酮洛芬醇质体体外经皮渗透研究

目的:考察酮洛芬醇质体的体外经皮渗透特性。方法:乙醇注入法制备酮洛芬醇质体,采用Franz扩散池,以离体小鼠皮为皮肤屏障,对酮洛芬醇质体的体外经皮渗透量、稳态透皮速率进行研究,并测定24 h时皮肤中的滞留量。结果:酮洛芬醇质体体外24 h累积渗透量Q为(720.88±2.04)μg.cm-2,稳态透皮速率J为(28.15±0.20)μg.cm-2.h-1,24 h皮肤中的滞留量(50.86±1.44)μg.cm-2,与同剂量酮洛芬脂质体及其30%醇溶液相比,均有明显提高(P<0.05)。结论:醇质体可显著增加酮洛芬的体外经皮渗透,值得进一步研发。     

酮洛芬二元醇质体凝胶的研制及其质量考察

目的:研制酮洛芬二元醇质体凝胶,并对其质量进行考察.方法:采用乙醇注入法制备酮洛芬二元醇质体,采用研和法制备醇质体凝胶;透析法测定包封率;Franz扩散池进行离体皮肤渗透试验,测定其体外累积渗透量及皮内滞留量;并对其体外稳定性进行了初步考察.结果:酮洛芬二元醇质体形态圆整,平均粒径为(289.86±44.75)nm,平均包封率为(73.85±2.62)%.体外透过皮肤进入接收液中的二元醇质体(乙醇/丙二醇=7:3)累积渗透量为一元醇质体的1.8倍,24 h时二元醇脂质体和醇质体皮肤中药物滞留量分别为(52.33±3.12)μg·cm-2和(40.25±2.85)μg·cm-2.在实验期内,体外稳定性较好.结论:酮洛芬二元醇质体具更好的透皮吸收性及皮肤滞留性,且质量稳定.     

醋酸泼尼松龙醇质体的制备及经皮渗透性研究

目的:制备醋酸泼尼松龙(PA)醇质体并考察其对离体小鼠皮肤的渗透性。方法:采用乙醇注入法制备PA醇质体,采用高效液相色谱法测定PA醇质体和PA溶液在Franz扩散池中12h透过离体小鼠皮肤的药物浓度,计算稳态渗透速率(Js)和12h单位面积累积渗透量(Qn)。结果:制得PA醇质体混悬液;PA醇质体和PA溶液的Js分别为5.637、2.487μg(/cm2·h),12hQn分别为(64.145±1.61)、(29.900±1.98)μg/cm2,体外经皮渗透均符合零级动力学方程(r分别为0.998、0.997)。结论:制备的PA醇质体具有较好的透皮性。     

尼美舒利醇质体抗炎镇痛作用与皮肤刺激性研究

目的考察尼美舒利醇质体经皮给药的镇痛抗炎作用及皮肤刺激性。方法采用小鼠热板法和醋酸扭体法观察尼美舒利醇质体的止痛作用;建立大鼠佐剂性关节炎模型,观察尼美舒利醇质体对大鼠足肿胀及滑膜关节组织的影响;利用健康豚鼠观察尼美舒利醇质体皮肤刺激反应。结果与对照组比较,中、高剂量尼美舒利醇质体能明显提高小鼠自身的热痛阈值（P＜0.05）;并能使醋酸致小鼠扭体次数显著减少（P＜0.05）;抗炎实验结果表明,尼美舒利醇质体对佐剂引起的大鼠足肿胀关节炎有明显的抑制作用（P＜0.05）;尼美舒利醇质体对豚鼠无皮肤刺激作用。结论尼美舒利醇质体具有明显的抗炎、镇痛作用,且皮肤刺激性较小,是一种有效的经皮给药制剂。     

纳洛酮醇质体的经皮渗透研究

目的 考察以醇质体为载体的纳洛酮经皮给药的可行性以及醇浓度、药物含量对药物渗透速率的影响.方法 采用注入法制醇质体,以SD雄性大鼠皮肤为媒介,Franz单室扩散池为体外模型,用HPLC法测定透过皮肤的纳洛酮含量.求算累积渗透量稳态透皮速率和皮肤中的滞留量,考察醇浓度和药物含量对渗透速率的影响.结果 纳洛酮为5 mg·mL-1时,含醇20%、30%、40%和50%的醇质体稳态透皮速率分别为(54.3±3.6),(92.0±8.8),(111.4±22.6)和(139.8±7.6)μg·h-1·cm-2,与纳洛酮水溶液(30.9±3.4)μg·h-1·cm-2相比,其增渗倍数分别为1.76,2.98,3.61和4.52倍;在皮肤中的滞留量和时滞的顺序一致50%醇质体＞40%醇质体＞30%醇质体＞20%醇质体＞药物水溶液.含纳洛酮0.625,1.25,2.5,5,7.5和10 mg·mL-1的30%的醇质体,其渗透速率分别为(2.8±1.3),(15.1±2.4),(43.8±5.0),(92.0±8.8),(145.2±4.6)和(193.8±5.7)μg·h-1·cm-2.结论 醇质体能显著地促进渗透,增加药物在皮肤中的滞留量.随着醇质体内醇的含量增加,其渗透速率增加.醇质体内药物含量增加,渗透速率也增加.     

