PMID- 20222026
OWN - NLM
STAT- MEDLINE
DCOM- 20101028
LR  - 20161125
IS  - 1520-6017 (Electronic)
IS  - 0022-3549 (Linking)
VI  - 99
IP  - 8
DP  - 2010 Aug
TI  - Hexyl aminolaevulinate is a more effective topical photosensitiser precursor than 
      methyl aminolaevulinate and 5-aminolaevulinic acids when applied in equimolar 
      doses.
PG  - 3486-98
LID - 10.1002/jps.22116 [doi]
AB  - Aminolaevulinic acid (ALA) is known to poorly penetrate into thick lesions, such 
      as nodular basal cell carcinomas. Short chain ALA esters, possessing increased 
      lipophilicity relative to their hydrophilic parent, have previously been shown to 
      be highly efficient at inducing protoporphyrin IX (PpIX) production in cell 
      culture, at equimolar concentrations. In contrast, in vitro skin permeation and 
      in vivo animal studies, which up to now have compared prodrugs on a % w/w basis, 
      have failed to demonstrate such benefits. For the first time, equimolar 
      concentrations of ALA, methyl-ALA (m-ALA) and hexyl-ALA (h-ALA) have been 
      incorporated into an o/w cream preparation. In vitro penetration studies into 
      excised porcine skin revealed that increased levels of h-ALA, compared to ALA and 
      m-ALA were found in the upper skin layers, at all drug loadings studied. Topical 
      application of the formulations to nude murine skin in vivo, revealed that creams 
      containing h-ALA induced significantly higher levels of peak PpIX fluorescence 
      (F(max) = 289.0) at low concentrations compared to m-ALA (F(max) = 159.2) and ALA 
      (F(max) = 191.9). Importantly, this study indicates that when compared on an 
      equimolar basis, h-ALA has improved skin penetration, leading to enhanced PpIX 
      production compared to the parent drug and m-ALA.
CI  - (c) 2010 Wiley-Liss, Inc. and the American Pharmacists Association
FAU - Morrow, Desmond I J
AU  - Morrow DI
AD  - School of Pharmacy, Queen's University Belfast, Medical Biology Centre, Belfast, 
      UK.
FAU - McCarron, Paul A
AU  - McCarron PA
FAU - Woolfson, A David
AU  - Woolfson AD
FAU - Juzenas, Petras
AU  - Juzenas P
FAU - Juzeniene, Asta
AU  - Juzeniene A
FAU - Iani, Vladimir
AU  - Iani V
FAU - Moan, Johan
AU  - Moan J
FAU - Donnelly, Ryan F
AU  - Donnelly RF
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PL  - United States
TA  - J Pharm Sci
JT  - Journal of pharmaceutical sciences
JID - 2985195R
RN  - 0 (Ointments)
RN  - 0 (Photosensitizing Agents)
RN  - 585NM85KYM (methyl 5-aminolevulinate)
RN  - 88755TAZ87 (Aminolevulinic Acid)
RN  - G7H20TKI67 (5-aminolevulinic acid hexyl ester)
SB  - IM
MH  - Administration, Topical
MH  - Aminolevulinic Acid/administration & dosage/*analogs & derivatives/chemical 
      synthesis/*pharmacology
MH  - Animals
MH  - Animals, Newborn
MH  - Chemistry, Pharmaceutical
MH  - Drug Delivery Systems
MH  - In Vitro Techniques
MH  - Isotope Labeling
MH  - Mice
MH  - Mice, Inbred BALB C
MH  - Ointments
MH  - Photosensitizing Agents/administration & dosage/chemical synthesis/*pharmacology
MH  - Skin/chemistry/drug effects
MH  - Skin Absorption
MH  - Swine
EDAT- 2010/03/12 06:00
MHDA- 2010/10/29 06:00
CRDT- 2010/03/12 06:00
PHST- 2010/03/12 06:00 [entrez]
PHST- 2010/03/12 06:00 [pubmed]
PHST- 2010/10/29 06:00 [medline]
AID - S0022-3549(15)32537-5 [pii]
AID - 10.1002/jps.22116 [doi]
PST - ppublish
SO  - J Pharm Sci. 2010 Aug;99(8):3486-98. doi: 10.1002/jps.22116.