding
MH  - Insect Repellents/administration & dosage/chemistry/*metabolism
MH  - Kinetics
MH  - Models, Molecular
MH  - Molecular Structure
MH  - Oxazolidinones/administration & dosage
MH  - Permeability
MH  - Pharmaceutic Aids/*administration & dosage/chemistry
MH  - Polyethylene Glycols/chemistry
MH  - Propylene Glycol/chemistry
MH  - Skin/*drug effects/metabolism
MH  - Skin Absorption/*drug effects
MH  - Solvents/chemistry
MH  - Structure-Activity Relationship
MH  - Sulfur Compounds/administration & dosage
MH  - Technology, Pharmaceutical/methods
MH  - Water/chemistry
EDAT- 2009/11/11 06:00
MHDA- 2010/04/09 06:00
CRDT- 2009/11/11 06:00
PHST- 2009/08/28 00:00 [received]
PHST- 2009/10/24 00:00 [revised]
PHST- 2009/10/28 00:00 [accepted]
PHST- 2009/11/11 06:00 [entrez]
PHST- 2009/11/11 06:00 [pubmed]
PHST- 2010/04/09 06:00 [medline]
AID - S0378-5173(09)00778-9 [pii]
AID - 10.1016/j.ijpharm.2009.10.052 [doi]
PST - ppublish
SO  - Int J Pharm. 2010 Feb 15;386(1-2):42-51. doi: 10.1016/j.ijpharm.2009.10.052. Epub 
      2009 Nov 10.