脂质体经皮给药研究进展

目的:分析总结近年来国外脂质体经皮或黏膜给药研究的特点和应用进展。方法:对近年来脂质体药物特点,主要对在皮肤疾病和美容方面,对局部伤口的治疗,在皮肤损伤和保护中的应用,在眼科疾病中的应用进行综述。结果与结论:脂质体是一种很好的定向药物载体,它的应用范围将越来越广     

脂质体-皮肤局部给药系统的研究进展

目的:介绍近年来脂质体在皮肤局部应用的研究进展.方法:查阅相关文献,对脂质体在皮肤局部应用的作用特点、脂质体的材料进行概述.结果:脂质体对皮肤具有选择作用,能提高皮肤局部药物浓度,降低全身给药时引起的毒副作用.结论:脂质体皮肤局部给药系统具有广阔的前景.     

含醇脂质体在透皮给药系统中的应用研究进展

目的 探讨含醇脂质体在透皮给药系统中的应用。方法 通过阐述脂质体在透皮给药系统中的特点、醇质体的制备、透皮吸收的实验及临床研究。了解含醇脂质体在透皮给药系统中的应用。结果 含醇脂质体应用于透皮给药系统具有许多优点,如醇质体能显著促进渗透。增加药物在皮肤中的滞留量。结论 含醇脂质体在透皮给药系统中的应用有巨大的发展潜力,有望成为一类新型的皮肤给药制剂。     

盐酸阿莫罗芬乙醇脂质体的制备及评价

目的：制备盐酸阿莫罗芬乙醇脂质体并对其进行体内外评价。方法：采用注入法制备盐酸阿莫罗芬乙醇脂质体并测定其体外释放百分率;采用Franz扩散池进行离体皮肤渗透实验,测定盐酸阿莫罗芬在接受液内的累积渗透百分数;在激光共聚焦显微镜下观察不同罗丹明B（探针药物）制剂在小鼠皮肤内分布的情况。结果：盐酸阿莫罗芬乙醇脂质体体外释放速度较慢;乙醇脂质体透过皮肤进入接受液中的药物量分别为乙醇溶液及脂质体的1.7和3倍,乙醇脂质体可有效增加探针药物的透皮量和穿透深度。结论：乙醇脂质体可显著提高盐酸阿莫罗芬的皮肤渗透性及增加皮内滞留量。     

脂质体药物治疗免疫性和皮肤疾病的研究

脂质体的应用可以提高药物的治疗指数,减少药物的治疗剂量和降低药物的毒性.脂质体药物已用于自身免疫性甲状腺炎、实验过敏性脑脊髓炎、角膜移植排斥反应等免疫性疾病的实验性治疗,还可用于痤疮、皮肤念珠菌病、丘疹脓泡性粉刺等皮肤疾病的治疗.     

硝酸益康唑脂质体凝胶的释放和经皮渗透性研究

目的：比较自制硝酸益康唑脂质体凝胶与市售硝酸益康唑霜剂的离体皮肤渗透性,探讨脂质体作为硝酸益康唑的载体对皮肤的渗透机制。方法：测定硝酸益康唑脂质体的体外释放百分率,采用双室渗透池作为离体皮肤的渗透试验装置,测定硝酸益康唑在接受液内的累计渗透百分数和在皮肤内的滞留百分数。结果：硝酸益康唑脂质体的体外释放速度较慢,其凝胶和霜剂透过皮肤进入接受液中的药物量都很少,累计渗透百分数均小于硝酸益康唑给药量的5%;其凝胶制剂的皮肤层内的滞留百分数（26%）高于其霜剂在皮肤层内的滞留百分数（11%）,2种不同制剂的经皮渗透性均符合Higuchi方程。结论：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。     

脂质体经皮局部给药研究进展

目的：探讨脂质体在皮肤局部给药系统中的作用.方法：通过阐述脂质体在皮肤给药系统中透皮吸收的作用机制、影响因素以及在各领域的应用,了解脂质体在皮肤局部给药系统中的作用.结果：脂质体应用于皮肤局部给药系统具有许多优势.结论：脂质体在皮肤局部给药系统中有很大的发展潜力.     

