Chronic Toxicity of Triptolide and Ferulic Acid Ethosomes Gel for Percutaneous Administration / 中国实验方剂学杂志

ObjectiveTo investigate the long-term safety of triptolide ferulic acid ethosome gel in percutaneous administration. MethodWe mixed triptolide with ferulic acid to make liposomes gel in different doses and then administrated the gel to SD rats of both sexes with intact skin and damaged skin for 12 weeks. The daily dosages calculated based on triptolide for the low-， middle-， and high-dose groups were 63.75， 127.50， 255.00 μg·kg-1， respectively. The body weight of each rat was measured weekly. The rats were sacrificed in the last week for the determination of serum biochemical parameters and organ indexes as well as the observation of histopathology. The toxicity was assessed based on the body weight and all the parameters and indexes. ResultAfter long-term administration， the body weight and serum biochemical parameters did not show significant difference between the gel-treated groups and the blank group with intact skin， which indicated that the percutaneous administration of triptolide and ferulic acid ethosomes gel was relatively safe. However， the rats in the high-dose group showed sparse hair and were easy to die in the case of unhairing with chloral hydrate at the late stage of the study. Comprared with the female rats with intact skin in the blank control group， the female rats with damaged skin in the middle-dose group showed decreased heart index （P<0.05）， which indicated certain cardiotoxicity. Moreover， damage appeared in skin and lung， which may be influeneced by dosage， sex， and skin state. ConclusionFerulic acid in combination with triptolide is relatively safe for percutaneous administration， whereas there are some risks of skin and lung damage in the case of long-term administration. Individualized administration scheme should be developed according to liver and kidney function and skin conditons to ensure the safety of clinical medication.

Preparation of dl-tetrahydropalmatine ethosomes and their ex vivo transdermal permeation properties / 中草药

Objective To prepare dl-tetrahydropalmatine (dl-THP) ethosomes (ETS) and elucidate their transdermal absorption properties. Methods Dl-tetrahydropalmatine ethosomes (dl-THP ETS) were prepared by ethanol injection combined with pH-gradient active drug-loading method. Their physicochemical properties including elasticity, vesicle size, morphology and entrapment efficiency were characterized. Franz diffusion cells were used to investigate the ex vivo skin permeation characteristics of the formulation with liposomes (LPS) and tinctures being used as reference preparations. Results According to a preferred formulation of dl-THP ETS [dl-THP 100 mg, vitamin E 1.3 mg, soybean lecithin 1 200 mg, cholesterol 120 mg, absolute ethanol 9 mL and citrate buffered saline (pH 3.0) 21 mL, 0.1 mol/L NaOH solution suitable quantity (to adjust the pH value to 5.5) ], the obtained dl-THP ETS had an elasticity index of (20.1 ± 1.1) mL, an average size of (85.8 ± 0.9) nm with a polydispersity index of (0.082 ± 0.003) and an entrapment efficiency of (81.7 ± 3.2)%. The cumulative permeated drug quantity per unit area (Qn) of dl-THP ETS in 24 h was (2 306.4 ± 592.3) μg/cm2 with no significant difference compared with the Qn of the LPS [(2 434.2 ± 564.4) μg/cm2] (P > 0.05) and about 4 times of that of the tincture [(633.1 ± 218.0) μg/cm2] (P < 0.05). And the averages of RSD of the Qn at each time point were (28.37 ± 10.9)% and (62.83 ± 44.1)% for the ETS and LPS, respectively, indicating that the Qn fluctuation among samples of the ETS was smaller than that of the LPS (P < 0.05). Average correlation coefficients of (0.968 ± 0.033) and (0.882 ± 0.078) (P < 0.05) were obtained for the ETS and LPS respectively when their 24 h permeation curves were fitted to linear relationship, indicating the permeation of the former was closer to zero-order kinetics than that of the latter. Conclusion The dl-THP ETS have a high elasticity, a suitable size, a high entrapment efficiency, and enhanced and stable percutaneous absorption in line with zero-order kinetics.