乙肝疫苗体外经大鼠皮肤渗透与离子导入给药特性研究(英文)

对乙肝疫苗进行体外经皮实验以评价疫苗在被动扩散和离子导入情况下的经皮渗透特性。体外透皮研究采用Franz扩散池,以SD大鼠的腹部皮肤为渗透屏障,以酶联免疫法测定药物累积渗透量和在皮肤中的滞留量。乙肝疫苗(质量浓度为23μg·mL-1与46μg·mL-1)经完整皮肤被动扩散的经皮渗透量与皮肤滞留量均极少,24 h累积渗透量仅(2.1±0.1)ng.cm-2和(2.3±0.1)ng.cm-2。去除角质层后,经皮渗透量与皮肤滞留量分别提高至(383.7±86.2)ng.cm-2和(16.8±4.6)ng.cm-2,是完整皮肤的171.6倍与2.1倍(46μg·mL-1)。离子导入对于乙肝疫苗具有明显的经皮渗透促进作用:完整皮肤经皮离子导入6 h,乙肝疫苗的累积渗透量是被动扩散6 h的2.7倍(23μg·mL-1)和6.6倍(46μg·mL-1);去角质层皮肤离子导入,乙肝疫苗的累积渗透量是被动扩散6 h的1.6倍(23μg·mL-1)和1.8倍(46μg·mL-1)。离子导入也能显著增加疫苗在皮肤中的滞留量。离子导入6 h疫苗在完整皮肤中的滞留量和去角质层皮肤中的滞留量均与被动扩散24 h的皮肤滞留量接近[完整皮肤...     

布洛芬乙醇脂质体的制备及体外透皮特性研究

目的:制备布洛芬乙醇脂质体并考察其透皮特性。方法:采用注入法制备布洛芬乙醇脂质体;以包封率为指标,考察磷脂浓度、乙醇浓度、药脂比等因素对脂质体包封率的影响;用Franz扩散池进行离体皮肤渗透实验,测定布洛芬在接收液内的累积渗透量及皮内滞留量。结果:磷脂、乙醇、布洛芬分别占处方量的3%,45%和1%时制得的乙醇脂质体包封率为(72.93±1.12)%;乙醇脂质体的累积渗透量分别为乙醇溶液及脂质体的1.91倍和3.46倍;24 h后皮肤中药物滞留量依次为:乙醇脂质体>45%乙醇水溶液>脂质体。结论:乙醇脂质体可显著增加布洛芬的皮肤渗透性及皮内滞留量。     

姜黄素醇质体体外透皮及其稳定性研究

目的：对姜黄素醇质体体外透皮及其稳定性进行考察方法：采用透皮扩散仪进行体外透皮实验,比较姜黄素醇质体、溶液、脂质体经小鼠离体皮肤的累积渗透量及皮肤滞留量;并将姜黄素醇质体4℃条件下冷藏,考察其稳定性。结果：姜黄素醇质体12h内单位面积皮肤的累计渗透量和皮肤滞留量是其溶液（含0．5％吐温-80）的2．71倍和2．81倍;但与其脂质体无显著差异。姜黄素醇质体4℃条件下冷藏1个月,其外观、包封率、粒径及多分散指数（PDI）变化较小。结论：醇质体作为透皮给药载体能促进姜黄素的透皮吸收,并能增加皮肤中的滞留量;姜黄素醇质体具有一定的稳定性。     

新型药物载体-醇质体的特点及研究进展

醇质体作为一种新型脂质体,具有包封率高、变形性好、皮肤刺激性小、透皮效果佳、皮肤滞留量大、可以进行细胞内传递药物等优点,使其在经皮给药过程中更加有效.本文根据国内外文献,对醇质体的特点、透皮吸收性及在抗感染药、激素透皮给药、关节炎用药及大分子药物透皮递送等方面的应用进行综述,结果表明醇质体具有良好的应用前景和开发价值.     

