Study On Transdermal Permeability Of Essential Oil From Angelica Sinensis And Clove And Their Effects On Percutaneous Absorption Of Drugs In Vitro

ObjectiveTo study transdermal permeability of essential oil from Angelica Sinensis and its effect on percutaneous absorption of nimodipine. To investigate the mechanism of essential oil from Angelica Slinesis in enhancing the nimodipine through fetal skin.To study transdermal permeability of essential oil from Clove and its effect on percutaneous absorption of ibuprofen.Method1. To establish HPLC methods for determination of nimodipine and ligustilide which is the major constituent of essential oil from Angelica Sinensis. Rabbit skin and fetal skin were used as permeation barrier and nimodipine was selected as a model drug. The transdermal characteristics were investigated using Franz diffusion cell. To observe the morphology change in fetal skin of the experimental groups by scanning electron microscope and transmission electron microscope.2. To establish HPLC methods for determination of ibuprofen and eugenol which is the major constituent of essential oil from Clove. Rat skin and fetal skin were used as permeation barrier and ibuprofen was selected as a model drug. The transdermal characteristics were investigated using Franz diffusion cell.Results1. The calibration curve of ligustilide was liner in the range of 0.5000 80.00μg·mL^-1. The regression equation was Y = 45342 C– 8462 ( r = 0.9998). The relative recovery was 100.07%, the intra-day and inter-day reproducibility were good with the RSD of 1.2% or below.The calibration curve of nimodipine was liner in the range of 0.2760 55.20μg·mL^-1 The regression equation was Y = 75465 C– 12042 ( r = 0.9998). The relative recovery was 99.29%, the intra-day and inter-day reproducibility were good with the RSD of 2.8% or below.The permeability coefficients of the essential oil from Angelica Sinensis for the rabbit and fetal skins increased with the concentration enhancing. The essential oil from Angelica Sinensis had promotions actions on percutaneous absorption of nimodipine. 1.0% essential oil from Angelica Sinensis exhibited the greatest permeation enhancing effect. In addition, the permeability coefficients of nimodipine in 1.0% essential oil from Angelica Sinensis for the rabbit and fetal skins were 3.22 and 5.75 times as much as that in normal saline.The changes of fetal skin ultrastuctures by scanning electron microscope were as follows: the wrinkles of the skin surface were increased; some areas of stratum corneum were peeled off and wond up as worn-out cotton paddin; the spaces of the hair were enlarged; and the cuticles of the hair shaft dropped off and became thinner.The changes of fetal skin ultrastuctures by transmission electron microscope were as follows: stratum corneum cells were peeled off; the cell junction in basal lamina and stratum spinosum were broke; intercellular space were enlarged.2. The calibration curve of eugenol was liner in the range of 0.1100 110.0μg·mL^-1. The regression equation was Y = 17.74 C + 1.518 ( r = 0.9999 ). The relative recovery was 100.1%, the intra-day and inter-day reproducibility were good with the RSD of 2.7% or below.The calibration curve of ibuprofen was liner in the range of 0.5375 53.75μg·mL^-1 The regression equation was Y = 36.83C + 7.729 ( r = 0.9997 ). The relative recovery was 99.29%, the intra-day and inter-day reproducibility were good with the RSD of 2.9% or below.The permeability coefficients of the essential oil from Clove for the rat and fetal skins rose as the concentration of essential oil increased. The cumulate penetrated amount, penetrating rate, lag time of ibuprofen in 24h had no obvious difference by different concentrations of clove oil. The essential oil from Angelica Sinensis had no promotions actions on percutaneous absorption of ibuprofen obviously.Conclusions1. The essential oil from Angelic Sinesis could penetrate through rabbit and fetal skin. Essential oil from Angelica Sinensis can enhance the percutaneous absorption of nimodipine in vitro, among which 1.0% essential oil from Angelic Sinensis showed significant penetration enhancing effect.The mechanism of the essential oil from Angelica Sinensis enhancing the transdermal absorption of nimodipine was closely related to the changes of the epidermis ultrastuctures. Essential oil from Angelica Sinensis can discrupt the stratum corneum and enlarge the intercellular space that is in favour of drug transdermal permeability2. The essential oil from Clove could penetrate through rat and fetal skin. Essential oil from Clove can not enhance the percutaneous absorption of ibuprofen in vitro obviously.