传递体作为双氯芬酸钠经皮渗透载体的体外研究

目的传递体作为双氯芬酸钠经皮渗透载体的体外研究.方法采用改良Franz扩散池体外经皮渗透实验技术,对双氯芬酸钠传递体、普通脂质体及其凝胶剂的经皮渗透作用进行了比较.结果24 h后双氯芬酸钠传递体、普通脂质体及其凝胶剂的累积透皮量分别为598.16μg·cm-2,209.15μg·cm-2,391.33μg·cm-2.皮肤内滞留量Q滞分别为191.54μg·cm-2,419.28μg·cm-2,8.77μg·cm-2.结论以传递体作为双氯芬酸钠的载体可以促进其经皮渗透,且皮内的滞留药物还表现出一定的贮库效应.而普通脂质体不能很好地促进药物透过皮肤,但利于药物在皮内的大量滞留.     

氟尿嘧啶泡囊凝胶剂的体外透皮试验

目的:研究氟尿嘧啶泡囊凝胶剂的体外透皮扩散率及皮内滞留率。方法:建立用分光光度法测定氟尿嘧啶的方法,通过离体鼠皮透皮扩散试验,测定氟尿嘧啶泡囊凝胶的透皮扩散率及皮外残留率,并与氟尿嘧啶凝胶剂和医院制剂乳膏等作对照。结果:氟尿嘧啶泡囊凝胶剂的12 h的透皮累积扩散率仅为乳膏的10%,但皮内滞留率却增加2倍以上。结论:氟尿嘧啶泡囊凝胶剂可大大减少透过皮肤进入全身的药量,显著增加局部浓度,利于提高对皮肤病的疗效和降低全身毒性。     

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。     

阿西美辛脂质体凝胶剂的体外透皮扩散研究

目的探究分析阿西美辛（ACM）脂质体凝胶剂的体外透皮扩散效果。方法使用离体鼠皮进行试验,在离体鼠皮上面使用阿西美辛脂质体凝胶剂还有阿西美辛凝胶剂,对比2种药物在不同时间点的体外透皮量、凝胶层滞留量还有皮肤层滞留量等数据,对比2种制剂的体外透皮规律,归纳其体外透皮扩散效果。结果2种制剂体外透皮扩散效果对比具有显著差异性（P〈0．05）,阿西美辛脂质体凝胶剂头皮扩散行为相对于阿西美辛凝胶剂更具有优越性,在24h透过药量累积达到40％,而相对于阿西美辛凝胶剂其皮肤层里面的滞留量也更具有优越性;而ACM没有经过包封则难以穿透皮肤,会有大量剂量依然存留在凝胶剂当中。结论使用阿西美辛脂质体凝胶剂能够使得药物透皮量极为显著的提高,是一种阿西美辛的外用新型制剂,值得临床推广。     

姜黄素脂质体的制备及体外透皮研究

采用乙醇注入法制备了姜黄素脂质体.采用透皮扩散试验仪进行体外透皮试验,比较姜黄素的溶液(含0.5％吐温-80)及其脂质体经小鼠离体皮肤的累积渗透量及皮肤滞留量.结果表明,12h时姜黄素脂质体的皮肤累积透过量和滞留量分别为姜黄素吐温-80溶液的2.11和3.05倍.脂质体作为姜黄素的透皮给药载体能促进姜黄素的透皮吸收,并能增加其在皮肤中的滞留量.     