Optimization of Preparation Technology of Tetracaine Hydrochloride Ethosomes / 中国药房

OBJECTIVE： To establish a method for determining the content of tetracaine hydrochloride （TCH） ethosomes， and to optimize the preparation technology. METHODS： The content of TCH was determined by HPLC. TCH ethosomes were prepared with injection-ultrasonic method. Using drug-loading amount， egg lecithin concentration and ethanol volume fraction as factor， encapsulation efficiency as index， central composite design-response surface methodology was used to optimize the prescription based on the single factor test. The prepared ethosomes were characterized and the stability was evaluated. RESULTS： The linear range of TCH was 10-100 μg/mL （r＝0.999 5）； the limit of quantification was 0.045 μg/mL， and detection limit was 0.021 μg/mL. RSD of precision， stability and repeatability tests were less than 2％. The recoveries ranged 97.80％-103.20％ （RSD＝0.36％， n＝9）. The optimal preparation technology included that the adding amount of TCH control was 1 mg； the concentration of egg lecithin was 7 mg/mL， and ethanol volume fraction was 33％. Under this technology， the average encapsulation efficiency was 64.50％ （n＝3）， the relative error of which from the predicted value （64.92％） was 0.64％. TCH ethosome was a clear blue liquid with a blue opalescence. Its appearance was spherical， its shape was round， smooth， uniform in size； the average particle size was （80.33±2.24） nm， and the average Zeta potential was （－22.6±1.33） mV. TCH ethosome was stable during 10 days under 4 ℃， sealed and protected from light. CONCLUSIONS： The optimal preparation process is stable and feasible. Established method is simple and rapid.

Preparation and evaluation of triptolide and ferulic acid ethosomes / 中草药

Objective In order to optimize the preparation technology of triptolide and ferulic acid ethosomes and evaluate its characteristics of the in vitro transdermal penetration and the preparations performance using ethosome as carrier. Methods The compatibility ratio between triptolide and ferulic acid was determined by MTT. The triptolide and ferulic acid ethosomes were prepared with injection method based on the results of single factor experiments, Box-Behnken design was used to optimize the particle size, electric potential, and encapsulation efficiency (EE) of the ethosomes, and the in vitro release behavior prepared by the optimal formulation were studied. The in vitro transdermal absorption experiment was carried out in optimized Franz diffusion cells. Results The ratio of triptolide to ferulic acid was 1:100. The optimized prescription of the ethosomes was 20% ethanol, 2.2% phospholipid, 90 s ultrasonic time. The results showed that the appearance of the triptolide and ferulic acid ethosomes was clear liquid with blue opalescence in an average diameter of (46.75 ± 2.39) nm at potential of (-46.32 ± 3.76) mV, and the EE was (67.72 ± 1.10)%. The in vitro transdermal behaviors of ferulic acid and triptolide in the ethosomes were in line with the Higuchi equation. Conclusion The ethosomes has the advantages of small particle size, uniform distribution, good stability, and good transdermal absorption property, so as to provide the basis for the development of the transdermal preparation of the effective components of Tripterygium wilfordii.

Preparation and transdermal permeation of triptolide and ferulic acid ethosomes gel / 中国中药杂志

The aim of this study was to prepare triptolide and ferulic acid ethosomes gel, investigate its transdermal permeation, and compare the results with ordinary gel and cream. Improved Franz diffusion cell method was used in the transdermal delivery experiment with rat abdominal skin as in vitro model. The receptor fluid at different time points was collected; ferulic acid concentration was determined by high performance liquid chromatography (HPLC) and triptolide concentration was determined by liquid chromatography-electrospray ionization mass spectrometry (LC-MS/MS). Then the penetration rate, transdermal volume and skin reserve of three dosage forms (hydroplasy gel, ordinary gel, and cream) to investigate the transdermal properties of ferulic acid and triptolide in vitro of triptolide and ferulic acid ethosomes gel. The results showed that the steady penetration rate of ferulic acid was 5.268 5, 8.990 9, 12.042 0 μg·cm⁻² ·h⁻¹ respectively in triptolide and ferulic acid ethosomes gel, ordinary gel and cream; the skin retention was (30.234 8±1.525 4), (20.402 6±0.402 6), (7.635 3±1.094 2) μg·cm⁻² . The steady-state permeation rate of triptolide was 67.238 0, 67.238 0 ng·cm⁻² ·h⁻¹ in triptolide and ferulic acid ethosomes gel, about 1.24 times of cream and 3.28 times of ordinary gel; the skin retention was (371.351 4±35.317 1) ng·cm⁻², about 3.35 times of cream and 5.25 times of ordinary gel. Therefore, the ethosomes gel showed good transdermal absorption property and it may be good for clinical safety administration.

