壳聚糖在新型给药系统中的应用

综述壳聚糖的物理化学和生物特性及在基因转染和不同给药系统中的应用研究近况。壳聚糖作为新型药用辅料,已受到越来越多的关注,对其应用的开发和研究已渗透到药剂学的多个领域。壳聚糖用作非病毒基因载体,也已成为近年来的研究热点之一。它也被广泛研究应用于眼部、鼻腔、口腔、胃内、小肠和结肠等靶向给药载体。     

阿昔洛韦眼用壳聚糖纳米粒的制备及家兔生物利用度研究

目的:应用离子交联法制备阿昔洛韦壳聚糖纳米粒,考察其体外性质及其经家兔眼部给药后的生物利用度.方法:壳聚糖与三聚磷酸钠通过离子交联作用制备纳米粒,考察了纳米粒的粒径、Zeta电位、包封率以及体外释放性质,通过家兔眼部结膜囊内给药,考察眼房水中药物浓度的变化,并与市售阿昔洛韦滴眼液相比较.结果:阿昔洛韦壳聚糖纳米粒的平均粒径为235 nm,多分散系数为0.256,Zeta电位为43.9 mV;平均包封率为15.6%,平均载药量为1.9%;家兔眼部给药后,AUC0→6 h达到3.69μg·h-1·mL-1,是市售制剂的2.4倍.结论:实验初步证实制备的壳聚糖纳米粒可以促进阿昔洛韦的眼部吸收.     

壳聚糖及其衍生物在智能给药系统中的应用

本文从单重敏感性智能给药系统、多重敏感性智能给药系统及生物传感器着手,主要介绍了壳聚糖及其衍生物在智能给药系统中的研究进展,并展望了其在智能给药系统中的应用前景。     

壳聚糖及其衍生物在药学研究领域的新进展

介绍了壳聚糖及其衍生物在药学领域的最新研究进展,重点阐述了壳聚糖及其衍生物的生物黏附性、促吸收作用和酶抑制剂的功能载体作用,及其在新型给药系统开发中的应用.     

壳聚糖纳米粒的研究进展

壳聚糖是一类带正电的直链多糖，具有良好的生物相容性和生物可降解性，且具有多种生物活性，能有效增加药物通过眼部、鼻腔及胃肠道粘膜上皮的吸收，降低药物的吸收前代谢，提高药物的生物利用度，因此壳聚糖在缓控释给药系统中具有广阔的应用前景，但其溶解性能有待于进一步提高。本文就壳聚糖纳米粒的制备方法、作物特点及应用作一概述。     

眼部给药剂型的研究进展

目的介绍眼部给药剂型的特点与发展。方法根据文献综述了眼部给药剂型及给药系统的特点和应用。结果目前滴眼剂、眼膏、眼用膜剂广泛应用于治疗眼病,眼部给药系统如原位凝胶给药系统、胶体给药系统、微球、植入剂等可以明显地提高药物的生物利用度。结论眼用给药系统在药学领域中有着广阔的发展前景。     

提高角膜滞留性的策略：黏附材料及递药系统的应用进展

由于眼睛复杂的解剖结构和特殊的保护屏障使得眼部给药存在很多挑战。传统的眼用制剂普遍存在剂量损失大、停留时间短等亟待解决的关键问题。通过改善药物在眼部的滞留性能，可以提高药物的眼内生物利用度。一方面是使用黏膜黏附聚合物，如壳聚糖及其季铵衍生物、聚乙二醇、透明质酸和卡波姆等，增强制剂与角膜的黏附作用；另一方面利用纳米递药体系及原位凝胶系统与眼部黏膜的相互作用，延长药物在眼部的停留时间。因此，本文基于改善药物角膜滞留性，对新型眼部递药体系及可修饰制剂性能的生物黏附性材料进行综述，并结合二者优势，旨在为新材料和新制剂用于眼部疾病的治疗提供有效参考。     

壳聚糖及其衍生物作为促渗剂在经皮给药系统中的研究进展

壳聚糖及其衍生物具有良好的生物特性,广泛应用于医药领域中。近些年,越来越多的研究发现其应用于经皮给药系统中具有一定的促渗作用,因此本文对壳聚糖及其衍生物在经皮给药系统中的透皮促渗机制、应用及前景进行综述。     

