Research On The Laws And Mechanisms Of Borneol On Promoting Penetration Of Different Traditional Chinese Medicine Ingredients

Transdermal drug delivery system has become one of the focus and hotspots of formulation development research.Due to the barrier function of the stratum comeum of the skin,the transdermal absorption of most drugs is difficult to meet the therapeutic needs.In order to achieve an effective level of drugs treatment of the transdermal formulation,it is often necessary to add a penetration enhancer to increase the level of transdermal permeation of the drugs.Bomeol is one of the commonly used traditional Chinese medicine volatile oils and has a broad market prospect.The 2015 edition of the Chinese Pharmacopoeia contains three kinds of bomeol:natural bomeol,blumea camphor and synthetic borneol.Whether the performance of these three kinds of borneol as a transdermal penetration enhancer is different,there is still no systematic research,and it is difficult to effectively guide its clinical application.To this end,this paper investigated the safety of three kinds of borneol using cell models and skin tissue,studied the penetration law of different properties of drugs using transdermal experiments in vitro,and explored its penetration mechanism using computer simulation and classical experiments.The main contents are as follows:1.Study on the safety of different bomeolIn this paper,skin cells and skin tissues were used to investigate the effects of three kinds of borneol on skin cytotoxicity and their effects on skin tissue morphology.The results showed that the effects of natural borneol,blumea camphor and synthetic borneol on skin cells and skin tissue were not significant,and th eir irritation to skin was small,indicating that these three kinds of borneol had high safety as a penetration enhancer.The results provided data support for their rational application in transdermal formulations.2.Study on the penetration effects and penetration law of different bomeolIn this paper,traditional Chinese medicines with different LogP values and different molecular weights were used as research carriers to evaluate the difference in the penetration effects of three kinds of borneol on different drugs,and the penetration law of different bomeol was summarized.The results showed that natural bomeol,blumea camphor and synthetic borneol had certain penetration effects on the different properties of the drugs,indicating that these borneol could be used as transdermal penetration enhancers.There was a certain difference in the penetration effects of drugs for these borneol,but the penetration law was similar.In general,the penetration effects of these borneol on hydrophilic drugs or drugs with large molecular weight were more significant.The above results could be used to predict the effect of borneol on the penetration effects of the drugs,and provided guidance for the selection of the penetration enhancers for the development of transdermal formulations.3.Study on the penetration mechanism of borneolIn this paper,classical experiments and computer simulation methods were used to investigate the effects of borneol on the structure and properties of the lipid bilayer membrane of the drugs,and to explore the intrinsic mechanism which borneol had more significant penetration effects for the hydrophilic drugs or drugs with larger molecular weight.The results showed that borneol disrupted the orderly arrangement of the stratum corneum lipids by disturbing the order parameters of the ceramide A chain,B chain and free fatty acid molecules in the stratum corneum lipids,and promoted by increasing the diffusion coefficient of the drugs.Through the above research,the intrinsic mechanism of the interaction between transdermal penetration enhancer,drugs and skin was deeply explored from the macroscopic and mesoscopic scales.The molecular mechanism of borneol was preliminarily explained,which provided guidance for further research and application.In summary,this paper investigated the safety of three kinds of borneol,studied the penetration effects and the penetration law of borneol on the different traditional Chinese medicine,and explored the penetration mechanism of borneol.The results of the study provided scientific guidance for the use of borneol as a transdermal penetration enhancer.At the same time,it also provided a method for screening transdermal penetration enhancers during the development of transdermal preparations,and promoted the research and development of transdermal preparations for Chinese traditional medicines.