Evaluation on Transdermal Absorption Properties and Efficacy of Huoxue Zhitong ;Cataplasm / 中国中医药信息杂志

Objective To study the effects of microemulsion/ethosomes on transdermal absorption properties and efficacy of Huoxue Zhitong Cataplasm. Methods The improved Franz diffusion cells were used for the in-vitro permeation experiment with rat skins as the barriers, which was used to evaluate the transdermal absorption properties. In the erxeriment, the contents of paeonol, eugenol and methyl salicylate were used as markers, and detected by ultra performance liquid chromatography to evaluate the transdermal absorption effects. The anti-inflammatory and analgesia activity were evaluated through the writhing plate experiments. Results The cumulative release rate of paeonol in Huoxue Zhitong Cataplasm, Microemulsion Huoxue Zhitong Cataplasm and Ethosomes Huoxue Zhitong Cataplasm were, in order, 65.30%, 61.30%and 60.20%in 24 h;eugenol were, in order, 51.08%, 54.71% and 55.66% in 24 h; methyl salicylate were, in order, 49.20%, 65.17% and 72.15% in 24 h. Furthermore, Microemulsion Huoxue Zhitong Cataplasm high-dose group and Ethosomes Huoxue Zhitong Cataplasm medium-dose group had good effects on reducing the inflammatory exudate of peritoneal capillary and capillary permeability (P<0.05) in animal models. Conclusion Huoxue Zhitong Cataplasm based on microemulsion/ethosomesnano-technology has good transdermal absorption properties and efficacy.

Application of New Carriers in Transdermal Drug Delivery System / 中国药师

Compared with traditional oral administration and parenteral administration, transdermal administration has such fea-tures as convenient application, high local drug concentration and strong security. This paper reviewed the composition, characteristics and applications of new carriers ( microemulsions, ethosomes, transfersomes, niosomes, proliposomes, gels and so on) in transdermal drug delivery system with increased drug transdermal transport efficiency in recent years. The advantages of the new transdermal drug delivery carriers make them possess high research value and broad development space.

In vitro and in vivo Transdermal Penetration of Testosterone Undecanoate Binary Ethosomes Gel / 中国药师

Objective:To study the in vitro and in vivo transdermal penetration of testosterone undecanoate ( TU) binary ethosomes gel. Methods:TU binary ethosomes were prepared by an ethanol injection method, and using carbopol 941 as the gel base, TU binary ethosomes gel was prepared. Using mouse skin as the barrier, Franz cells were applied to explore the in vitro transdermal penetration of TU binary ethosomes and the gel. Rats were used as the animals, and TU binary ethosomes and the gel was respectively administrated on the back skin. At the predetermined time points, plasma samples were withdrawn to detect the concentration of TU, and the main pharmacokinetics parameters were calculated. Results: The in vitro transdermal penetration of TU binary ethosomes and the gel was both fitted first-order equation:Q=8. 68t+6. 78(r=0. 998 2) and Q=6. 09t+3. 09(r=0. 999 3), and the stable penetration rate was 8. 68 μg·cm-2 ·h-1 and 6. 09μg·cm-2 ·h-1 , respectively. After the 24-hour penetration, the residual amount in skin of TU binary ethosomes and the gel was (208. 80 ± 55. 26)μg·g-1 and (225. 60 ± 38. 90)μg·g-1 , respectively. The main pharmacokinet-ics parameters of TU binary ethosomes and the gel were Cmax of(18.50 ±2.75)mg·L-1 and(20.80 ±2.42)mg·L-1, tmax of(6.20 ± 0. 14)h and(9. 54 ± 0. 52)h, and AUC0-48h of(336. 74 ± 2. 05)h and(486. 30 ± 1. 68)h. Conclusion:TU binary ethosomes and the gel both exhibit promising in vitro transdermal penetration, and the gel shows better sustained release property.

Ethosomes as Novel Drug Delivery System: A Review.

