ABSTRACT
OBJECTIVE：To study the effects of different penetration enhancers on in vitro transdermal permeation of Flavaspidic acid BB cream. METHODS ：Flavaspidic acid BB cream was prepared ，containing 11 kinds of different penetration enhancers as 1％ azone，2％ azone，3％ azone，4％ azone，1％ menthol，1％ propylene glycol ，1％ oleic acid ，1％ azone+1％ menthol，1％ azone+1％ propanediol，1％ azone+1％ oleic acid or 1％ menthol+1％ propanediol. Modified Franz diffusion cell was adopted using abdominal skin of isolated male rat as transdermal barrier. The content of flavaspidic acid BB was determined by UPLC. The accumulative transdermal amount （Q24 h）and percutaneous permeability （Jss）within 24 h were calculated ；and compared with Flavaspidic acid BB cream without transdermal enhancer ，the enhancement ratio （ER）was calculated. RESULTS ： Q24 h of Flavaspidic acid BB cream with above 11 kinds of transdermal enhancers were （82.96±7.15），（80.17±0.66），（78.22± 1.87），（73.53±1.24），（35.65±2.23），（34.02±1.73），（42.68±2.66），（33.94±1.37），（34.16±1.54），（46.78±1.21），（43.66±1.69） μg/cm2，respectively. Jss value were （5.26±0.10），（4.69±0.12），（4.45±0.45），（4.00±0.06），（3.74±0.33），（3.23±0.18）， （3.73±0.53），（3.14±0.47），（3.54±0.11），（3.98±0.34），（4.34±0.14）μg（/ cm2·h），respectively. ER were 2.055，1.831，1.738， 1.564，1.462，1.263，1.456，1.227，1.385，1.557，1.698，respectively. CONCLUSIONS ：All of the above transdermal absorption enhancers can enhance the percutaneous absorption of Flavaspidic acid BB cream ，among which ，1％ azone is the best.
ABSTRACT
Objective To prepare a novel drug delivery system camptothecin loaded nanogel (CPT-PPO gel),and inves-tigate its contents,physical and chemical properties and in vitro transdermal permeability.Methods The solvent evaporation method was utilized to prepare core-shell nano-drug delivery systems (CPT-PLGA-PAMAM,CPT-PP),in which the Poly lac-tic-co-glycolic acid (PLGA ) was used to load camptothecin as the nucleus and the polyamidoamine (PAMAM ) G3.0 was wrapped in the surface of PLGA as the shell.Then the oleic acid (OA) was connected to CPT-PP to obtain the surface modified drug delivery system (CPT-PLGA-PAMAM OA,CPT-PPO).HPLC was used to determine the content of camptothecin in nanoparticles,transmission electron microscopy was applied to identify the nanoparticles morphology,and laser analyzer was used to determine the particle size.The hydroxypropyl methylcellulose (HPMC) was added as the base for the preparation of the nanogel (CPT-PPO gel) at last.The Franz-diffusion cell was used to determine the permeation rate of nanogel in vitro. Results The resulting CPT-PPO gel was stable at 4℃,the average particle size was (246.7 ± 5.4) nm and the encapsulation efficiency was up to (78.7 ± 6.9)%.Comparing to the normal gel,(CPT gel),the cumulative penetration amount and the re-tention amount in the skin of the nanogels (CPT-PPO gel,CPT-PP gel) were significant higher (P＜0.01),the retention and cumulative penetration amount of CPT-PPO gel was significant higher than that of CPT-PP gel (P＜0.05).Conclusion After modified by OA,CPT-PPO gel can increase the cumulated amount and absorption in skin and can be used as a carrier of CPT in the new formulation for topical treatment of psoriasis.
ABSTRACT
OBJECTIVE:To study the effects of common percutaneous enhancers on transdermal permeability of cetirizine hy-drochloride(CET). METHODS:Using pH 7.4 phosphate buffer as receiving solution,accumulative permeation rate as index,mod-ified Franz diffusion cell was used to investigate the effects of common percutaneous enhancers on transdermal permeability of CET in skin of abdomen isolated from mice,such as azone (0.06%-2.5%),oleic acid (0.5%-10%),1,3-propanediol (0.5%-10%),propanetriol(0.5%-5%). RESULTS:1,3- propanediol had no improvement effect on the permeability of CET. 24 h accu-mulative permeation amount of CET in 0.06% azone,0.5% oleic acid and 1% propanetriol were the highest among same types, being 227.94,85.25 and 215.15 μg/cm2,respectively. CONCLUSIONS:Of four percutaneous enhancers,the transdermal enhanc-ing efficiencies from high to low are azone>glycerol>oleic acid>1,3-propanediol. Azone and glycerol have the conspicuous pene-tration enhancing effects.
