透皮给药系统的研究进展

介绍了透皮给药系统的特点、剂型、促渗技术和体内外研究模型,为透皮给药系统的研究提供参考。重点查阅了国外有关透皮给药系统的相关文献并进行分析总结。随着新材料、新技术、新设备的不断发展,促渗方法取得了很大的进步,透皮给药系统具有广阔的发展前景。     

微针给药系统的研究进展

微针是一种具有微米尺度的经皮给药技术,从内部结构可分为实心与空心微针.制作微针的材料主要有硅、金属、聚合物等.微针增强了皮肤对药物尤其是大分子药物的渗透性,不会到达神经分布丰富的皮肤深层组织,并且使用方便,因此是一种高效、无痛、安全的经皮给药方式.微针在胰岛素给药、卵清蛋白的免疫接种、缓控释给药、微量输液等方面的研究为微针经皮给药提供了应用可能.     

几种挥发油对黄藤素透皮给药的促渗作用研究

为给黄藤素透皮给药选择合适的挥发油促渗剂,以高效液相色谱法测定黄藤素的含量,采用立式扩散池法研究桉叶油、艾叶油、当归油、连翘油对黄藤素透皮给药的影响;实验结束后,用DSC扫描观察皮肤的特征峰变化。结果表明,5 h时,艾叶油组药物的累积透过量分别是被动扩散组、桉叶油组、当归油组、连翘油组的1.82,1.16,1.48,1.63倍,药物的累积渗透量随着艾叶油浓度的增加而增加,艾叶油浓度1.5%时,其促渗能力最强。DSC图谱表明,不同挥发油对皮肤的特征峰具有不同的影响,促渗能力较好的挥发油使皮肤的特征峰消失;当艾叶油的浓度由0.5%增加到1.5%,DSC图谱发生相应变化,浓度为1.5%和2.0%时具有相似的图谱,而浓度为2.5%时的DSC图谱与0.5%的图谱相似。艾叶油能够显著促进黄藤素的透皮给药,且最佳的浓度为1.5%,其机理可能是通过扰乱或破坏皮肤角质层的有序结构来增强皮肤对药物的渗透性,因此,艾叶油可作为黄藤素透皮给药的理想促渗剂而具有广泛的应用前景。     

几种挥发油对黄藤素透皮给药的促渗作用研究

为给黄藤素透皮给药选择合适的挥发油促渗剂,以高效液相色谱法测定黄藤素的含量,采用立式扩散池法研究桉叶油、艾叶油、当归油、连翘油对黄藤素透皮给药的影响;实验结束后,用DSC扫描观察皮肤的特征峰变化。结果表明,5 h时,艾叶油组药物的累积透过量分别是被动扩散组、桉叶油组、当归油组、连翘油组的1.82,1.16,1.48,1.63倍,药物的累积渗透量随着艾叶油浓度的增加而增加,艾叶油浓度1.5%时,其促渗能力最强。DSC图谱表明,不同挥发油对皮肤的特征峰具有不同的影响,促渗能力较好的挥发油使皮肤的特征峰消失;当艾叶油的浓度由0.5%增加到1.5%,DSC图谱发生相应变化,浓度为1.5%和2.0%时具有相似的图谱,而浓度为2.5%时的DSC图谱与0.5%的图谱相似。艾叶油能够显著促进黄藤素的透皮给药,且最佳的浓度为1.5%,其机理可能是通过扰乱或破坏皮肤角质层的有序结构来增强皮肤对药物的渗透性,因此,艾叶油可作为黄藤素透皮给药的理想促渗剂而具有广泛的应用前景。     

化妆品功能性成分经皮给药与研究

化妆品经皮给药的概念和技术来源于现代药剂学。物质经皮作用全过程 :经皮渗透、皮肤吸收、在作用部位积聚。与药物经皮给药的最大区别 ,化妆品经皮给药的最终目的是功能性成分的经皮渗透 ,在皮肤作用部位积聚并发挥功效作用。脂质体技术是种较好的控制释放系统。利用该技术研究制备维生素A脂体 ,包封率为 98.5 % ,粒径 0 .191μm。     