脂质体在鼻腔给药中的应用

通过介绍脂质体的特点，指出脂质体在鼻腔给药的优点。探讨脂质体在鼻腔黏膜的作用机制。利用脂质体增加药物鼻腔黏膜的透过吸收的原理，可以对疾病进行有效的治疗。介绍脂质体作为鼻腔药物载体的研究现状，展望脂质体纳米化是脂质体鼻腔给药药物的发展趋势。     

新型药物载体非离子表面活性剂囊泡的应用研究进展

目的：介绍新型药物载体非离子表面活性剂囊泡的应用研究进展。方法：检索近几年国内外相关文献，对其组成制备、理化性质特点特别是作为药用载体的应用研究作出综述。结果：非离子表面活性剂囊泡是和脂质体相似的新型给药系统，不仅具有脂质体优点，同时能克服脂质体不稳定易氧化变质的缺点，具有更高的稳定性；其在药物输送领域得到广泛研究，国内外研究者已经把囊泡系统应用于多种给药途径的研究。结论：非离子表面活性剂囊泡作为脂质体的替代载体在药物传输领域有着广泛的应用前景。     

脂质体肺部给药的研究进展

目的：介绍脂质体肺部给药的方式，评价其安全性。方法：查阅国内外有关文献进行综合分析。结果：主要概述近年来国内外有关脂质体作为抗菌药物、平喘药物、抗癌药物、多肽和蛋白类药物以及基因药物的载体，通过肺部给药发挥局部或全身疗效的研究。结论：可有效地减少药物对正常组织的刺激性和毒性，增加药物疗效；在基因工程上的应用为肺部给药开拓了更为广阔的前景。     

Transfollicular Drug Delivery

The hair follicle, hair shaft, and sebaceous gland collectively form what is recognized as the pilosebaceous unit. This complex, three-dimensional structure within the skin possesses a unique biochemistry, metabolism and immunology. Recent studies have focused on the hair follicle as a potential pathway for both localized and systemic drug delivery. Greater understanding of the structure and function of the hair follicle may facilitate rational design of drug formulations to target follicular delivery. Targeted drug delivery may enhance current therapeutic approaches to treating diseases of follicular origin. Presented here is a review of follicular drug delivery and a discussion of the feasibility of the pilosebaceous unit as a target site.     

Strategies for therapy of retinal diseases using systemic drug delivery: relevance of transporters at the blood-retinal barrier

INTRODUCTION: There is an increasing need for managing rapidly progressing retinal diseases because of the potential loss of vision. Although systemic drug administration is one possible route for treating retinal diseases, retinal transfer of therapeutic drugs from the circulating blood is strictly regulated by the blood-retinal barrier (BRB). AREAS COVERED: This review discusses the constraints and challenges of drug delivery to the retina. In addition, this article discusses the properties of drugs and the conditions of the BRB that affect drug permeability. The reader will gain insights into the strategies for developing therapeutic drugs that are able to cross the BRB for treating retinal diseases. Further, the reader will gain insights into the role of BRB physiology including barrier functions, and the effect of influx and efflux transporters on retinal drug delivery. EXPERT OPINION: When designing and selecting optimal drug candidates, it's important to consider the fact that they should be recognized by influx transporters and that efflux transporters at the BRB should be avoided. Although lipophilic cationic drugs are known to be transported to the brain across the blood-brain barrier, verapamil transport to the retina is substantially higher than to the brain. Therefore, lipophilic cationic drugs do have a great ability to increase influx transport across the BRB.     

