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Objective To conduct in vitro transdermal test on triamcinolone acetonide spray solution, and investigate the effects of ethanol and propylene glycol alone or in combination on the in vitro transdermal function of triamcinolone acetonide spray solution. Methods Rabbit abdominal skin was selected, and the in vitro penetration test of triamcinolone acetonide spray solution was carried out by Franz diffusion cell method, and the content of triamcinolone acetonide was determined by HPLC. The rate of transdermal absorption was compared. Results The transdermal absorption rate of the combined use of ethanol and propylene glycol was significantly higher than that of the single use (P<0.05), and the order of promoting the penetration of triamcinolone acetonide spray solution when ethanol and propylene glycol were combined by 10% ethanol + 25% propylene glycol >10% ethanol + 20% propylene glycol >15% ethanol + 25% propylene glycol >15% ethanol + 20% propylene glycol. Conclusion The combination of 10% ethanol and 25% propylene glycol could optimize the transdermal function of triamcinolone acetonide spray solution.
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ObjectiveTo compare the differences in resistance and structure of skin between acupoints and non-acupoints， and to study the difference in skin permeability characteristics of Corydalis Rhizoma total alkaloid patches （CTTP） after administration at Shenque acupoint and non-acupoint， so as to provide experimental support for its clinical acupoint application to prevent and treat chronic pain. MethodTaking corydaline （CD）， tetrahydropalmatine （THP） and corydalis L （CDL） as evaluation indexes， and the quantitative analysis was carried out by high performance liquid chromatography （HPLC）. The mobile phase was methanol-0.04 mol·L-1 phosphoric acid aqueous solution （70∶30， pH 6.0 adjusted with triethylamine）， the detection wavelength was 281 nm. In vitro transdermal test in Franz diffusion cell and in vivo transdermal test were used to study the skin permeability characteristics of CTTP through Shenque acupoint and non-acupoint administration. At the same time， the skin resistance between Shenque acupoint and non-acupoint was measured before and after the administration， and the distribution of the drug in each layer of the skin was compared by freezing sectioning， and visual verification was performed with fluorescence inverted microscope. ResultAfter 24 h of administration， the results of in vivo and in vitro experiments showed that the cumulative permeation and retention of CD， THP and CDL at Shenque acupoint skin were higher than those at non-acupoint skin （P<0.05， P<0.01）， the skin resistance of Shenque acupoint was lower than that of non-acupoint at all time points. The fluorescence microscopic observation results showed that the drug content of each layer of the skin was all Shenque acupoint>non-acupoint， indicating that the skin of Shenque acupoint had better effect on drug penetration and storage than non-acupoint. ConclusionThe 24 h cumulative permeation and retention of CTTP in Shenque acupoint skin are higher than those in non-acupoint skin， and the mechanism may be related to the thin skin， low electrical resistance and large number of hair follicle bodies at Shenque acupoint.
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ObjectiveTo compare the differences in resistance and structure of skin between acupoints and non-acupoints， and to study the difference in skin permeability characteristics of Corydalis Rhizoma total alkaloid patches （CTTP） after administration at Shenque acupoint and non-acupoint， so as to provide experimental support for its clinical acupoint application to prevent and treat chronic pain. MethodTaking corydaline （CD）， tetrahydropalmatine （THP） and corydalis L （CDL） as evaluation indexes， and the quantitative analysis was carried out by high performance liquid chromatography （HPLC）. The mobile phase was methanol-0.04 mol·L-1 phosphoric acid aqueous solution （70∶30， pH 6.0 adjusted with triethylamine）， the detection wavelength was 281 nm. In vitro transdermal test in Franz diffusion cell and in vivo transdermal test were used to study the skin permeability characteristics of CTTP through Shenque acupoint and non-acupoint administration. At the same time， the skin resistance between Shenque acupoint and non-acupoint was measured before and after the administration， and the distribution of the drug in each layer of the skin was compared by freezing sectioning， and visual verification was performed with fluorescence inverted microscope. ResultAfter 24 h of administration， the results of in vivo and in vitro experiments showed that the cumulative permeation and retention of CD， THP and CDL at Shenque acupoint skin were higher than those at non-acupoint skin （P<0.05， P<0.01）， the skin resistance of Shenque acupoint was lower than that of non-acupoint at all time points. The fluorescence microscopic observation results showed that the drug content of each layer of the skin was all Shenque acupoint>non-acupoint， indicating that the skin of Shenque acupoint had better effect on drug penetration and storage than non-acupoint. ConclusionThe 24 h cumulative permeation and retention of CTTP in Shenque acupoint skin are higher than those in non-acupoint skin， and the mechanism may be related to the thin skin， low electrical resistance and large number of hair follicle bodies at Shenque acupoint.
