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ObjectiveTo study the in vitro kinetics of Jiaojiang cataplasms and evaluate its pharmacodynamics， so as to provide a feasible basis for the development of this preparation. MethodThe improved Franz diffusion cell was used for the in vitro release in semipermeable membrane and transdermal absorption in in vitro mouse skins. The contents of hydroxy-α-sanshool， 6-gingerol， ginsenoside Rb1 were determined by high performance liquid chromatography （HPLC）， to evaluate the in vitro release and transdermal absorption of Jiaojiang cataplasms. The mobile phase of 6-gingerol and hydroxy-α-sanshool was water-acetonitrile-methanol （2∶1∶1） with the detection wavelength of 280 nm. The mobile phase of ginsenoside Rb1 was acetonitrile-0.1% phosphoric acid aqueous solution （31∶69） with the detection wavelength of 203 nm. A mouse intestinal paralysis model was established， and mice were randomly divided into five groups， namely sham operation group， model group， domperidone group （3.9 mg·kg-1） and high- and low-dose groups of Jiaojiang cataplasms （6.2， 3.1 g·kg-1， measured by crude drug dosage）， to observe the effect of this preparation on gastrointestinal propulsion function. ResultAverage release rates of hydroxy-α-sanshool， 6-gingerol and ginsenoside Rb1 at 24 h were 16.41， 4.23， 4.15 μg∙cm-2∙h-1， the average transdermal rates of them at 24 h were 2.31， 0.64， 0.29 μg∙cm-2∙h-1， their skin retention values were 19.56， 3.59， 1.61 μg， respectively. According to the Ritger-Peppas equation， the release of hydroxy-α-sanshool， 6-gingerol， ginsenoside Rb1 was non-Fick diffusion. The high-dose group of Jiaojiang cataplasms could improve intestinal function of model mice after small intestinal friction injury， and promote intestinal peristalsis and small intestinal propulsion rate （P<0.05）. ConclusionJiaojiang cataplasms has in vitro release and transdermal properties， the in vitro release conforms to Higuchi equation， and transdermal absorption behavior conforms to zero-order kinetic equation， which can improve the postoperative function of the small intestine and the propulsion function of small intestine. It preliminarily indicates that the preparation has certain clinical development value.
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@#This paper aimed at studying the effects of hyaluronic acid (HA) with different molecular weights on the transdermal absorption and retention of reduced glutathione (GSH) in the isolated skin of SD rats. Franz diffusion cell method was used to investigate the effects with different molecular weights HA on the in vitro transdermal penetration of GSH and the storage in different layers of the skin. AutoDock molecular docking was used to study the interaction between GSH and HA. Attenuated total reflection Fourier transformed infrared spectroscopy (ATR-FTIR) and H&E section staining were used to characterize the changes and effects of lipids and proteins in the rat stratum corneum after HA acts on the skin. The results of in vitro transdermal experiments showed that HA with different molecular weights had a significant impact on the amount of GSH passing through the skin, that as the molecular weight of HA increased, the effect of preventing GSH from passing through the skin became stronger, that in terms of skin storage, HA with different molecular weights could increase the storage of GSH in the stratum corneum, and that HA with a molecular weight below 7K could also significantly increase the storage of GSH in the dermis. The molecular docking results showed that HA and GSH had a relatively strong interaction, which could form intermolecular hydrogen bonds; and the results of ATR-FTIR and H&E staining showed that HA could interact with lipids and keratins in the stratum corneum of the skin. Such interaction can increase the permeability of the stratum corneum of the drug, however, as a water-soluble GSH, it may be involved in the formation of intermolecular hydrogen bonds with HA. In the structure of HA hydrogel, the amount of GSH drug passing through the intact skin is reduced; but at the same time, this interaction also provides a reservoir for the formation of GSH, thus increasing its storage in the skin. Through comparison of the storage capacity of GSH in the stratum corneum and dermis of the isolated skin due to the increase of HA with different molecular weights, it has been found that the storage capacity of HA with low relative molecular weight is the best.
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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.
