Morphological effect of lipid carriers on permeation of lidocaine hydrochloride through lipid membranes.
We have studied how the transdermal delivery of lidocaine hydrochloride (LHC) is affected by the morphology of lipid carriers, liposomes and micelles, having the same lipid composition of 1-stearoyl-sn-glycero-3-phosphocholine (LPC) and cholesteryl hemisuccinate (CHEMS). In vitro drug permeation study, carried out on guinea pig skin, has revealed that the liposomes made of LPC and CHEMS significantly enhance the permeation rate of entrapped LHC; by contrast, the mixed micelles with the same composition decrease the degree of delivering co-existing LHC. Basically, we have also investigated the release kinetics of LHC through the cellulose membrane and found that both liposomes and micelles have a similar releasing profile. To experimentally demonstrate this unique behavior, we have observed the fluidity of stratum corneum liposomal membranes in the presence of either our liposomes or micelles. From this study, we have found that LPC/CHEMS liposomes fluidize the lipid membrane of stratum corneum lipids; however, lipid micelles rather make the membrane rigid. These findings highlight that controlling the morphology of drug carriers provides us with a means to modulate the permeability of encapsulated drug molecules.
Shim
Jongwon
J
Amorepacific Corporation R&D Center, 314-1, Bora-ri, Giheug-eup, Yeongin-si, Gyeonggi-do 446-729, Republic of Korea.
Kim
Mi Jin
MJ
Kim
Han-Kon
HK
Kim
Do-Hoon
DH
Oh
Seong Geun
SG
Ko
Seung Yong
SY
Jang
Ho Gyeom
HG
Kim
Jin-Woong
JW
D000279:Administration, Cutaneous; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods; D002788:Cholesterol Esters / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D008012:Lidocaine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008081:Liposomes; D008244:Lysophosphatidylcholines / Q000737:chemistry; D008563:Membrane Lipids / Q000378:metabolism; D008823:Micelles; D010539:Permeability; D012867:Skin / Q000187:drug effects / Q000378:metabolism; D012869:Skin Absorption
D002788:Cholesterol Esters; D004337:Drug Carriers; D008081:Liposomes; D008244:Lysophosphatidylcholines; D008563:Membrane Lipids; D008823:Micelles; C026564:stearoyl alpha-lysolecithin; D008012:Lidocaine; C013440:cholesteryl succinate