ABSTRACT
OBJECTIVE： To prepare pogostone transfersomes， and to evaluate its quality. METHODS： Film dispersion method was used to prepare pogostone transfersomes. Using the accumulative penetration volume （Qn） and accumulative penetration ratio （PR） of pogostone as evaluation indexes， the types of surfactant， formulation were screened in respects of the dosage of surfactant and the dosage of pogostone. The pogostone transfersomes were prepared with optimal formulation； the morphology， particle size distribution and Zeta potential were observed and the entrapment efficiency was measured. RESULTS： The optimal formulation was as follows as the sodium cholate was selected as surfactant； the dosage of sodium cholate was 0.25 g； the dosage of pogostone was 15 mg. The optimal pogostone transfersomes were ivory-white suspension； average particle size was （115.6±3.65） nm （RSD＝3.20％，n＝3）； PDI was 0.185±0.008 （RSD＝4.30％， n＝3）； Zeta potential was （－13.76±0.225） mV （RSD＝1.70％，n＝3）； entrapment efficiency of pogostone was （46.01±0.40）％ （RSD＝0.87％，n＝3）； Qn was （378.76±0.61） μg/cm2 （RSD＝0.20％，n＝3）； PR was （89.02±0.96）％ （RSD＝1.10％，n＝3）. CONCLUSIONS： Prepared pogostone transfersomes are in line with quality requirements， which can provide reference for the further study of new dosage form of pogostone.
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Objective: To prepare plumbagin transfersomal (PBG-T) gel and investigate its transdermal penetration characteristics in vitro. Methods: Plumbagin transfersomes were prepared by film-ultrasonic dispersion method. The optimal prescription condition of PBG-T was selected by central composite design and response surface method. The formula of PBG-T gel was optimized by orthogonal test. The Franz diffusion cell was used to investigate transdermal penetration characteristics of PBG-T gel in vitro. Results: The optimal prescription condition of transfersomes was determined as drug 10.0 mg, phospholipids 700.0 mg, Tween-80 91.5 mg, ultrasonication time 13 min. The optimal prescription condition of transfersomal gel was 1% carbomer 940 as gel matrix, and 5% glycerol as the humectant. According to the optimized prescription, the entrapment efficiency, the mean particle size, and Zeta potential of PBG-T were (79.88 ± 2.26)%, (125.64 ± 4.54) nm, and (-30.97 ± 1.13) mV. The cumulative penetration rate of PBG-T gel was 70.0% at 12 h. Conclusion: The optimal preparation technique is stable and feasible. Transfersomal gel features a sustained release in vitro, the transfersomal gel can increase penetration rate of plumbagin through the skin of rats.
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To prepare the liposomes and transfersomes of brucine, characterize their pharmaceutical properties, and compare their in vitro transdermal permeation properties. The liposomes and transfersomes of brucine were prepared by ammonium sulfate gradient method to investigate their pharmaceutical properties such as the particle size, encapsulation efficiency and deformation. The transdermal permeation properties in vitro of liposome and transfersomes from different prescriptions were compared by using modified Franz-diffustion cells with rat skin as the transdermal barrier. The results showed that the particle size of liposomes and transfersomes for brucine ranged from 100 nm to 150 nm, with even distribution for particle size. As compared with the soybean phosphatidylcholine (SPC) transfersomes, the encapsulation efficiency of complex phospholipid transfersomes was significantly improved. The deformation index of complex phospholipid transfersomes in brucine was 2.09 times and 1.76 times as much as SPC liposomes and SPC transfersomes respectively. The steady state flux of complex phospholipid transfersomes was 3.43 times and 1.41 times as much as SPC liposomes and SPC transfersomes. The steady state flux of the physical mixture of brucine and blank complex phospholipid transfersomes was 2.20 times as much as brucine solution. The concentration of complex phospholipid had effect on transdermal permeation of blank transfersomes. In conclusion, as compared with liposomes, the permeation behavior of transfersomes was significantly improved; complex phospholipid technology can improve the membrane phase behavior of transfersomes, and further improve the deformation index and transdermal flux of transfersomes; in addition, blank transfersomes have promoting effect on transdermal absorption of brucine.
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OBJECTIVE: To prepare mangiferin transfersomes and investigate its transdermal delivery characteristics. METHODS: Mangiferin transfersomes were prepared by the method of film-dispersion, the in vitro percutaneous penetration study was conducted in the modified Franz diffusion cell, the distribution of transfersomes in skin was investigated by fluorescent tracer method, and the rat back airbag inflammation model was used to preliminarily evaluate the anti-inflammatory effect of mangiferin transfersomes with prostaglandin E2 (PGE2) content as the indicator. RESULTS: The average particle size of mangiferin transfersomes was (84.50 ± 5.26)nm, the polydispersity index (PDI) was (0.21 ± 0.012), the Zeta potential was(-10.83 ± 0.66)mV, the encapsulation efficiency (EE) was (64.07 ± 2.10)%, and the deformability was (20.00 ± 0.30)%; the cumulative permeation quantities in 24 h and intradermal retention of mangiferin transfersomes were (313.67 ± 22.62) and (60.34 ± 8.10) μg · cm-1, respectively. Fluorescent tracer method showed that the fluorescence intensity of FITC transfersomes in the inside of skin was stronger than that of FITC solution at 8 h. Anti-inflammatory test showed that the PGE2 contents in the middle and high dose mangiferin transfersomes groups decreased significantly. The anti-inflammatory effect of the high dose mangiferin transfersomes was even close to that of compound dexamethasone cream. CONCLUSION: Transfersomes can promote the percutaneous penetration of mangiferin, increase its intradermal retention, and enhance the anti-inflammatory effect of mangiferin significantly.