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AIM To compare the percutaneous penetration performance of three paeonol gels.METHODS Franz diffusion cell method was applied to investigating the penetration and retention behaviors of eutectic mixturebased nanoemulsion,ordinary nanoemulsion and saturated solution gels onto mouse skins in vitro.The retention and permeation amounts in stratum corneum and hair follicles of volunteers smeared with gels were compared by tape stripping method.RESULTS The accumulative permeation and retention amounts of various gels onto mouse skins in vitro were in sequence of eutectic mixture-based nanoemulsion gel ＞ ordinary nanoemulsion gel ＞ saturated solution gel.The main retention of all the three gels was observed on the volunteers' skin surface,and the permeation amounts of eutectic mixture-based nanoemulsion,ordinary nanoemulsion gels,and their accumulative permeation amounts in stratum corneum and hair follicles were significantly higher than those of saturated solution gel (P ＜0.05).CONCLUSION Nanoemulsion technology can significantly promote the percutaneous penetration performance of paeonol.
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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.
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The sample preparation of samples containing bovine serum albumin (BSA), e.g., as used in transdermal Franz diffusion cell (FDC) solutions, was evaluated using an analytical quality-by-design (QbD) approach. Traditional precipitation of BSA by adding an equal volume of organic solvent, often successfully used with conventional HPLC-PDA, was found insufficiently robust when novel fused-core HPLC and/or UPLC-MS methods were used. In this study, three factors (acetonitrile (%), formic acid (%) and boiling time (min)) were included in the experimental design to determine an optimal and more suitable sample treatment of BSA-containing FDC solutions. Using a QbD and Derringer desirability (D) approach, combining BSA loss, dilution factor and variability, we constructed an optimal working space with the edge of failure defined as Do0.9. The design space is modelled and is confirmed to have an ACN range of 8373%and FA content of 170.25%.
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OBJECTIVE:To study the percutaneous permeability of Hydrocortisone cream with different substrates in diabetic model rats. METHODS:The Hydrocortisone O/W(oil/water)cream,water-soluble cream and oil-soluble cream were respectively prepared. Wistar rats were randomly divided into normal control group and model group. Model group was given streptozotocin(40 mg/kg)to reproduce diabetic model. Franz diffusion cell percutaneous test and HPLC were used to detect the percutaneous permea-bility rates of Hydrocortisone O/W cream,water-soluble cream and oil-soluble cream in rats of 2 groups. RESULTS:Compared with normal control group,the percutaneous permeability rates of Hydrocortisone O/W cream and water-soluble cream were obvi-ously increased,with significant difference(P0.05). CONCLUSIONS:Hydrocortisone O/W cream and water-soluble cream are easier to go through the skin of diabetic model rats,and Hydrocortisone oil-soluble cream is hard.
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The present work was performed to develop and evaluate buccal tablet containing antidiabetic drug (Repaglinide). Ethyl cellulose was used as backing membrane and Carbopol 934p, Polyox wsr N-80 NF, HEC and HPC was used as bucco adhesive polymer. Aspartame was used as sweetener. Thickness, Hardness, weight variation and drug uniformity were investigated. The tablet formulations were also subjected to drug release in 250ml 6.8 phosphate buffer. Ex vivo bioadhesion, retention time and permeation through porcine buccal mucosa membrane. Effects of different bucco adhesive polymer were evaluated on release and bioadhesion, retention time and permeation of drugs. F5 formulations showed maximum amounts of drugs release (87.18%) at the end of 10 h dissolution study. F5 also showed maximum bioadheion (0.0754N) and the resident time of F5 formulation was 9.2 h. It shows 41.52% drug release after 10 h permeation study through porcine buccal mucosa mounted in Franz cell. The tablet also found stable in human saliva after 10hr. The tablet was not showed any type of physical changes after the completion of 10 h. The results of the study suggested that new buccal tablet formulations of combined bucco adhesive polymers can be suitably developed as an alternate to conventional dosage forms.
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Trandolapril is an antihypertensive agent which undergoes extensive first pass metabolism making it a possible candidate for transdermal delivery. Patches were prepared using hydroxypropylmethylcellulose, eudragit RL 100, gantrez and carbopol. The results of FTIR and DSC revealed no interaction between drug and polymers. The loss of moisture and uptake of moisture were within the limits. The formulations showed an extended release of the drug upto period of 24 hours during in vitro permeation studies and showed non-Fickian drug release. Stability of the optimized formulation was investigated as per ICH guidelines and was found to be stable with respect to drug content and in vitro permeation.