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In order to increase the stability and solubility of essential oil in Jieyu Anshen Formula, this study was to prepare the essential oil into liposomes. In this experiment, the method for the determination of encapsulation efficiency of liposomes was established by ultraviolet spectrophotometer and dextran gel column. The encapsulation efficiency and particle size of liposomes were used as evaluation indexes for single factor investigation and Box-Behnken design-response surface method was used to optimize the design. Then the optimal formulation of volatile oil liposome was characterized using methyleugenol, elemin, β-asarone and α-asarone as index components. Finally, the in vitro transdermal properties of liposomes were studied by modified Franz diffusion cell. The results showed that the concentration of lecithin, the mass ratio of lecithin to volatile oil, and the stirring speed were the three most significant factors affecting the liposome preparation. The optimum formulation of volatile oil liposome was as follows: the concentration of lecithin was 7 g·L~(-1); mass ratio of lecithin to volatile oil was 5∶1; and the stirring speed was 330 r·min~(-1). Under such conditions, the prepared liposomes had blue emulsion light, good fluidity, half translucent, with particle size of(102.6±0.35) nm, Zeta potential of(-17.8±0.306) mV, permeability of(1.67±1.01)%, and stable property if liposome was stored at 4 ℃. 24 h after percutaneous administration, the cumulative osmotic capacity per unit time was(30.485 2±1.238 9),(34.794 8±0.928 3),(26.677 1±1.171 7),(3.066 2±0.175 3) μg·cm~(-2)respectively for methyleugenol, elemin, β-asarone and α-asarone. In vitro transdermal behaviors of methyleugenol, elemin, β-asarone and α-asarone in liposomes were all consistent with Higuchi equation. The prepared volatile oil liposomes met the relevant quality requirements, providing a reference for further research on preparation of multi-component Chinese medicine essential oil liposomes.
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Administration, Cutaneous , Drugs, Chinese Herbal , Liposomes , Oils, Volatile , Particle Size , SolubilityABSTRACT
In general, when topical non-steroidal anti-inflammatory patches (hereinafter NSAIDs patches) are prescribed in clinical practice, adverse events, such as gastroduodenal ulcers, are not considered. However, patients often increase the number of NSAIDs patches they use in a single day even though they should only use 1 or 2 for local administration. Daily use of many NSAIDs patches (more than 4 large patches) may maintain the blood concentration of NSAIDs at a significantly level and cause adverse events similar to those by oral administration of standard-dose NSAIDs.We present a case of prolonged gastric ulcer caused by the daily use of many NSAIDs patches. In this case, Helicobacter pylori infection was negative and no oral NSAIDs were administered, and the discontinuation of NSAIDs patches resulted in the rapid healing of a gastric ulcer that was present for 2 years.
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Objective:To prepare self-emulsifying carrier system which was suitable for three Chinese medicinal ingredients(baicalein,berberine and allicin),and investigate transdermal absorption effect in vitro of these three self-emulsifying preparations. Method:The optimum formulation and dosage were screened by the saturated solubility method,pseudo-ternary phase diagram method and orthogonal experiment.Transdermal absorption test in vitro was carried out with excised rats skin and Franz diffusion cell.The cumulative penetration amounts of baicalein,berberine and allicin in the identical self-emulsifying system were determined by HPLC and compared with baicalein powder,berberine powder and allicin powder,respectively. Result:The optimum formulation was ethyl oleate-cremophor RH40-polyethylene glycol(PEG)400.The self-emulsifying preparation had a suitable particle size with a relatively regular spherical shape.At 10 h of transdermal absorption,the transdermal rates of baicalein,berberine and allicin in identical self-emulsifying system were 6.898 6,7.600 4,190.040 μg·cm-2·h-1,the cumulative penetration amounts of them were 71.38,85.54,1 795.16 μg·cm-2,respectively. Conclusion:The self-emulsifying carrier system is prepared successfully,which can be used by different kinds of Chinese medicinal ingredients,and the transdermal absorption effect in vitro of these self-emulsifying preparations is good,which can provide experimental basis for the preparation and transdermal absorption of self-emulsifying preparation of Chinese herbal compound.