阿西美辛脂质体凝胶剂的体外透皮扩散研究

目的：研究阿西美辛(ACM)脂质体凝胶剂的体外透皮扩散。方法：采用Franz扩散池，离体鼠皮，分别考察不同时间点阿西美辛脂质体凝胶剂与阿西美辛凝胶剂的体外造度量、皮肤层滞留量、凝胶层滞留量，并对两种制剂的体外造皮规律进行拟合，得出规律方程。结果：阿西美辛脂质体凝肢剂与阿西美辛凝胶剂的透皮扩散行为差异有显著性。前者可显著提高药物的造皮药量，24h时累积透过药量约40％，且在皮肤层内的滞留量多于ACM凝胶剂；而ACM在非包封状态下，不易穿速皮肤，大部分仍存在于凝胶剂中。结论：阿西美辛脂质体凝胶剂可显著提高药物的造度量，有望成为阿西美辛的一种外用新剂型。     

乳酸左氧氟沙星脂质体凝胶剂经小鼠在/离体的透皮吸收

目的:研究乳酸左氧氟沙星脂质体凝胶剂的皮肤渗透性。方法:以普通凝胶剂为对照,将乳酸左氧氟沙星脂质体制备成凝胶剂并应用于小鼠皮肤,用改良的Franz扩散池研究其透皮速率,以高效液相色谱法测定接受液、皮肤、血液及其他组织中的乳酸左氧氟沙星的含量。结果:所制脂质体凝胶剂有较大的透皮速率,平均为(13.5±1.0)μg.cm-2.h-1(n=6),透皮吸收行为符合Fick’s第一定律;经皮吸收结果显示体内吸收量均较普通凝胶剂低,而皮内滞留量无论是在体还是离体均较高。结论:该制剂具有良好的局部皮肤靶向性。脂质体有促进药物进入皮肤的能力,而药物进入血循环的量并不增加。     

甘草酸二铵脂质囊泡的体外经皮渗透研究

目的 考察不同种类的甘草酸二铵(DG)脂质囊泡的体外经皮渗透情况,并制备脂质囊泡凝胶剂。方法 分别采用非质子传递溶剂法制备磷脂复合物,薄膜分散法制备柔性脂质体,注入法制备醇质体,并测定粒径;采用改良的Franz扩散池,以离体人皮进行经皮渗透实验;HPLC测定接收液和皮肤组织中药物含量。最后,将皮肤渗透性较好的囊泡处方制备成凝胶剂,考察凝胶的经皮渗透情况。结果 DG磷脂复合物24 h累计透过量为(8.07±5.42)μg·cm^-2,其余处方透过液中均未检测到药物。24 h药物在皮肤中的累积量大小顺序为磷脂复合物>醇质体>柔性脂质体>水溶液。DG磷脂复合物凝胶透皮效果与卡波姆浓度有关,0.5%卡波姆处方的皮肤中药物滞留量为1%卡波姆处方的2.2倍,降低卡波姆的浓度不但能提高DG在表皮层的含量,而且还能使药物进一步渗透至真皮层。结论 磷脂复合物能显著促进DG在皮肤中的渗透,并增加药物在皮肤中的蓄积。采用0.5%卡波姆制备磷脂复合物凝胶具有较好的经皮渗透性。     

局部用咪喹莫特泡囊凝胶剂的制备、表征及皮内滞留效应

目的:制备并表征局部用咪喹莫特泡囊凝胶剂,考察药物皮内滞留效应。方法:制备并表征咪喹莫特泡囊凝胶剂,离体鼠皮透皮实验考察药物皮内滞留量和透过量,切片观察药物皮内分布。结果:泡囊的平均粒径197.2 nm,Zeta电位-42.97 m V,包封率27.44%;泡囊凝胶剂体外释放t1/2与泡囊相似,但为凝胶剂的4.94倍和市售乳膏的3.83倍,12 h透过药量均比凝胶剂和市售乳膏小一半,单位面积皮内药物滞留量约为它们的2倍,切片显示药库效应显著。结论:泡囊凝胶剂具缓释作用和药库效应,可增加皮内滞留,减少角质层拦截和透过皮肤的药量,将有利于皮肤病的治疗,并可降低局部刺激性和全身毒性的风险。     

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。     

Triamcinolone permeation from different liposome formulations through rat skin in vitro