医用聚合物柔性皮肤给药微针的研究进展

随着微电子机械系统(MEMS)的发展,微针成为科技界的研究热点,并且在生物医学上得到了广泛的应用.微针的应用改善了过去药物注射所遇到的疼痛、效率低下等缺点,显著提高了药物,尤其是大分子药物注射的性能.由于聚合物材料具有应用广泛、价廉、生物相容性好且可生物降解等特点,聚合物微针得到了越来越广泛的关注.主要介绍近年来聚合物微针的加工材料、结构、力学性能分析及其研究进展,并提出运用微注射加工聚合物微针的前景.     

药物纤维及其在新型给药系统中的应用

综述了制备药物纤维的材料和技术以及药物纤维在新型给药系统(DDS)中的应用。分析了目前药物纤维DDS技术存在的问题。药物纤维可分为原料型、天然纤维的后整理型、聚合物型及复合型。其制备方法主要有传统纺丝方法、静电纺丝技术、非织造布技术以及后整理技术。指出中草药纤维的DDS、智能释药纤维DDS及多药多级控释DDS是今后药物纤维DDS研究的方向。     

3种促透剂对氨基葡萄糖体外透皮吸收的影响

采用改良Franz扩散池法,以离体大鼠腹部皮肤为透皮屏障,生理盐水为接受液,用UPLC测定接受液中氨基葡萄糖含量,比较3种促透剂对氨基葡萄糖透皮吸收的影响。从而考察3种促透剂对氨基葡萄糖体外透皮吸收的影响,为氨基葡萄糖经皮给药制剂开发的促透剂选择提供参考。结果显示氮酮、薄荷油和冰片对盐酸氨基葡萄糖皆具有促渗透作用;其中5%薄荷油促透效果最好,平均渗透速率为95.50μg/cm~2/h;3%氮酮效果次之64.45μg/cm~2/h,冰片促透作用最小27.68μg/cm~2/h,使氨基葡萄糖透皮速率分别提高7.38,4.98,2.14倍。因此,证明了促透剂薄荷油、氮酮均可显著增加氨基葡萄糖的透皮吸收,在实验浓度范围内,其中5%薄荷油为最佳促透剂。     

草炭腐植酸钠经皮给药的动力学研究

经皮给药系统(Transderm Delivery Sys-tem.TDS)又称经皮治疗系统(TransdermalTherapeutic System.TTS)是药物以一定的速率通过皮肤、经毛细血管吸收进入体循环产生药效的一类制剂。经皮给药系统近十年来发展很快。据不完全统计美国1986-1988年的药学年会中就有200余篇有关透皮吸收的研究论文;日本1985年和1986年在东京召开了两次学术讨论会,有61篇关于经皮给药的学术论文发表;法国、英国经皮给药的研究也同样是热门领域。我国1985年以来,经皮给药系统研究发展也很快,1987-1990年各种药学刊物公开发表论文25篇。     

Microneedle Array-Based Platforms for Future Theranostic Applications

Theranostics involves finding the biomarkers of a disease, fighting them through site specific drug delivery and following them for prognosis of the disease. Microneedle array technology has been used for drug delivery and extended for continuous monitoring of analytes present in the skin compartment. We envisage the use of microneedle arrays for future theranostic applications. The potential of combining microneedle array-based drug delivery and diagnostics as part of closed-loop control system for the management of diseases and delivery of precision drugs in individual patients is reported in this paper.     

Microwave‐Assisted Preparation of Hydrogel‐Forming Microneedle Arrays for Transdermal Drug Delivery Applications