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OBJECTIVE: To investigate the effect of natural and synthetic borneol on the transdermal absorption of emodin. METHODS: The supplying and receiving solutions containing emodin were selected from the abdominal skin of mice in vitro, and the samples were analyzed by HPLC. The cumulative permeability, permeability rate and permeability enhancement factor were used as the evaluation indexes of the permeability enhancement effect. RESULTS: The saline containing 1% Tween 80-80% ethanol and 60% ethanol could increase the solubility of emodin to 648 μg•mL -1 and obtain conditions of leaking trough. The penetration rate of emodin was 648 μg•mL - 1 > 569 μg•mL -1 > 457 μg•mL -1 in the range of concentration. The penetration enhancement effect of synthetic borneol was 2% > 4% > 1% > blank control group > 3% and 5%, and the steady-state permeation rates of 2% natural borneol (15.90 μg•cm- 2•h - 1 ) were higher than those of 2% synthetic borneol(12.44 μg•cm-2•h-1). CONCLUSION: Natural borneol and synthetic borneol can promote the transdermal penetration of emodin, which is limited by their concentration. This provides an experimental basis for the selection of emodin transdermal enhancers.
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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.
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AIM To study the effect of azone on transdermal absorption of 6-gingerol.METHODS In vitro transdermal diffusion test was performed by TP-6 horizontal diffusion pool.In vitro rat skins were selected as permeation barrier,the effects of different concentrations of ethanol and azone on permeation performance of 6-gingerol were investigated.RESULTS Both 30％ ethanol and 3％ azone contributed to the significant permeation enhancement of 6-gingerol.CONCLUSION This research can provide reference for the preparation of transdermal drug delivery systems containing 6-gingerol.
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Objective To compare the percutaneous absorption of experimentally prepared mupirocin ointment and commercially sold mupirocin ointment, and to study the dynamics mode of transdermal absorption of mupirocin ointment. Methods Inerstil ODS-SP column (4.6 mm× 150 mm,5 μm) was used with a mixture of 0.1 mol·L-1 sodium dihydrogen phosphate buffer solution (pH value was adjusted to 6.3 by 0.1 mol·L-1 sodium hydroxide solution) and acetonitrile (75:25) as a mobile phase by HPLC.The detection wavelength was set at 230 nm.The flow rate was 1.0 mL·min-1 .Improved Franz type diffusion cells were used for in vitro permeation studies and excised Obama Suckling pig skins in vitro were used as the transdermal barrier.The concentration of the receptor solution was determined by HPLC to investigate its cumulative permeation quantities at different time and the two sets of ointment were compared. Results The average recovery rate of hydrophilic medium was 99.4％,and RSD was 1.2％(n= 9).The average recovery rate of lipophilic medium was 99.0％,and RSD was 1.3％(n= 9).There was no significant difference of the concentration between two ointment within 12 h.The osmotic release of the drug of the sample and the reference preparation, which were in hydrophilic medium, was similar to that of the Zero equation, and roughly Higuchi equation in the lipophilic medium. Conclusion The results showed that the release behavior of mupirocin ointment followed Zero equation in the hydrophilic medium,and Higchi equation in the lipophilic medium.
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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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Objective: To evaluate the feasibility of the application of composite phospholipid liposome-based artificial skin membrane (CPLASM) for measuring biopharmaceutical properties of active fraction extracted from Xiangfu Siwu Decoction (XSD) via transdermal administration. Methods: The HPLC method was established for the determination of active ingredients (ferulic acid, tetrahydrocolumbamine, tetrahydropalmatine, senkyunolide I, and senkyunolide H) in active fraction of XSD. The oil/water partition coefficient values of these active ingredients were measured. The CPLASM was prepared to determine the in vitro permeability parameters of active fraction of XSD. The obtained parameters were further compared with those obtained by porcine ear skin. Results: The oil-water partition coefficients of ferulic acid, tetrahydrocolumbamine, tetrahydropalmatine, senkyunolide I, and senkyunolide H in active fraction of XSD (pH 5.5) were measured to be 1.220 ± 0.280, 0.670 ± 0.085, 0.920 ± 0.110, 1.040 ± 0.092, 1.030 ± 0.093 (n = 3), respectively. The permeability parameters of the active ingredients through porcine ear skin and CPLASM indicated a significant correlation (r > 0.9). Compared with the classical oil-water partition coefficients, the 6 h- cumulative permeation ratio of five active ingredients through CPLASM can be characterized as effectively predicting permeability parameters through porcine ear skin. Conclusion: The biopharmaceutical properties of active fractions from Chinese material medica can be effectively characterized by the application of CPLASM for the determination of in vitro permeability parameters of active ingredients.
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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.