The permeation of triamcinolone acetonide (TRMA) from various liposome formulations through rat skin was studied in vitro. The penetrated amount, permeability and intradermal retention of TRMA were compared among various lipid compositions, different vesicle sizes (0.2, 0.4 and 1 μm), charges (positive, negative and neutral), as well as between multilamellar vesicles (MLV) and small unilamellar vesicles (SUV). All of the liposome formulations resulted in significantly higher flux and permeability of TRMA than a commercial TRMA ointment. The ‘skin lipid’ liposome provided the most effective transdermal delivery of incorporated TRMA. Presence or absence of cholesterol in the lipid bilayers did not reveal any difference in transdermal delivery of the associated TRMA. The flux and permeability of TRMA through skin were not influenced by the vesicle size of MLV, but was significantly increased by negative SUV. Intradermal retention of TRMA from positive MLV was significantly higher, while that from neutral SUV was significantly lower, than from other formulations. Liposomal lipid was not detectable on the receptor compartment. These results suggest that liposome itself may not penetrate through the skin, but that it does enhance the transfer of incorporated TRMA. Liposomal lipid composition is the most important factor affecting the efficiency of transdermal delivery of incorporated drugs, but was not correlated with its phase transition temperature.     

马钱子总碱脂质体凝胶的制备及其体外透皮作用

目的：制备马钱子总碱脂质体凝胶,研究马钱子总碱脂质体凝胶体外透皮特点。方法：采用硫酸铵梯度法制备马钱子总碱脂质体,以泊洛沙姆407为基质制备成脂质体凝胶,采用Franz扩散池比较马钱子总碱脂质体凝胶和普通凝胶的经皮渗透性和皮肤滞留量。结果：马钱子总碱脂质体的平均粒径为140 nm,其中马钱子碱的包封率为82.2%,士的宁的包封率为90.3%。体外透皮实验表明,脂质体凝胶能缓慢的透过小鼠皮肤,皮肤滞留量大于普通凝胶。结论：脂质体是马钱子总碱经皮吸收的理想载体。     

塞来昔布脂质体凝胶的研制及其体外经皮渗透动力学考察

目的研制塞来昔布脂质体凝胶,并对其体外经皮渗透动力学进行考察。方法采用薄膜分散法制备塞来昔布脂质体,均匀设计筛选最佳处方及制备工艺,并以卡波姆940为基质制成脂质体凝胶;用Franz扩散池研究塞来昔布脂质体凝胶与塞来昔布普通凝胶的经皮渗透规律。结果塞来昔布脂质体凝胶的平均粒径为(369.5±10.8)nm,平均包封率为(81.6±2.2)%(n=3);体外透皮试验表明塞来昔布脂质体凝胶的累积透过量显著大于普通凝胶(P<0.05),药物透皮速率与皮肤蓄积量显著大于普通凝胶(P<0.01)。结论塞来昔布脂质体凝胶制备简单,能促进药物透皮吸收,值得进一步研究。     

酮洛芬不同透皮制剂的体外透皮性和释放性

分别制备含1%、3%、5%酮洛芬的混合型巴布剂、交联型巴布剂、透皮贴剂,以同浓度的酮洛芬凝胶剂作为对照组,采用改良Franz透皮扩散池,以离体小鼠皮肤为透皮屏障,考察酮洛芬在不同制剂中的体外透皮和释放性能.结果表明,同浓度酮洛芬在不同受试制剂的透皮速率依序为交联型巴布剂＞混合型巴布剂＞凝胶剂＞透皮贴剂;3%酮洛芬在不同贴膏剂中的释放速率依序为混合型巴布剂＞交联型巴布剂＞透皮贴剂.     