Drug delivery to the eye with a transdermal therapeutic system

A matrix-type transdermal therapeutic system was developed for treating diseases of the eye where it is difficult for drug molecules to reach with conventional topical instillation. Prednisolone was employed as a model drug. An in vivo study using rats showed that the daily application of the patch maintained a constant plasma concentration of the drug, which was equivalent the therapeutic plasma level following three times daily oral administration (30 mg), for approximately 24 h. Transdermal delivery provided equivalent to or higher bioavailability (drug distribution) to the eyeball of topical administration. Moreover, pharmacokinetic analysis indicated that the present transdermal therapeutic system may be clinically effective as a new treatment for ocular diseases.     

Intracochlear drug delivery systems

INTRODUCTION: Advances in molecular biology and in the basic understanding of the mechanisms associated with sensorineural hearing loss and other diseases of the inner ear are paving the way towards new approaches for treatments for millions of patients. However, the cochlea is a particularly challenging target for drug therapy, and new technologies will be required to provide safe and efficacious delivery of these compounds. Emerging delivery systems based on microfluidic technologies are showing promise as a means for direct intracochlear delivery. Ultimately, these systems may serve as a means for extended delivery of regenerative compounds to restore hearing in patients suffering from a host of auditory diseases. AREAS COVERED: Recent progress in the development of drug delivery systems capable of direct intracochlear delivery is reviewed, including passive systems such as osmotic pumps, active microfluidic devices and systems combined with currently available devices such as cochlear implants. The aim of this article is to provide a concise review of intracochlear drug delivery systems currently under development and ultimately capable of being combined with emerging therapeutic compounds for the treatment of inner ear diseases. EXPERT OPINION: Safe and efficacious treatment of auditory diseases will require the development of microscale delivery devices, capable of extended operation and direct application to the inner ear. These advances will require miniaturization and integration of multiple functions, including drug storage, delivery, power management and sensing, ultimately enabling closed-loop control and timed-sequence delivery devices for treatment of these diseases.     

Cell-mediated drug delivery

INTRODUCTION: Drug targeting to sites of tissue injury, tumor or infection with limited toxicity is the goal for successful pharmaceutics. Immunocytes (including mononuclear phagocytes (dendritic cells, monocytes and macrophages), neutrophils and lymphocytes) are highly mobile; they can migrate across impermeable barriers and release their drug cargo at sites of infection or tissue injury. Thus, immune cells can be exploited as Trojan horses for drug delivery. AREAS COVERED: This paper reviews how immunocytes laden with drugs can cross the blood-brain or blood-tumor barriers to facilitate treatments for infectious diseases, injury, cancer, or inflammatory diseases. The promises and perils of cell-mediated drug delivery are reviewed, with examples of how immunocytes can be harnessed to improve therapeutic end points. EXPERT OPINION: Using cells as delivery vehicles enables targeted drug transport and prolonged circulation times, along with reductions in cell and tissue toxicities. Such systems for drug carriage and targeted release represent a new disease-combating strategy being applied to a spectrum of human disorders. The design of nanocarriers for cell-mediated drug delivery may differ from those used for conventional drug delivery systems; nevertheless, engaging different defense mechanisms in drug delivery may open new perspectives for the active delivery of drugs.     

皮肤病治疗药物的临床应用与进展

目的：了解皮肤病治疗药物，展示近年来皮肤病治疗药物的临床应用与进展，为临床合理用药提供参考依据。方法：分四类介绍了皮肤病治疗药物，包括：1．抗细菌药物2．抗病毒药物3．中药内服制剂4．中药外用制剂。结果：抗菌药物和抗病毒药物在当代皮肤病和性病治疗中发挥了极其重要的作用，临床应用呈上升趋势，天然药物种类偏少，有广阔的开发前景，且越来越多的应用于临床。     

Strategies for therapy of retinal diseases using systemic drug delivery: relevance of transporters at the blood–retinal barrier

Introduction: There is an increasing need for managing rapidly progressing retinal diseases because of the potential loss of vision. Although systemic drug administration is one possible route for treating retinal diseases, retinal transfer of therapeutic drugs from the circulating blood is strictly regulated by the blood–retinal barrier (BRB).