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Objective To optimize the matrix formulation for Shaofu Zhuyu Cataplasm (SZC) by Plackett-Burman design combined with Box-Behnken response surface method and study its transdermal permeation properties in vitro. Methods In this paper, the appearance description, initial bonding strength, endurance bonding strength, and peel strength were taken as indexes. Based on the result of a single factor experiment, the formula for the SZC was optimized by Plackett-Burman combined with Box-Behnken method. Franz diffusing cells method was chosen to investigate the tansdermal infiltration capacity of SZC with different dosage penetration enhancers of azone in vitro, taking ferulic acid, paeoniflorin, isorhamnetin-3-O-neohesperidin, and typhaneoside as index components. Results NP-700, tartaric acid and kaolin had significant effects on the properties of SZC. The optimal ratio of the prescription was as follows: NP-700-tartaric acid-kaolin (2.42:0.16:0.96). The promoting effect of 3% concentration for index component was better, and the transdermal rates of ferulic acid, paeoniflorin, isorhamnetin-3-O-neohesperidin, and typhaneoside were 6.889 4, 1.917 4, 0.852 0, and 0.893 7 μg/(cm2∙h), respectively. Conclusion The SZC was uniform, without residual behavior in application. And it had a good release and transdermal properties, and transdermal actions were consistent with zero-order kinetics.
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The aim of this paper is to investigate the topical pharmacodynamics behavior of different lipophilic model drugs after treatment with essential oil from Zanthoxyli Pericarpium by using the cutaneous microdialysis technique, and then evaluate its in vivo transdermal penetration enhancing properties. Two traditional Chinese medicine active components, namely tetramethylpyrazine and puerarin, were chosen as lipophilic and hydrophilic model drugs, respectively. Firstly, the concentration difference method was employed to measure the in vitro recovery rate and loss of the microdialysis probe, and the in vivo recoveries of two model drugs were determined by using the retrodialysis method. Secondly, the skin pharmacodynamics behaviors of two model drugs were studied after treatment with different concentrations of the essential oil, and the well-established and standard penetration enhancer Azone was selected as a positive control. It was found that the recovery of microdialysis probe was equal to its loss for two model drugs, with no interaction between drugs in dialysis membranes. The retrodialysis studies revealed that the in vivo recovery of tetramethylpyrazine and puerarin were 59.17%, 19.85%, respectively. The skin pharmacodynamics studies showed that the essential oil could facilitate the transdermal absorption of tetramethylpyrazine in a concentration-dependent manner, and the enhancement ratio (ER) for 5% essential oil was 98.64, which was higher than that of the optimum concentration of Azone (3% Azone, ER=89.11). Meanwhile, the Zanthoxyli Pericarpium could effectively promote the transdermal permeation of the puerarin in a concentration-dependent manner. Hence, this study further confirmed that the Zanthoxyli Pericarpium had excellent penetration-enhancing activity as a natural transdermal penetration enhancer, providing data support for its application in traditional Chinese medicine external preparations.
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The aim of this study was to investigate the transdermal penetration enhancement effect of wintergreen oil and its action mechanisms. The in vitro transdermal tests were carried out to study the transdermal penetration enhancement effect of wintergreen oil by using osthole and geniposide as the lipophilic and hydriphilic model drugs. Fourier-transform infrared spectroscopy was used to investigate the effect of wintergreen oil on the molecular structure of rat stratum corneum, and the scanning electron microscope was employed to observe the change of rat skin surface after treatment by the oil. The wintergreen oil at proper concentrations could effectively promote the transdermal permeation of osthole and geniposide, and exhibited better penetration-enhancing activity for the lipophilic osthole, close to the commonly used classical penetration enhancer azone. The infrared spectroscopy study and scanning electron microscope showed that wintergreen oil mainly acted on the stratum corneum lipids, reduced dense stratum corneum, and reduced the skin barrier function. Thus, the wintergreen oil could effectively facilitate the transdermal absorption of the lipophilic and hydrophilic drugs, resulting from the lowed skin barrier function.