A microwave (MW)‐assisted crosslinking process to prepare hydrogel‐forming microneedle (MN) arrays was evaluated. Conventionally, such MN arrays are prepared using processes that includes a thermal crosslinking step. Polymeric MN arrays were prepared using poly(methyl vinyl ether‐alt‐maleic acid) crosslinked by reaction with poly(ethylene glycol) over 24 h at 80 °C. Polymeric MN arrays were prepared to compare conventional process with the novel MW‐assisted crosslinking method. Infrared spectroscopy was used to evaluate the crosslinking degree, evaluating the area of the carbonyl peaks (2000–1500 cm^?1). It was shown that, by using the MW‐assisted process, MN with a similar crosslinking degree to those prepared conventionally can be obtained in only 45 min. The effects of the crosslinking process on the properties of these materials were also evaluated. For this purpose swelling kinetics, mechanical characterisation, and insertion studies were performed. The results suggest that MN arrays prepared using the MW assisted process had equivalent properties to those prepared conventionally but can be produced 30 times faster. Finally, an in vitro caffeine permeation across excised porcine skin was performed using conventional and MW‐prepared MN arrays. The release profiles obtained can be considered equivalent, delivering in both cases 3000–3500 μg of caffeine after 24 h.

     

Transdermal Drug Delivery Systems and Their Use in Obesity Treatment

Transdermal drug delivery (TDD) has recently emerged as an effective alternative to oral and injection administration because of its less invasiveness, low rejection rate, and excellent ease of administration. TDD has made an important contribution to medical practice such as diabetes, hemorrhoids, arthritis, migraine, and schizophrenia treatment, but has yet to fully achieve its potential in the treatment of obesity. Obesity has reached epidemic proportions globally and posed a significant threat to human health. Various approaches, including oral and injection administration have widely been used in clinical setting for obesity treatment. However, these traditional options remain ineffective and inconvenient, and carry risks of adverse effects. Therefore, alternative and advanced drug delivery strategies with higher efficacy and less toxicity such as TDD are urgently required for obesity treatment. This review summarizes current TDD technology, and the main anti-obesity drug delivery system. This review also provides insights into various anti-obesity drugs under study with a focus on the recent developments of TDD system for enhanced anti-obesity drug delivery. Although most of presented studies stay in animal stage, the application of TDD in anti-obesity drugs would have a significant impact on bringing safe and effective therapies to obese patients in the future.     

紫杉醇聚合物胶束载药体系的研究进展

紫杉醇（paclitaxel,PTX）是一种常用的抗肿瘤药物,但其极差的水溶性限制了其在临床上的应用。为使其能更好的为人体所利用,近年来,研究者们开发了多种紫杉醇载药体系,其中聚合物胶束载药体系以其特有的优点为目前研究的热点,并具有广阔的发展前景。介绍了近年来采用两亲嵌段共聚物制备紫杉醇聚合物给药体系的研究进展。展望了该体系今后的发展方向。     

Development of transdermal drug‐delivery films with castor‐oil‐based polyurethanes

Two different types of polyurethanes (PUs) were prepared with castor oil, ethylene glycol, isophorene diisocyanate and castor oil, and isophoren diisocyanate and poly‐(ethylene glycol) (400 or 600). PU films were prepared and characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, and gel permeation chromatography. We prepared transdermal patches by loading different amounts of drug, plasticizer, and penetration enhancer. In vitro drug permeability through the castor‐oil‐based aliphatic PU patches was examined with a Keshary–Chien diffusion cell. The effect of castor oil on the film‐forming properties and the effect of penetration enhancers on diffusion characteristics of indomethacin (IDM) drug through the castor‐oil‐based PU were investigated. Prolonged release of IDM was observed from the prepared PU patches. In vitro drug diffusion revealed that slow and prolonged release of IDM was achieved in the absence of penetration enhancers. The use of penetration enhancers showed a significant effect on drug diffusion. © 2006 Wiley Periodicals, Inc. J Appl Polym Sci 103: 779–788, 2007     

Evaluation of micellar architecture based on functionalized chitosan for the in vitro release of an antibiotic

Polymeric micelles are enjoying high resurgence of interest in biomedical field as promising candidates for the delivery of water-insoluble drugs. This property was used to design and synthesize fatty acid grafted polysaccharide-based copolymer micelles for the sustained release of Cefixime trihydrate (CFX): a third-generation cephalosporin. Chitosan (CS), a polysaccharide obtained by the alkaline deacetylation of chitin emerged as a useful drug delivery matrix because of its polycationic nature, biodegradability, biocompatibility and mucoadhesiveness. The drug release was monitored in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (7.4). The in vitro release studies revealed 52% of drug release after 24 h of incubation and were enhanced to 83% after 72 h in simulated intestinal fluid condition. Antibacterial studies confirmed that the inherent properties of the drug were retained as well as enhanced by micelle formation. Thus, the synthesized copolymer micelle assures to be an excellent carrier vehicle for the sustained release of a model hydrophobic drug CFX. Smaller particle size ensures increased drug uptake and controlled release facilitates patient compliance.     

