Drug Release Under The Law Of Percutaneous - "ethosomes Microneedle Arrays" Combined Gentiana Gentiopicroside

Compared with the main traditional Chinese medicine clinical delivery systems(oral, injection), topical transdermal drug delivery, can avoid the first pass effect, drug release Stability, and can reduce the liver and other organs damage, but it have abuse such as insufficient dosage and the low efficiency of the drawbacks of transdermal drug delivery, thus impeding the development and application of topical transdermal drug system. Therefore, how to improve the drug percutaneous absorption efficiency has becomed a research focus in Chinese medicine transdermal drug delivery system.Inspired by the administration ideas of "effective integration" of ancient effective way of clinical dosage of traditional Chinese medicine,such as Bai Jiang Dan point classified method and traditional treatment "Gua Sha" with medicated wine, at the same time,in view of the characteristics that oil/water distribution of the two barrier of cuticle lipophilic layer and hydrophilic epidermis activity skin layer in the model theory of the skin;our group has proposed a new topical combined with micro needle array and the hydrophilic drug carrier for transdermal drug delivery sytem. According to the difference release characteristics of cuticle lipophilic layer and hydrophilic epidermis activity skin layer, we break the physical and lipid barrier of the stratm corneum with micro needle, and then use the hydrophilic characteristics of ethosomes to carry drug, that based on the principle of "similar miscibility"to make the drug flux into active cuticular layer, so as to improve the transdermal effect of drugs.The contents of this thesis as follows:1.The experiment established the method that determining the content of gentio picroside in radix gentianae macrophyllae extract by HPLC; Through the single factor investigation and star design-response surface method to optimize the extraction process of gentio picroside in radix gentiana macrophylla.To investigate the effects of gentio picroside transdermal delivery in vitro under difference shapes, lengths, pretreatment pressure and time of micro needle.2.Gentio picroside will be prepared into ethosomes. Encapsulation efficiency as the indexes and optimizing of preparation process; through studied the quality of ethosomes to determine the best method for preparing ethosomes, it was inject-ultrasonic bonding.The best preparation process is the hydration temperature35℃,hydration time30min, homogeneous time5min,ultrasonic time5min.3.To study the effect of Gentio picroside transdermal drug delivery in vitro under different combinations of "micro needle array-ethosomes" that were made up with different micro needle arrays and differen alcohol of ethosomes, and obtain the best administration conditions of "microneedle array-ethosomes.Under this condition, compared with gentio picroside in aqueous solution of passive administration,this combination regimen that drug24hours cumulative penetration amount was increased about81times.In addition, through the skin tissue slice of experiment, it was found that this way of combination can open skin stratum corneum lipotropy barrier in the process of drug delivery, the drug gentio picroside was transported to the dermis with hydrophilic activity primarily by the hydrophilic characteristics ethosomes, so as to improve drug accumulated permeation amount.4.Investigated the anti-inflammation and analgesic action of gentio picroside under the combination of "microneedle arrays-ethosomes", that was found that this combination administration can significantly improve the action of anti-inflammatory and analgesic of gentio picroside.Through this research, it was found that the combination of "micro needle array-ethosomes" were made full use of the distinct nature of the two layers of the skin barrier to give medication, significantly improved the efficiency of the percutaneous absorption of drugs and realized the big flux of drug percutaneous drug release.It will be a new and efficient way of release, which can make drugs with small doses of the clinical efficacy of percutaneous absorption and play to drugs,and overcome the conventional way of transdermal drug release release quantity shortage and low bioavailability of bottleneck; the This ideas and methods of combination, will promote the application and development of transdermal drug delivery systems.