Areas covered: This review discusses the constraints and challenges of drug delivery to the retina. In addition, this article discusses the properties of drugs and the conditions of the BRB that affect drug permeability. The reader will gain insights into the strategies for developing therapeutic drugs that are able to cross the BRB for treating retinal diseases. Further, the reader will gain insights into the role of BRB physiology including barrier functions, and the effect of influx and efflux transporters on retinal drug delivery.

Expert opinion: When designing and selecting optimal drug candidates, it's important to consider the fact that they should be recognized by influx transporters and that efflux transporters at the BRB should be avoided. Although lipophilic cationic drugs are known to be transported to the brain across the blood–brain barrier, verapamil transport to the retina is substantially higher than to the brain. Therefore, lipophilic cationic drugs do have a great ability to increase influx transport across the BRB.     

Site-specific drug delivery in the skin for the localized treatment of skin diseases

ABSTRACT

Introduction: Due to the well-organized structure and barrier function of the skin, it is generally difficult for drugs applied directly on the surface of skin to reach their expected site of action. Accordingly, site-specific drug delivery in the skin has been increasingly explored to facilitate the treatment of skin diseases and reduce the systemic toxicity.

Area covered: An overview of the generally used sites for drug delivery in the skin is herein presented. Different strategies including particle-based carriers, physical technologies, and chemical approaches are discussed with regards to their potential application in site-specific drug delivery in the skin.

Expert opinion: Particle-based carriers are of particular significance for the enhancement of drug delivery in the skin. Although no recommendation can be made regarding which type of carriers can provide better skin penetration, the lipid-based colloidal systems appear to be favored due to their compatibility. In addition, the physical technologies provide unique advantages in delivering hydrophilic macromolecules for the skin immunization. As a new class of permeation enhancers, skin penetrating peptides are gaining more attention in drug delivery to skin cells. For the design of robust site-specific drug delivery systems, the impacts of diseased state and drug properties should not be disregarded.     

New Techniques for Drug Delivery to the Posterior Eye Segment

Ocular drug delivery has become an increasingly important field of research especially when treating posterior segment diseases of the eye, such as age-related macular degeneration, diabetic retinopathy, posterior uveitis and retinitis. These diseases are the leading causes of vision loss in developed countries which require repeated long-term administration of therapeutic agents. New drugs for the medication of the posterior ocular segment have emerged, but most drugs are delivered by repeated intravitreal injections associated with ocular complications. Advances in ocular drug delivery system research are expected to provide new tools for the treatment of the posterior segment diseases, providing improved drug penetration, prolonged action, higher efficacy, improved safety and less invasive administration, resulting in higher patient compliance. This review provides an insight into the recent progress and trends in ocular drug delivery systems for treating posterior eye segment diseases, with an emphasis on transscleral iontophoresis.     

Percutaneous Permeation of Betamethasone 17-Valerate Incorporated in Lipid Nanoparticles

Corticosteroids are therapeutic agents widely used in the pharmacological treatment of skin diseases such as eczema or psoriasis. Unfortunately, their use is restricted by the side effects that frequently occur at the systemic level. The goal of the research described here was to develop and characterize a solid lipid nanoparticle (SLN) system containing corticosteroids for prolonged and localized delivery of the active drugs into the skin. In vitro measurements of Betamethasone 17-valerate (BMV) permeation through human epidermis were conducted using static Franz diffusion cells. The reservoir formation of the drug in the epidermal and dermal layers of the skin was also investigated. Monostearin SLN showed remarkable controlled release properties and a significant epidermis drug reservoir. On the other hand, beeswax SLN could not reduce the drug permeation through the skin, nor increase the drug content in the upper layers of the skin. The diffusion of corticosteroids into the skin appeared to be dependent on the lipid composition of the monostearin SLN. Topical SLN products show great potential for treating dermatological conditions by targeting corticosteroids to epidermal/upper dermal disease sites while minimizing systemic drug absorption.