Nanoparticle-Mediated Brain-Specific Drug Delivery,Imaging, and Diagnosis

Central nervous system (CNS) diseases represent the largest and fastest-growing area of unmet medical need. Nanotechnology plays a unique instrumental role in the revolutionary development of brain-specific drug delivery, imaging, and diagnosis. With the aid of nanoparticles of high specificity and multifunctionality, such as dendrimers and quantum dots, therapeutics, imaging agents, and diagnostic molecules can be delivered to the brain across the blood-brain barrier (BBB), enabling considerable progress in the understanding, diagnosis, and treatment of CNS diseases. Nanoparticles used in the CNS for drug delivery, imaging, and diagnosis are reviewed, as well as their administration routes, toxicity, and routes to cross the BBB. Future directions and major challenges are outlined.     

磁靶向给药系统的研究进展

磁靶向给药系统有利于提高药物疗效,降低毒副作用,为癌症化疗开辟了新的途径,可望在不久的将来。广泛用于临床。介绍和评价了磁靶向给药系统的制备、性质和药效等,并综述该系统的研究进展。     

肝靶向微粒给药系统的研究进展

目的对近年来微粒给药系统在肝靶向治疗的研究进展做一综述。方法根据国内外文献资料进行整理归纳。结果纳米粒、微球、脂质体及微乳等微粒系统具有被动靶向于肝的趋势,利用肝细胞表面某些受体则可特异性靶向于肝达到主动靶向作用。结论微粒给药系统在肝靶向治疗领域具有重要意义。     

聚合物胶束在肿瘤靶向给药系统中的研究进展

摘 要 聚合物胶束作为一种有效的药物运送载体已经受到广泛关注,其在肿瘤治疗方面具有高效,长效和高载药量等优势。本文综述了聚合物胶束的类型,制备材料,载药方法,主要讨论了肿瘤靶向载药系统中的靶向策略和应用实例。     

脑靶向给药系统研究进展

血-脑屏障阻碍药物进入脑组织,不利于中枢神经系统疾病的治疗.本文介绍了近年来脑靶向给药系统的研究进展,包括通过受体(如载脂蛋白受体、转铁蛋白受体等)介导的主动靶向系统、被动靶向系统(如纳米粒、碳纳米管等)及其他靶向系统(如磁性微粒、阳离子制剂等).     

Drug Delivery Systems for Intraperitoneal Therapy

Disorders associated with the peritoneal cavity include peritoneal adhesions and intraperitoneal (IP) malignancies. To prevent peritoneal adhesions, physical barrier devices are used to prevent organs from contacting other structures in the abdomen and forming adhesions, or pharmacological agents that interfere with adhesion formation are administered intraperitoneally. IP malignancies are other disorders confined to the peritoneal cavity, which are treated by combination of surgical removal and chemotherapy of the residual tumor. IP drug delivery helps in the regional therapy of these disorders by providing relatively high concentration and longer half-life of a drug in the peritoneal cavity. Various studies suggest that IP delivery of anti-neoplastic agents is a promising approach for malignancies in the peritoneal cavity compared to the systemic administration. However, IP drug delivery faces several challenges, such as premature clearance of a small molecular weight drug from the peritoneal cavity, lack of target specificity, and poor drug penetration into the target tissues. Previous studies have proposed the use of micro/nanoparticles and/or hydrogel-based systems for prolonging the drug residence time in the peritoneal cavity. This commentary discusses the currently used IP drug delivery systems either clinically or experimentally and the remaining challenges in IP drug delivery for future development.     

Schizophrenia and Drug Delivery Systems

Abstract

Schizophrenia is a severe non-curable illness of the brain with serious consequences if not properly treated and kept under control. Antipsychotic drugs have revolutionised the therapy and management of schizophrenia. However, patient compliance rates are notoriously poor due to the nature of the disease and troublesome side-effects, and are major causes of symptom recurrence. Although some new antipsychotic agents have been marketed to offer broader efficacy with much reduced side-effect profiles, the drug delivery systems for antipsychotics are still in the stage of conventional dosage forms, such as tablets, capsules and solutions, and need to be dosed at the frequency of 2-4 times daily. Doubtless, novel drug delivery systems, such as sustained and controlled release systems, will be useful for antipsychotics. They should reduce the frequency of dosing, enhance drug bioavailability and improve patient compliance. In this article, the specificity and characterisation of schizophrenia and pathophysiology, drug therapy, and the development and future prospects of neuroleptic drug delivery systems are reviewed.     

药物传递系统和传递策略

一种药物被聚合物或脂质体包裹或吸附,其使用安全性和效率能被极大地改善,并且使新的治疗成为可能。这将为促进可降解材料的设计智能化传递系统和探讨体内各类传递途径等主动性研究提供了原动力。     

ATP-Responsive Drug Delivery Systems

The combination of targeted drug delivery and controlled-release technology may pave the road for more effective yet safer chemotherapeutic options for cancer therapy. Drug-encapsulated polymeric nanoparticle–aptamer bioconjugates represent an emerging technology that can facilitate the delivery of chemotherapeutics to primary and metastatic tumours. Aptamers are short nucleic acid molecules with binding properties and biochemical characteristics that may make them suitable for use as targeting molecules. The goal of this review is to summarise the key components that are required for creating effective cancer targeting nanoparticle–aptamer bioconjugates. The field of controlled release and the structure and properties of aptamers, as well as the criteria for constructing effective conjugates, will be discussed.     