The ethosomes are vesicular carrier comprise of hydroalcoholic or hydro/alcoholic/glycolic phospholipid in which the concentration of alcohols or their combination is relatively high. To provide continuous drug infusion through an intact skin, several transdermal therapeutic systems have been developed for topical application onto the intact skin surface to control the delivery of drug and its subsequent permeation through the skin tissue. Transdermal route is promising alternative to drug delivery for systemic effect. An attempt was made to formulate the highly efficient ethosomal drug delivery system and enalapril meleate is used as model drug. The following conclusion are drown from the result and discussion described in the previous chapter. Liposomal formulation was also prepared by the thin film hydration method. The techniques used were simple and reproducible. The prepared ethosomes were spherical and discrete in shape. The size of vesicles were found to be in the range of 3.26-5.79 tim,o.716-1.3o1 tim and 5.32 tim for unsonicated ethosomes, sonicated ethosomes and liposomes respectively. However ethosomes prepared by sonication method were more uniform and smaller in size, which is essential for skin permeation. While comparing the entrapment efficiency, ethosomes containing 3o% w/w ethanol and prepared by sonication showed highest value with respect to all other formulation, so it is concluded ethosomes prepared by sonication and containing 3o% w/w ethanol as the best formulation considering all other aspects. The highest value of transdermal flux for sonicated ethosomes containing 3o% w/w ethanol is the indication of complete and rapid penetration through the skin may be because of tiny vesicular size.

Comparison of Transdermal Penetration of Two New Kinds of Triamcinolone Acetonide Lipid Carriers / 医药导报

Objective To compare transdermal penetration of triamcinolone acetonide liposparticles (TAA-LPPs) and TAA-Ethosomes in vitro. Methods The TAA-LPPs and TAA-Ethosomes were produced and the morphology was observed by transmission electron microscope,particle size was detected by laser particle analyzer. The percutaneous permeability in vitro was tested by modified Franz diffusion pools. The amount of penetrated triamcinolone acetonide and the retention in the skin were de-termined by HPLC. Results The shape of TAA-LPPs and TAA-Ethosomes was almost spherical with mean diameter of (99. 9±1. 3) and (105±1. 4) nm, respectively. The cumulative transdermal penetration of TAA-LPPs, TAA-Ethosomess and TAA suspension was (53. 59±4. 40),(87. 03±4. 87),and (30. 54±8. 61) μg·(cm2 ) -1 , respectively . The drug retention in the skin after 32 h was (1. 02±0. 13), (0. 62±0. 08), (0. 55±0. 17) μg·(cm2 ) -1 , respectively. Conclusion TAA-LPPs is better for transdermal administration of triamcinolone acetonide by reducing systemic absorption of the drug.

Determination of Entrapment Efficiency of Loratadine Binary Ethosomes by Sephadex Microcolumn Com-bined with HPLC / 中国药师

Objective:To establish a method to determine the entrapment efficiency of loratadine binary ethosomes. Methods:The gel microcolumn centrifugation method was employed to separate the free drug from loratadine binary ethosomes. The content of lorata-dine was determined by HPLC to calculate the entrapment efficiency. Results: A calibration linear curve of loratadine concentration was within the range of 10. 2-102. 0 μg·ml-1(r=0. 999 5). The average entrapment efficiencies of three batches of loratadine binary ethosomes were 86. 75%, 87. 26% and 86. 00%, respectively. Conclusion:The method is simple and rapid, and can be used to de-termine the entrapment efficiency of loratadine binary ethosomes accurately.

Study on Preparation of Celastrol Ethosome and Its Skin Penetration Properties in Vitro / 广州中医药大学学报

Objective To prepare celastrol ethosomes and to observe the permeability characteristics of the ethosomes which act as the transdermal delivery carriers of celastrol in vitro. Methods Celastrol ethosomes were prepared by ethanol injection method, and then the encapsulation efficiency, particle size, polydispersity index ( PDI) and zeta potential of the ethosomes were analyzed. TP2A intelligent percutaneous penetration instrument was used to compare the skin penetration properties of celastrol ethosomes, celastrol solution and the mixture of blank ethosomes with celastrol solution. Results The prepared celastrol ethosomes were spherical, and the average particle size was (401.3 ± 5.5) nm, PDI was 0.21± 0.02, steady zeta potential was (-2.75 ± 0.1) mV, and average encapsulation efficiency was ( 80.6 ± 0.7) %. The amount of accumulative penetration of celastrol ethosomes at 48 h was 76.86 μg·cm -2 and the permeation rate was 1.640 9 μg·cm -2·h -1, which were significantly higher than the celastrol solution and the mixture of blank ethosomes with celastrol solution. Conclusion The prepared ethosomes have high encapsulation efficiency, uniform particle size and stable quality, and are beneficial to the transdermal absorption of celastrol.