脂质体在化妆品中的研究进展

介绍了国内外脂质体作为化妆品载体的研究进展。通过对脂质体作为化妆品活性成分载体的特点,脂质体经皮吸收的促透机制及影响其吸收的因素和最新的基础实验和应用研究进展的综合分析显示,脂质体在化妆品领域中的应用具有广阔的前景。     

(Trans) dermal insulin delivery based on polymeric systems

Abstract

Diabetes is one of the leading lethal diseases, which is often treated by hypodermic injection of insulin or by oral delivery. Oral drug delivery systems show limitations due to poor absorption and degradation that occurs in the GI tract and in the liver. Due to the patient discomfort that leads to poor patient compliance, alternative methods to administer insulin are of great interest. In recent years, much attention has been paid to transdermal delivery devices because of drug? delivery reliability to a target site with patient-friendly technologies. The major part of integumentary systems is skin, but skin drug delivery is challenging due to barrier properties exhibited by the outermost layer of skin stratum corneum. Transdermal drug delivery systems (TDDS) control the rate of release of the drug into the patient so that blood concentration maintains a steady state, and gastrointestinal absorption is avoidable. Controlled drug release causes minimum side effects and improves bioavailability of drugs, which showed poorly bioavailable drugs over other routes of delivery. The limiting factor in TDDS is stratum corneum, which is the outer layer of the skin and which acts as an effective barrier to the transport of biomolecules into the skin. For this reason, an effective method for drug delivery is hypodermic injection, which is a painful delivery. Besides, it needs a high level of expertise to administer the injection and the occasional risk of infections acquired through needle sticks. In recent year^’s microneedle (MN)-mediated drug delivery systems have been developed which can meet all the above goals.

?Microneedles are microscopic needles, which can deliver the drug to the target site by the degradation or dissolution of the polymer in the skin after insertion. This results in delivery of the encapsulated molecules, and no needles are left afterward. Microneedles are large and strong enough to insert into the skin and to deliver drugs into the skin, but they are short enough so that they do not reach the deeper layers of the skin to cause nerves stimulation. Microneedles offer an efficient and attractive method for delivering several classes of biomolecules and drugs to the skin in a self-administered manner. The overall goal of this research is TDDS and polymer micromodels system for insulin drug delivery, which can deliver an active biopharmaceutical in vivo for producing the desired physiological response.     

Characterisation of the Molecular Mechanism of Permeation of the Prodrug Me-5ALA across the Human Stratum Corneum Using Molecular Dynamics Simulations

The barrier imposed by the outer layer of the skin, the stratum corneum, creates an almost impermeable environment for exogenous substances. Few lipophilic drugs with low molecular mass can passively diffuse through this layer, highlighting the need to develop methods to enable the delivery of more drugs via the transdermal route. The prodrug approach involves modifying the structure of a drug molecule to enhance its permeability across the skin, but it is often difficult to predict how exactly changes in chemical structure affect permeation. This study uses molecular dynamics simulations to predict permeability values and adequately characterise the molecular mechanism of permeation of the prodrugs Me-5ALA and its parent compound 5ALA across a molecular model of the lipid bilayers of the human stratum corneum. The influence of increased hydrophobicity in Me-5ALA on its permeation revealed a reduction in hydrogen bonding capability that enables it to interact more favourably with the hydrophobic region of the bilayer and diffuse at a faster rate with less resistance, thus making it a better permeant compared to its more hydrophilic parent compound. This molecular simulation approach offers a promising route for the rational design of drug molecules that can permeate effectively across the stratum corneum.