PMID- 23135817
OWN - NLM
STAT- MEDLINE
DCOM- 20130703
LR  - 20211021
IS  - 1573-904X (Electronic)
IS  - 0724-8741 (Linking)
VI  - 30
IP  - 2
DP  - 2013 Feb
TI  - Lecithin-based microemulsions for targeted delivery of ceramide AP into the 
      stratum corneum: formulation, characterizations, and in vitro release and 
      penetration studies.
PG  - 538-51
LID - 10.1007/s11095-012-0899-x [doi]
AB  - PURPOSE: To improve the solubility and penetration of Ceramide AP (CER [AP]) into 
      the stratum corneum that potentially restores the barrier function of aged and 
      affected skin. METHODS: CER [AP] microemulsions (MEs) were formulated using 
      lecithin, Miglyol(R) 812 (miglyol) and water-1,2 pentandiol (PeG) mixture as 
      amphiphilic, oily and hydrophilic components, respectively. The nanostructure of 
      the MEs was revealed using electrical conductivity, differential scanning 
      calorimeter (DSC) and electron paramagnetic resonance (EPR) techniques. Photon 
      correlation spectroscopy (PCS) was used to measure the sizes and shape of ME 
      droplets. The release and penetration of the CER into the stratum corneum was 
      investigated in vitro using a multi-layer membrane model. RESULTS: The MEs 
      exhibited excellent thermodynamic stability (>2 years) and loading capacity (0.5% 
      CER [AP]). The pseudo-ternary phase diagrams of the MEs were obtained and PCS 
      results showed that the droplets are spherical in shape and bigger in size. In 
      vitro investigations showed that the MEs exhibited excellent rate and extent of 
      release and penetration. CONCLUSIONS: Stable lecithin-based CER [AP] MEs that 
      significantly enhance the solubility and penetration of CER [AP] into the stratum 
      corneum were developed. The MEs also have better properties than the previously 
      reported polyglycerol fatty acid surfactant-based CER [AP] MEs.
FAU - Sahle, Fitsum F
AU  - Sahle FF
AD  - Dept. of Pharmaceutical Technology & Biopharmaceutics Institute of Pharmacy, 
      Martin Luther University Halle-Wittenberg, Halle (Saale), Germany.
FAU - Metz, Hendrik
AU  - Metz H
FAU - Wohlrab, Johannes
AU  - Wohlrab J
FAU - Neubert, Reinhard H H
AU  - Neubert RH
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20121108
PL  - United States
TA  - Pharm Res
JT  - Pharmaceutical research
JID - 8406521
RN  - 0 (Ceramides)
RN  - 0 (Emulsions)
RN  - 0 (Lecithins)
RN  - 0 (Membranes, Artificial)
SB  - IM
MH  - Ceramides/*administration & dosage/pharmacokinetics
MH  - *Drug Delivery Systems
MH  - Electric Conductivity
MH  - Emulsions/*chemistry
MH  - Epidermis/*metabolism
MH  - Humans
MH  - Lecithins/*chemistry
MH  - Membranes, Artificial
MH  - Particle Size
MH  - Refractometry
MH  - Viscosity
EDAT- 2012/11/09 06:00
MHDA- 2013/07/05 06:00
CRDT- 2012/11/09 06:00
PHST- 2012/08/04 00:00 [received]
PHST- 2012/10/08 00:00 [accepted]
PHST- 2012/11/09 06:00 [entrez]
PHST- 2012/11/09 06:00 [pubmed]
PHST- 2013/07/05 06:00 [medline]
AID - 10.1007/s11095-012-0899-x [doi]
PST - ppublish
SO  - Pharm Res. 2013 Feb;30(2):538-51. doi: 10.1007/s11095-012-0899-x. Epub 2012 Nov 
      8.