Application of Novel Liposomes in Transdermal Drug Delivery System / 中国药师

The stratum corneum barrier and the other issues in transdermal drug delivery system have attracted more and more at-tention, and the novel liposomes as the drug delivery vehicles effectively solve the problems. The novel liposomes can significantly im-prove transdermal drug penetration, therefore, can enhance efficacy and shows high application value and development prospects. In the paper, combined with some domestic and foreign current researches, the classification, penetration mechanisms and application of the novel liposomes were reviewed.

Formula Optimization and Quality Evaluation of Testosterone Undecanoate Binary Ethosomes / 中国药师

To screen the optimal formula and evaluate the quality of testosterone undecanoate ( TU) binary ethosomes to lay the foundation for the transdermal delivery system of TU. Methods:The mixture of ethanol and propylene glycol was used as the softeners, and TU binary ethosomes were prepared by ethanol injection method. The ratio of TU to lipids ( A) , the quality percentage of the mixture of ethanol and propylene glycol ( B) and the ratio of ethanol to propylene glycol ( C) as the influencing factors, and the entrapment efficiency as the index, an orthogonal test was used to optimize the formula of TU binary ethosomes. The morphology, size, zeta potential, in vitro drug release and stability of TU binary ethosomes were studied. Results:The optimal formula of TU binary etho-somes were as follows:the ratio of TU to lipids was 1∶15, the quality percentage of the mixture of ethanol and propylene glycol was 10% and the ratio of propylene glycol to ethanol was 6∶4. The optimal TU binary ethosomes were concentric circles under an optical microscope with uniform size, and the average size was (185. 5 ± 52. 8)nm, zeta potential was ( -15. 87 ± 0. 26)mV, and the entrap-ment efficiency was (79. 14 ± 0. 66)%. TU release from the binary ethosomes in vitro was fitted the first-order equation:Q=20. 79t-11. 01 (r2 =0. 998 4). Under the high temperature, the entrapment efficiency was decreased significantly, while under the other test conditions, all the indices of TU binary ethosomes showed no significant difference. Conclusion:The optimal TU binary ethosomes are easy to be prepared with promising quality and sustained release property in vitro, which are valuable to be studied further.

Preparation of colchicine ethosomes containing TPGS and in vitro transdermal permeation / 中草药

Objective: To prepare and optimize the prescription of colchicine ethosomes containing D-α-tocopherol polyethylene glycol 1000 succinate (TPGS) and to investigate its feasibility as a carrier for transdermal drug delivery. Methods: The colchicine ethosomes containing TPGS were prepared by the injection-sonication method. And the encapsulation efficiency (EE) was determined by minicolumn centrifugation method. The prescription of ethosomes was optimized by uniform design with EE as the evaluation index, and the physicochemical properties of the optimized ethosomes were investigated. Characterization of the vesicles was based on particle size, Zeta potential, entrapment efficiency, and transmission electron microscopy (TEM). The transdermal permeation characteristics of ethosomes, colchicine 30% ethanol solution, and colchicine ethosomes containing TPGS were compared by using Franz diffusion cells. Results: The optimized formulation was as follows: The contents of soybean phospholipid and TPGS were 350 and 50 mg, respectively. In addition, the concentration of ethanol was 36.44%. The average EE, particle size, polydispersity index, and Zeta potential were (74.71 ± 2.18)%, (89.6 ± 3.5) nm, 0.201 ± 0.008, and (-34.6 ± 2.7) mV, respectively. The in vitro experiment showed that the transdermal flux, permeation rate, and skin deposition of colchicine ethosomes were (64.49 ± 5.61) μg/cm2, (2.84 ± 0.23) μg/(cm2∙h), (128.22 ± 11.64) μg/cm2, and the transdermal flux, permeation rate, and skin deposition of colchicine ethosomes containing TPGS were (91.36 ± 7.11) μg/cm2, (4.73 ± 0.38) μg/(cm2∙h), and (182.84 ± 14.37) μg/cm2, respectively, which was significantly higher than those in ethosomes. Conclusion: The colchicine ethosomes containing TPGS show high EE and obviously enhance the percutaneous absorption of colchicine, which might be a potential carrier for transdermal drug delivery.