自乳化药物传递系统的应用与前景

自乳化药物传递系统对于亲脂性和难溶性药物是一个非常有希望的新型载体系统。本文综述了自乳化药物的传递系统的物化生物药剂学特性和其目前存在的问题,并预测了该药物传递系统的发展趋势。     

Improved Delivery Through Biological Membranes LX: Intradermal Targeting of Acyclovir Using Redox-Based Chemical Drug Delivery Systems

Two types of novel chemical drug delivery systems (CDS's) for acyclovir, A-CDS-1 (based on oxidation, which utilized the 1,4-dihydrotrigonelline moiety) and A-CDS-2 (based on reduction, which utilized the lipoic acid moiety), were designed to create reservoirs of metabolic precursors for the enhanced local delivery of the antiviral agent acyclovir to the skin. They were evaluated in two-compartment diffusion cells using hairless-mouse skin in vitro. This approach could be useful in the treatment of mucocutaneous herpes simplex virus (HSV-1) infection in the epidermal region of the skin. Upon application to the freshly excised hairless-mouse skin, A-CDS-1 was rapidly oxidized to form the quaternary metabolite AQ⁺, which was extensively localized in the skin. AQ⁺ then served as a reservoir for the release of the antiviral agent in the skin. A-CDS-1 delivered almost equivalent amounts of acyclovir not only to the skin but also transdermally. On the other hand, A-CDS-2 specifically localized acyclovir delivery to the skin as opposed to transdermal delivery. Due to their redox properties, both CDS's demonstrated significant depot formation of metabolic precursors, thus enhancing intradermal acyclovir delivery. The CDS's exhibited greater skin membrane partition coefficients than the parent underivatized acyclovir and were able to release the antiviral agent in the skin tissue. The CDS's were susceptible to hydrolysis in biological media, resulting in the release of acyclovir under near physiological conditions. Thus, the CDS's can serve to enhance intradermal targeting and delivery of the antiviral agent acyclovir.     

生物技术药物给药系统研究进展

生物技术药物给药系统按其途径分为注射和非注射两大结药系统。本文综述了国内外近年来生物技术药物新型给药系统的研究进展。     

Intranasal Delivery of Proteins and Peptides in the Treatment of Neurodegenerative Diseases

The blood–brain barrier (BBB) is a major impediment to the therapeutic delivery of peptides and proteins to the brain. Intranasal delivery often provides a non-invasive means to bypass the BBB. Advantages of using intranasal delivery include minimizing exposure to peripheral organs and tissues, thus reducing systemic side effects. It also allows substances that typically have rapid degradation in the blood time to exert their effect. Intranasal delivery provides the ability to target proteins and peptides to specific regions of the brain when administered with substrates like cyclodextrins. In this review, we examined the use of intranasal delivery of various proteins and peptides that have implications in the treatment of neurodegenerative diseases, focusing especially on albumin, exendin/GLP-1, GALP, insulin, leptin, and PACAP. We have described their rationale for use, distribution in the brain after intranasal injection, how intranasal administration differed from other modes of delivery, and their use in clinical trials, if applicable. Intranasal delivery of drugs, peptides, and other proteins could be very useful in the future for the prevention or treatment of brain related diseases.KEY WORDS: blood–brain barrier, cognition, intranasal, memory     

Vaginal Drug Delivery Systems for HIV Prevention

Microbicides have become a principal focus for HIV prevention strategies. The successful design of drug delivery systems for vaginal microbicide drug candidates brings with it a multitude of challenges. It is imperative that the chemical and physical characteristics of the drug candidate and its mechanism of action be clearly understood and considered to successfully deliver and target drug candidates efficiently. In addition, an understanding of the dynamic nature of the vaginal environment, the tissue and innate barriers present, as well as patient preferences are critical considerations in the design of effective microbicide products. Although the majority of drug candidates clinically evaluated to date have been delivered using conventional semisolid aqueous-based gel dosage forms, drug delivery system design has recently been extended to include advanced delivery systems such as vaginal rings, quick-dissolve films, and tablets. Ultimately, it may be necessary to develop multiple dosage platforms for a single active agent to provide users with options that can be used within the constraints of their social environment, personal choice, and environmental conditions.     

Sustained-Release Delivery Systems for Treatment of Dental Diseases

Sustained-release delivery systems allow the effective targeting of drugs for treating dental and periodontal diseases. Since dental diseases are chronic, the therapeutic agents used should persist in the oral cavity for as long as possible. Implanting fluoride, chlorhexidine, and other antiseptic agents embedded into sustained-release polymeric matrices into the oral cavity prevents cariogenic plaque accumulation. Both fibers and slab-like sustained-delivery devices bearing chemotherapeutic agents reduced periopathogenic bacteria levels associated with clinical improvement. This review provides useful background information for researchers seeking to develop controlled-release delivery systems for dental applications.     

壳聚糖介导的靶向药物传递系统

目的:综述了以壳聚糖或其衍生物为基础的多种特殊靶向载体系统的研究现状。方法:以国内外近年有代表性的文献为依据,进行分析、整理和归纳。结果与结论:由于壳聚糖具有一些独特的物理和生物特性,并且通过修饰后增加了壳聚糖的一些性质,使其成为优良的药物载体,从而实现药物的靶向性。这一载体材料近年来逐渐受到重视,具有良好的开发和应用前景。     

壳聚糖微球给药系统

主要介绍壳聚糖微球的制备方法，影响其载药的主要因素，及其在缓控释、靶向给药、黏膜给药、生物大分子给药等方面的应用。近年来壳聚糖微球作为新型给药系统备受关注。