PMID- 20582492
OWN - NLM
STAT- MEDLINE
DCOM- 20110307
LR  - 20211020
IS  - 1530-9932 (Electronic)
IS  - 1530-9932 (Linking)
VI  - 11
IP  - 3
DP  - 2010 Sep
TI  - Percutaneous penetration modifiers and formulation effects: thermal and spectral 
      analyses.
PG  - 1068-83
LID - 10.1208/s12249-010-9469-x [doi]
AB  - The study investigated the formulation effects of laurocapram and iminosulfurane 
      derived penetration modifiers on human stratum corneum using thermal and spectral 
      analyses. Firstly, formulations of penetration modifiers were assessed as 
      enhancers/retardants using the model permeant, diethyl-m-toluamide followed by 
      investigation of their mechanisms of action using differential scanning 
      calorimetry (DSC) and attenuated total reflectance Fourier-transform infra-red 
      spectroscopy. The penetration modifiers investigated were 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) that were formulated in either water, propylene glycol (PG), ethanol or 
      polyethylene glycol 400 (PEG 400). The results explain the mechanism for the 
      first time why an enhancer can become a retardant or vice versa depending upon 
      the vehicle in which it is applied to the skin. DSC indicated that penetration 
      modifier formulations enhanced permeation of active mainly by disruption and 
      fluidization of the stratum corneum lipid bilayers while IR data indicated 
      characteristic blue shifts with decreases in peak intensity. On the other hand, 
      DSC of penetration modifier formulations showing retardation depicted elevated T 
      (m2) with a strengthening of lipid-protein complex while IR results indicated 
      formation of multiple peaks around 1,738 cm(-1) transition in stratum corneum 
      spectra suggesting retardation may be caused by organization of SC lipids by 
      increased H-bonding.
FAU - Kaushik, Diksha
AU  - Kaushik D
AD  - Ernest Mario School of Pharmacy, Rutgers-The State University of New Jersey, 
      Piscataway, New Jersey 08854, USA.
FAU - Michniak-Kohn, Bozena
AU  - Michniak-Kohn B
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20100626
PL  - United States
TA  - AAPS PharmSciTech
JT  - AAPS PharmSciTech
JID - 100960111
RN  - 0 (Azepines)
RN  - 0 (Emollients)
RN  - 0 (N-(4-bromobenzoyl)-S,S-dimethyliminosulfurane)
RN  - 0 (Sulfur Compounds)
RN  - 1F3X9DRV9X (laurocapram)
SB  - IM
MH  - Azepines/*chemistry/pharmacokinetics
MH  - Drug Compounding/methods
MH  - Emollients/chemistry/*pharmacokinetics
MH  - Humans
MH  - Skin/chemistry/*metabolism
MH  - Skin Absorption/physiology
MH  - Spectrum Analysis/methods
MH  - Sulfur Compounds/*chemistry/pharmacokinetics
PMC - PMC2974143
EDAT- 2010/06/29 06:00
MHDA- 2011/03/08 06:00
PMCR- 2011/06/26
CRDT- 2010/06/29 06:00
PHST- 2010/01/12 00:00 [received]
PHST- 2010/06/07 00:00 [accepted]
PHST- 2010/06/29 06:00 [entrez]
PHST- 2010/06/29 06:00 [pubmed]
PHST- 2011/03/08 06:00 [medline]
PHST- 2011/06/26 00:00 [pmc-release]
AID - 9469 [pii]
AID - 10.1208/s12249-010-9469-x [doi]
PST - ppublish
SO  - AAPS PharmSciTech. 2010 Sep;11(3):1068-83. doi: 10.1208/s12249-010-9469-x. Epub 
      2010 Jun 26.