芎姜超临界CO_2提取物透皮凝胶的经皮渗透研究

目的:研究川芎、炮姜超临界CO2提取物透皮凝胶(简称芎姜超临界CO2提取物凝胶)的经皮渗透性。方法:通过透皮扩散仪测定芎姜超临界CO2提取物凝胶经离体大鼠皮肤的渗透性,分别以藁本内酯、6-姜酚为指标成分,高效液相色谱(HPLC)法测定药物含量求算累积渗透量(Q)与稳态透皮速率(JS)。结果:芎姜超临界CO2提取物凝胶中藁本内酯和6-姜酚均能有效经皮渗透,Js分别为(47.57±3.77)、(8.29±1.47)μg/(cm2·h),14 h平均累积渗透百分数分别为(26.99±1.89)%和(14.40±1.18)%。结论:芎姜超临界CO2提取物凝胶具有良好的经皮渗透性,经皮给药有望作为芎姜超临界CO2提取物的一种新给药途径。     

In vitro study of ethosome penetration in human skin and hypertrophic scar tissue

The purpose of this study is to characterize a novel transdermal delivery carrier, ethosomes containing 5-fluorouracil. The delivery of drugs from ethosomes in human hypertrophic scar (HS) and the mechanisms of action of ethosomes in human HS were investigated. Percutaneous ethosome permeation was evaluated in vitro in human HS and skin using a Franz's cell. The amount of 5-fluorouracil that permeated HS and skin after 24 hours was most abundant in ethosomes via HS (E-Scar), followed by hydroethanolic solution via HS (H-Scar), ethosomes via skin (E-Skin), and hydroethanolic solution via skin (H-Skin). The penetration of ethosomes in HS and skin was analyzed by ethosomes fluorescently labeled with rhodamine 6GO using confocal laser scanning microscopy. The fluorescence intensity after application for 24 hours was highest in E-Scar, followed by E-Skin, H-Scar, and H-Skin, which indicates the penetration of ethosomes in HS was greatest. In conclusion, we consider that ethosomes are a highly efficient carrier in HS.     

Ethosomes,binary ethosomes and transfersomes of terbinafine hydrochloride: A comparative study

The aim of this study was to compare the skin permeation of ethosomes, binary ethosomes and transfersomes of Terbinafine Hydrochloride (TH) under non-occlusive conditions. These lipid vesicles were prepared and characterized for shape, size, zeta-potential and entrapment efficiency. Franz diffusion cells and confocal laser scanning microscopy (CLSM) were used for the percutaneous absorption studies. The quantity of drug in the skin from ethosomes, binary ethosomes (the weight ratio of ethanol to propylene glycol 7:3, ethanol-PG = 7:3, w/w), and transfersomes was 1.26, 1.51 (p <0.05), 1.56 (p <0.01) times higher than that of TH from traditional liposomes (control). The skin deposition of the applied dose (DD%) of TH from ethosomes, binary ethosomes, and transfersomes was 3.34 (p < 0.05), 9.88 (p < 0.01), 2.52 times higher than that of TH from control. The results of CLSM experiments showed that penetration depth and fluorescence intensity of Rhodamine B from binary ethosomes was much greater than that from ethosomes and transfersomes. These results indicated the binary ethosomes (ethanol-PG = 7:3, w/w) most effectively permitted drug penetration through skin; transfersomes made drug easiest to accumulate in the skin. Ethosomes improved drug delivery with greater improvement in skin permeation than improvement in skin deposition.     

Comparative study of liposomes,transfersomes, ethosomes and cubosomes for transcutaneous immunisation: characterisation and in vitro skin penetration

Objectives Lipid colloidal vaccines, including liposomes, transfersomes, ethosomes and cubosomes, were formulated, characterised and investigated for their ability to enhance penetration of a peptide vaccine through stillborn piglet skin in vitro. Methods Liposomes and transfersomes were formulated using a film‐hydration method, ethosomes using a modified reverse phase method and cubosomes using a lipid precursor method. The size, zeta potential, peptide loading and interfacial behaviour of the formulations were characterised. Skin penetration studies were performed using Franz diffusion cells with piglet skin as the membrane. The localization of peptide in the skin was examined using confocal laser scanning microscopy. Key finding The various formulations contained negatively charged particles of similar size (range: 134–200 nm). Addition of the saponin adjuvant Quil A to the formulations destabilised the monolayers and reduced peptide loading. Cubosomes and ethosomes showed superior skin retention compared with the other systems. Confocal laser scanning microscopy showed greater peptide penetration and accumulation in the skin treated with cubosomes and ethosomes. With the other systems peptide was only located in the vicinity of the hair follicles and within the hair shaft. Conclusions We conclude from the in‐vitro studies that cubosomes and ethosomes are promising lipid carriers for transcutaneous immunisation.     