Topical delivery of different acyclovir palmitate liposome formulations through rat skin in vitro

The objective of this investigation was to examine the permeation of acyclovir palmitate from various liposome formulations through hairless rat skin in vitro. The penetrated amount, permeability and intradermal retention of ACV-C16 were compared among various lipid compositions and different vesicle charges. We found that all of the liposome formulations resulted in higher flux and permeability of ACV-C16 than a common ointment form. The 'skin lipid' liposome provided the most effective transdermal delivery of incorporated ACV-C16. Presence or absence of cholesterol in the lipid bilayers did not reveal any difference in transdermal delivery of the associated ACV-C16. Intradermal retention of ACV-C16 from positive liposomes was significantly higher than that from other formulations. These findings suggested that liposomes itself might not penetrate through the skin, but enhance the transfer of incorporated ACV-C16. Liposomal lipid composition was the most important factor affecting the efficiency of transdermal delivery of incorporated drugs, but was not correlated with its phase transition temperature.     

Elastic liposomes mediated transdermal delivery of an anti-hypertensive agent: propranolol hydrochloride

One major problem encountered in transdermal drug delivery is the low permeability of drugs through the skin barrier. In the present investigation ultradeformable lipid vesicles, that is, elastic liposomes were prepared incorporating propranolol hydrochloride for enhanced transdermal delivery. Elastic liposomes bearing propranolol hydrochloride were prepared by conventional rotary evaporation method and characterized for various parameters including vesicles shape and surface morphology, size and size distribution, entrapment efficiency, elasticity, turbidity, and in vitro drug release. In vitro flux, enhancement ratio (ER), and release pattern of propranolol hydrochloride were calculated for transdermal delivery. In vivo study conducted on male albino rats (Sprague Dawley) was also taken as a measure of performance of elastic liposomal, liposomal, and plain drug solution. The better permeation through the skin was confirmed by confocal laser scanning microscopy (CLSM). Results indicate that the elastic liposomal formulation for transdermal delivery of propranolol hydrochloride provides better transdermal flux, higher entrapment efficiency, ability as a self-penetration enhancer and effectiveness for transdermal delivery as compared to liposomes.     

盐酸西替利嗪凝胶剂的制备及体外透皮特性

目的：制备盐酸西替利嗪凝胶剂,研究其体外透皮特性。方法：以卡波姆940为辅料制备西替利嗪凝胶剂,采用改良Franz扩散池,以离体大鼠皮肤为透皮屏障,采用HPLC法测定西替利嗪的透皮行为。结果：西替利嗪凝胶体外透皮释药方程为Q=110．03t＋17．17（r=0．99）,透皮速率为110．03μg/（cm^2·h）。结论：西替利嗪凝胶具有良好的透皮效果,其体外经皮渗透符合一级动力学过程。     

Effect of limonene on the in vitro permeation of nicardipine hydrochloride across the excised rat abdominal skin

The aim of the present investigation was to study the effect of limonene on in vitro permeation of nicardipine hydrochloride across the excised rat abdominal skin from a 2% w/w hydroxypropyl cellulose (HPC) gel. The HPC gel formulations containing 1% w/w of nicardipine hydrochloride and selected concentrations of limonene (0% w/w to 12% w/w) were prepared, and subjected to in vitro permeation of the drug through excised rat abdominal epidermis. The drug content in the gels was found to be uniform and the drug was found to be stable in the HPC gel formulations. The permeation flux of nicardipine hydrochloride across rat epidermis was increased markedly by the addition of limonene to the HPC gels. A maximum flux was observed (246 +/- 1 micrograms/cm2/h) with an enhancement ratio of about 8 when limonene was incorporated at a concentration of 4% w/w. However, there was no further increase in the permeability of nicardipine hydrochloride beyond 4% w/w of limonene. The DSC and FT-IR data indicated that limonene increased the permeability of nicardipine hydrochloride across the rat epidermis by partial extraction of lipids in the stratum corneum. The results suggest that limonene may be useful for enhancing the skin permeability of nicardipine hydrochloride from transdermal therapeutic system containing HPC gel as a reservoir.