ABSTRACT
Objective: To compare the differences in transdermal permeability, pharmacodynamics, and skin irritation of Guanjie Zhitong Patches based on two different formulations taking hot-melt pressure sensitive adhesive and rubber as matrixes. Methods: In vitro transdermal permeation was performed by means of Franz diffusion cells; The analgesic effect was evaluated by HAc-induced writhing response in mice and hot-plate test, while the anti-inflammatory action was assessed by xylem-induced ear edema in mice and albumin-induced paw edema in rats. The skin irritation of the two matrixes was investigated using guinea pig as model animal. Results: Patches based on hot-melt pressure sensitive adhesives showed better transdermal permeability, analgesic, and anti-inflammatory effects but less skin irritation than the rubber type patches. Conclusion: Hot-melt pressure sensitive adhesive is a kind of appropriate material to compose the patch matrix for Chinese herbal medicine, which has the good transdermal permeability and efficacy and less skin irritation.
ABSTRACT
Objective: To investigate the effect of different animal's skin and different concentration of one penetration enhancer on the transdermal permeability of Xiaoer Fuxie Navel Plaster. Methods: Using Franz diffusion cell and HPLC, and taking psoralen and isopsoralen as index components, the differences in transdermal permeability of abdominal skin of rats and rabbits, back skin of mice, and ear skin of pigs, and the effects of different concentration of 1%, 3%, and 5% of Azone on transdermal permeability of Xiaoer Fuxie Navel Plaster were compared and studied. Results: Abdominal skin of rats profited to the transdermal penetration of psoralen and isopsoralen, the 24 h-accumulated permeattion of both psoralen and isopsoralen reached the maximum and the penetration rate was the highest and the effect of penetration enhancers was the strongest at the concentration of 1% Azone. Conclusion: The transdermal effect of Xiaoer Fuxie Navel Plaster could be best when choosing 1% Azone as the penetration enhancer and abdominal skin of rats as screening model of penetration enhancer.
ABSTRACT
OBJECTIVE:To study the effect of five penetration enhancers on the transdermal permeability of sodium phenytoin in vitro.METHODS:Experiments were carried on penetration experimental facility using modified Franz-type horizontal diffusion cell with 0.9% sodium chloride as receptor solution.The content of sodium phenytoin in the receptor solution was determined by HPLC,and its accumulative permeation amounts and steady permeation rate were computed as well.The permeability of sodium phenytoin across the excised rat abdomen skin which has been pretreated with different penetration enhancers-ocenol(3%,5%,and 10%),menthol(3%,5%,and 8%),eucalyptus oil(0.5%,1%,and 3%),azone(1%,3%,and 5%) and N-methyl pyrolidone(3%,5%,and 8%) was observed.RESULTS:Five enhancers did improve the transdermal delivery of sodium phenytoin in a concentration dependent manner.At a respective optimum concentration,the permeation enhancing effects of enhancers in ascending order were 5% N-methyl pyrolidone
ABSTRACT
Objective To investigate the in-vitro transdermal permeability of cyclovirobuxine D ethosomes.Methods Ethosomes,liposomes,saturated aqueous solution and 35.5% saturated alcohol solution of cyclovirobuxine D were prepared.The in-vitro transdermal permeability of different kinds of preparations of cyclovirobuxine D was studied by in-vitro permeation experiments.Results Cyclovirobuxine D ethosomes enhanced transdermal flux rate of cyclovirobuxine D and the enhancement ratio was 8.85,superior to liposomes and saturate alcohol.The dermatic hold-up amount of cyclovirobuxine D in 35.5% saturated alcohol solution,liposomes and ethosomes was in a decreasing sequence.Conclusion Compared with the liposomes,the ethosomes can enhance the transdermal flux rate of cyclovirobuxine D,which could increase the systematic action of the drug.
ABSTRACT
Objective:To study the transdermal permeability of Psoralen (Pro) and Isopsoralen (Isopro). Methods:V C two compartment was adopted to research the permeability deferences between Pso and Isopso in nude mouse skin in vitro, and investigated the effect of penetration enhancers, such as EtOH, azone and glycerol on the permeability of them. Results: Pso and Isopso are suitable compounds for transdermal delivery system and the permeability coeffient of Isopso is larger than that of Pso. 10% EtOH-1% Azone greatly increased the permeability coefficient. Conclusion: The results can offer reference for Psoralea corylifolia TDS.