根皮素醇质体的制备、表征及对体外透皮吸收的影响

目的：制备根皮素醇质体,考察醇质体作为根皮素经皮给药载体的可行性。方法：乙醇注入法制备根皮素醇质体。采用包封率和粒径为考察指标,正交试验优化大豆磷脂用量、胆固醇用量、乙醇体积及水浴温度。测定根皮素醇质体粒径分布、多分散指标和Zeta电位,采用Franz扩散池比较根皮素及其醇质体体外透皮特征。结果：根皮素醇质体最佳处方工艺：磷脂用量为220 mg、胆固醇用量为14 mg、乙醇体积为5 mL、水浴温度为40℃,根皮素醇质体平均包封率为（83.09±1.24）%,载药量为（4.86±0.89）%,粒径为（162.19±5.88） nm,PDI为（0.067±0.011）;Zeta电位为（-15.09±2.16） mV。根皮素以醇质体形式给药后单位累积透过量提高了3.43倍,且渗透过程符合零级动力学。结论：醇质体具有包封率高,粒径分布均匀等特点,可提高根皮素的渗透速率和经皮渗透量,值得进一步研究。     

醋氯芬酸醇质体的制备及体外经皮渗透考察

目的:制备醋氯芬酸(ACF)醇质体并考察其对离体大鼠的透皮能力。方法:采用乙醇注入均质法制备醋氯芬酸醇质体,利用正交试验优化处方;对其粒径、包封率、形态及大鼠离体皮肤经皮渗透量进行考察。结果:优选处方为乙醇用量45%,大豆磷脂用量3%,醋氯芬酸用量0.35%。制备的醇质体平均粒径为102 nm,包封率为48%。醋氯芬酸醇质体的24 h经皮渗透量为821.8μg.cm-2是其45%乙醇溶液的6.36倍。结论:醇质体能显著提高醋氯芬酸经皮渗透量,是经皮给药的优良载体。     

Topical delivery of 5-aminolevulinic acid-encapsulated ethosomes in a hyperproliferative skin animal model using the CLSM technique to evaluate the penetration behavior

Psoriasis, an inflammatory skin disease, exhibits recurring itching, soreness, and cracked and bleeding skin. Currently, the topical delivery of 5-aminolevulinic acid-photodynamic therapy (ALA–PDT) is an optional treatment for psoriasis which provides long-term therapeutic effects, is non-toxic and enjoys better compliance with patients. However, the precursor of ALA is hydrophilic, and thus its ability to penetrate the skin is limited. Also, little research has provided a platform to investigate the penetration behavior in disordered skin. We employed a highly potent ethosomal carrier (phosphatidylethanolamine; PE) to investigate the penetration behavior of ALA and the recovery of skin in a hyperproliferative murine model. We found that the application of ethosomes produced a significant increase in cumulative amounts of 5–26-fold in normal and hyperproliferative murine skin samples when compared to an ALA aqueous solution; and the ALA aqueous solution appeared less precise in terms of the penetration mode in hyperproliferative murine skin. After the ethosomes had been applied, the protoporphyrin IX (PpIX) intensity increased about 3.64-fold compared with that of the ALA aqueous solution, and the penetration depth reached 30–80 μm. The results demonstrated that the ethosomal carrier significantly improved the delivery of ALA and the formation of PpIX in both normal and hyperproliferative murine skin samples, and the expression level of tumor necrosis factor (TNF)-α was reduced after the ALA–ethosomes were applied to treat hyperproliferative murine skin. Furthermore, the results of present study encourage more investigations on the mechanism of the interaction with ethosomes and hyperproliferative murine skin.     

粉防已碱纳米醇质体的制备、表征和抗关节炎疗效(英文)

本研究旨在探索醇质体用于改善粉防己碱局部给药治疗关节炎的可行性。用pH梯度法制备醇质体, 并对其粒径、形态和包封率进行表征。所制备的粉防己碱醇质体为球形, 平均粒径约为78 nm, 包封率为 (52.87±3.81)%。而粉防己碱脂质体具有较大的粒径 (99 nm) 和较高的包封率 (98.80±0.01)%。此外, 与粉防己碱脂质体相比, 粉防己碱醇质体显示出显著的体外透皮性能和抗大鼠关节炎疗效, 并与市售地塞米松软膏的疗效无显著性差异。结果表明, 醇质体有望成为粉防己碱皮肤局部给药的纳米载体。