Study on preparation and in vitro transdermal penetration of betulinic acid ethosomes modified by sodium deoxycholate / 中草药

Objective: To prepare and optimize the prescription of betulinic acid (BA) ethosomes modified by sodium deoxycholate (SDC) and then to investigate its transdermal penetration as carrier of BA. Methods: The BA ethosomes modified by SDC were prepared by the ethanol injection method. The encapsulation efficiency (EE) was considered as the evaluation index to optimize the prescription of the ethosomes by orthogonal design, and the shape and particle size of the optimized ethosomes were analyzed. The in vitro transdermal absorption of BA was evaluated using Franz diffusion cells. The accumulated permeation amounts and permeation rate of liposomes, ethosomes, and BA ethosomes modified by SDC were compared. Results: The best formulation consisted of soybean lecithin-SDC-BC (18:1:1) and 35% ethanol. The average EE and the particle size were (93.8 ± 1.6)% and (102.3 ± 3.6) nm, respectively. The accumulated permeation amount of BA ethosomes modified by SDC in 12 h was (99.62 ± 9.44) μg/cm2, which was 1.67, 3.85, and 8.33 times of ethosomes, liposomes, and satuated solution containing 10% isopropanol, respectively. Conclusion: The BA ethosomes, modified by SDC with high EE, obviously enhance the percutaneous absorption of BA and might be one of the most perspective percutaneous preparations.

Preparation of ethosomes-based gel of demethylzeylasteral and its transdermal behavior in vitro / 中草药

Objective: To prepare the ethosomes-based gel of demethylzeylasteral (DMZ) and to investigate its properties and transdermal absorption behavior. Methods: The infusion method was used to prepare DMZ ethosomes. The particle size, entrapment efficiency (EE), analysis methodology, and in vitro release behavior were examined, respectively. The in vitro transdermal absorption of ethosomes-based gel of DMZ was evaluated by Franz diffusion cells. Results: The DMZ ethosomes was yellowish emulsion. The average particle size of the ethosomes was (365.2 ± 14.4) nm and the EE was (72.30 ± 2.31)%. The cumulative permeation curve of DMZ in ethosomes-based gel was consistent with Higuchi equation (Q=80.198 t1/2-71.641, r=0.986 8). Compared with common gel, the ethosomes-based gel had 3.94 times higher cumulative permeation amount in 24 h. Conclusion: The prepared ethosomes- based gel of DMZ could enhance the transdermal permeation, which provides evidence for the development of transdermal drug delivery system of DMZ.

A Comprehensive Review on Ethosomes.

Ethosomes are noninvasive delivery carriers that enable drugs to reach the deep skin layers and the systemic circulation. Although ethosomal systems are conceptually sophisticated, they are simple in their preparation, safe for use a combination that can highly expand their application. Ethosomes are soft, malleable vesicles tailored for enhanced delivery of active agents. Because of their unique structure, ethosomes are able to encapsulate and deliver through the skin highly lipophilic molecules such as cannabinoids, testosterone, and minoxidil, as well as cationic drugs such as propranolol, trihexaphenidyl, Cyclosporine, insulin, salbutamol etc. Enhanced delivery of bioactive molecules through the skin and cellular membranes by means of an ethosomal carrier opens numerous challenges and opportunities for the research and future development of novel improved therapies. Ethosomes are gaining popularity in designing drug delivery systems for topical and transdermal use for their capability to reach deep skin layers and systemic circulation. Although ethosomes are conceptually sophisticated, they are simple in preparation and safe for use. Although with their high efficiency, the ethosomes show potential for expansion of their applications. The aim of the review to make a comprehensive account on properties and preparation of ethosomes followed by the characterization and the list of drugs encapsulated in ethosomes in last 15 years.

Percutaneous permeation characteristic of podophyllotoxin ethosomes in vitro / 中草药

Objective To study the percutaneous permeability characteristic of podophyllotoxin (POD) ethosomes in vitro. Methods Excised SD-rat abdomen skin was used as penetration barrier. The steady penetration rate and the skin residual amount were calculated to evaluate the percutaneous permeability of POD from ethosomes, tinctures, liposome, 30% hydro-ethanolic suspension, mixture of drug and blank ethosomes, respectively. Results The skin residual amount of POD in the ethosomes group was 8.17 ug/cm2 in 12 h, higher than those in the other groups. In addition, the steady penetration rate of POD in the ethosomes group decreased significantly compared with those in the liposome group with POD loading being 0.5%, and the hydro-ethanolic suspension group (P < 0.05), while no obvious difference was seen among the ethosomes group and the other groups. Conclusion Higher skin residual amount and lower steady penetration rate are observed in the ethosomes group.

Studies on In-vitro Transdermal Permeability of Cyclovirobuxine D Ethosomes / 广州中医药大学学报

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.