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The aim of this paper was to explore the effects of Frankincense and Myrrh essential oil on transdermal absorption in vitro of Chuanxiong, and to investigate the possible penetration mechanism of their essential oil from the perspective of skin blood perfusion changes. Transdermal tests were performed in vitro with excised mice skin by improved Franz diffusion cells. The cumulative penetration amounts of ferulic acid in Chuanxiong were determined by HPLC to investigate the effects of Frankincense and Myrrh essential oil on transdermal permeation properties of Chuanxiong. Simultaneously, the skin blood flows were determined by laser flow doppler. The results showed that the cumulative penetration amount of ferulic acid in Chuanxiong was (8.13±0.76) μg•cm⁻² in 24 h, and was (48.91±4.87), (57.80±2.86), (63.34±4.56), (54.17±4.40), (62.52±7.79) μg•cm⁻² respectively in Azone group, Frankincense essential oil group, Myrrh essential oil, frankincense and myrrh singly extracted essential oil mixture group, and frankincense and myrrh mixed extraction essential oil group. The enhancement ratios of each essential oil groups were 7.68, 8.26, 7.26, 8.28, which were slightly greater than 6.55 in Azone group. In addition, as compared with the conditions before treatment, there were significant differences and obvious increasing trend in blood flow of rats in Frankincense essential oil group, Myrrh essential oil group, frankincense and myrrh singly extracted essential oil mixture group, and frankincense and myrrh mixed extraction essential oil group when were dosed at 10, 20, 30, 10 min respectively, indicating that the skin blood flows were increased under the effects of Frankincense and Myrrh essential oil to a certain extent. Thus, Frankincense and Myrrh essential oil had certain effect on promoting permeability of Chuanxiong both before and after drug combination, and may promote the elimination of drugs from epidermis to dermal capillaries through increase of skin blood flow, thus enhancing the transdermal permeation amounts of drugs.
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Objective: To determine the transdermal absorption of phloretin and ligustilide in Fufang phloretin cream.Methods: In vitro percutaneous absorption test using the Franz intelligent transdermal absorption apparatus was adopted, an HPLC method was used to determine the contents of phloretin and ligustilide in the accepting solution at different time points, and then the cumulative release amount and the total penetration amount were calculated to evaluate the percutaneous absorption behavior.Results: Phloretin and ligustilide showed a good linearity within the range of 0.044 2-4.42 μg·ml-1(r=0.999 9) and 0.048 7-4.87 μg·ml-1(r=0.999 9), respectively, the average recovery was 99.85% and 99.92%, and RSD was 0.67% and 0.66% (n=9), respectively.The in vitro permeation behavior of phloretin and ligustilide through the skin of rats fit Higuchi equations(r>0.9), suggesting a good linear correlation between the cumulatine penetration amount (Qn) and (time).Conclusion: Fufang phloretin cream has a good percutaneous permeation property in vitro.
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Objective: To screen the best transdermal enhancers of naringenin in Premna fulva extract. Methods: Using abdominal skin of rats as experimental barrier, the in vitro percutaneous absorption experiment was established by modified Franz diffusion cell method. The cumulative infiltration and permeation rate of naringenin in three different penetration enhancers were determined by HPLC. Results: The borneol, menthol, and azone could enhance transdermal absorption of naringenin in different degree. Several penetration enhancers were increased in the following order: borneol > menthol > azone. The average percutaneous rate of naringenin was 0.136 8 mg/(cm2∙h), using 5% borneol as penetration enhancer. Conclusion: The 5% borneol is an effective transdermal enhancer for naringenin in P. fulva extract.
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Objective To prepare Sanqi Traumatic Ointment (STO) and study its transdermal permeation properties in vitro. Methods In this paper, the appearance description, high-temperature test, low-temperature test and centrifugal test were taken as indexes. Based on the result of a single factor experiment, the formula for the STO was optimized by Box-Behnken test. Franz diffusing cells method was chosen to investigate the tansdermal infiltration capacity of ointment with different mentha camphor penetration enhancers' in vitro, taking dracorhodin, ginsenoside Rg1, asperosaponi VI, and ginsenoside Rb1 as index components. Results The optimal ratio of the prescription was as follows: lauryl sodium sulfate-stearyl alcohol-vaseline (1.61:26.72:27.10). The promoting effect of different concentration of penetration enhancers on dracorhodin, ginsenoside Rg1, ginsenoside VI, and asperosaponin Rb1 penetration were better; The promoting effect of 3% concentration for index component was better, and this preparation had good stability; The transdermal rates of dracorhodin, ginsenoside Rg1, asperosaponi VI, and ginsenoside Rb1 were 3.971, 6.368, 0.415, and 2.780 μg/(cm2∙h).Conclusion STO had a good release and transdermal properties, and transdermal actions were consistent with zero-order kinetics.