Skin penetration and retention of L-ascorbic acid 2-phosphate using multilamellar vesicles.
Transdermal formulation of L-ascorbic acid 2-phosphate magnesium salt (A2P) was prepared using multilamellar vesicles (MLV). A2P was either physically mixed with or entrapped into three different MLVs of neutral, cationic, and anionic liposome vesicles. For the preparation of neutral MLVs, phosphatidylcholine (PC) and cholesterol (CH) were used. For cationic and anionic MLVs, dioleoyl-trimethylammonium-propane and dimyristoyl glycerophosphate were added as surface charge inducers, respectively, in addition to PC and CH. Particle size of the three A2P-loaded MLVs was submicron, and polydispersity index revealed homogenous distribution of the prepared MLVs except neutral ones. Skin penetration study with hairless mouse skin showed that both physical mixtures of A2P with empty MLVs and A2P-loaded MLVs increased penetration of the drug compared to aqueous A2P solution. During the penetration, however, significant amount of the drug was metabolized into L-ascorbic acid, which has no beneficial effect on stimulation of hair growth. Out of the physical mixtures and A2P-loaded MLVs tested, physical mixture of A2P with empty cationic MLV resulted in the greatest skin penetration and retention in hairless mouse skin.
Yoo
Juno
J
College of Literature Science and the Arts, University of Michigan, Ann Arbor, MI, USA.
Shanmugam
Srinivasan
S
Song
Chung-Kil
CK
Kim
Dae-Duk
DD
Choi
Han-Gon
HG
Yong
Chul-Soon
CS
Woo
Jong-Soo
JS
Yoo
Bong Kyu
BK
D000814:Aniline Compounds / Q000737:chemistry; D000818:Animals; D001205:Ascorbic Acid / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D002627:Chemistry, Physical; D002784:Cholesterol / Q000737:chemistry; D002851:Chromatography, High Pressure Liquid; D004563:Electrochemistry; D005229:Fatty Acids, Monounsaturated / Q000737:chemistry; D054709:Lecithins / Q000737:chemistry; D008297:Male; D008567:Membranes, Artificial; D051379:Mice; D008812:Mice, Hairless; D010316:Particle Size; D010713:Phosphatidylcholines / Q000737:chemistry; D000644:Quaternary Ammonium Compounds / Q000737:chemistry; D012869:Skin Absorption / Q000187:drug effects*
D000814:Aniline Compounds; D005229:Fatty Acids, Monounsaturated; D054709:Lecithins; D008567:Membranes, Artificial; D010713:Phosphatidylcholines; D000644:Quaternary Ammonium Compounds; C011669:ascorbate-2-phosphate; C050795:N,N-dimethyl-4-anisidine; D002784:Cholesterol; C070046:1,2-dioleoyloxy-3-(trimethylammonium)propane; D001205:Ascorbic Acid