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。     

壳聚糖衍生物胶束的功能化修饰及其在不同给药系统中的应用进展

目的:综述壳聚糖(CS)衍生物胶束功能化修饰及其在不同给药系统中的应用进展,以期为其深入研究和应用提供参考。方法:以"壳聚糖""胶束""给药系统""Chitosan""Micelle""Drug delivery system"等为关键词,组合查询1995年1月-2019年5月在中国知网、万方数据、Web of Science等数据库中发表的相关文献,对其各衍生物胶束的功能化修饰及其在不同给药系统中的应用进行综述。结果与结论:共检索到相关文献478篇,其中有效文献37篇。CS作为一种性能优良、可修饰性强、生物相容性高的天然高分子材料,可通过疏水骨架、长循环、P-糖蛋白抑制、靶向、刺激信号响应等多种功能化修饰装载疏水性药物,制成CS衍生物胶束,在黏膜给药、眼部给药、口服给药等多种给药系统中均展现出巨大的应用潜力。目前,CS衍生物胶束在解决难溶性药物溶解度、促进药物渗透、增强靶向、提高生物利用度等方面已取得长足发展,但多停留在体外研究,且对详细作用机制的研究较少。若要将其成功应用于临床,尚需对CS衍生物胶束的体内稳定性、药物释放度、药物靶向效率等关键问题进行深入考察。     

Impact of chitosan composites and chitosan nanoparticle composites on various drug delivery systems: A review

Chitosan is a promising biopolymer for drug delivery systems. Because of its beneficial properties, chitosan is widely used in biomedical and pharmaceutical fields. In this review, we summarize the physicochemical and drug delivery properties of chitosan, selected studies on utilization of chitosan and chitosan-based nanoparticle composites in various drug delivery systems, and selected studies on the application of chitosan films in both drug delivery and wound healing. Chitosan is considered the most important polysaccharide for various drug delivery purposes because of its cationic character and primary amino groups, which are responsible for its many properties such as mucoadhesion, controlled drug release, transfection, in situ gelation, and efflux pump inhibitory properties and permeation enhancement. This review can enhance our understanding of drug delivery systems particularly in cases where chitosan drug-loaded nanoparticles are applied.     

壳聚糖微/纳米粒在定向给药系统中的应用研究

目的：介绍壳聚糖微/纳米粒在新型定向给药系统中的应用,为发展安全高效的壳聚糖微/纳米粒定向给药系统提供参考。方法：综合近年来出版的有关文献,对壳聚糖基本性质,定位给药于各组织部位进行了探讨。结果：壳聚糖微/纳米粒可应用于脑、眼、鼻、口、肺、胃、小肠、结肠等器官靶向给药。结论：壳聚糖微/纳米粒作为一种新型药用辅料,在定位给药系统中已经得到了开发和应用。     

A review of implantable intravitreal drug delivery technologies for the treatment of posterior segment eye diseases

Intravitreal implantable device technology utilizes engineered materials or devices that could revolutionize the treatment of posterior segment eye diseases by affording localized drug delivery, responding to and interacting with target sites to induce physiological responses while minimizing side‐effects. Conventional ophthalmic drug delivery systems such as topical eye‐drops, systemic drug administration or direct intravitreal injections do not provide adequate therapeutic drug concentrations that are essential for efficient recovery in posterior segment eye disease, due to limitations posed by the restrictive blood‐ocular barriers. This review focuses on various aspects of intravitreal drug delivery such as the impediment of the blood‐ocular barriers, the potential sites or intraocular drug delivery device implantation, the various approaches employed for ophthalmic drug delivery and includes a concise critical incursion into specialized intravitreal implantable technologies for the treatment of anterior and posterior segment eye disease. In addition, pertinent future challenges and opportunities in the development of intravitreal implantable devices is discussed and explores their application in clinical ophthalmic science to develop innovative therapeutic modalities for the treatment of various posterior segment eye diseases. The inherent structural and functional properties, the potential for providing rate‐modulated drug delivery to the posterior segment of the eye and specific development issues relating to various intravitreal implantable drug delivery devices are also expressed in this review. © 2009 Wiley‐Liss, Inc. and the American Pharmacists Association J Pharm Sci 99: 2219–2239, 2010     

壳聚糖及其衍生物在药物载体中的应用

摘 要壳聚糖及其衍生物具有无毒、良好的生物相容性和可降解性、黏膜黏附性和促渗性等优点,在药物载体领域具有较为广阔的研究及应用前景。本文结合国内外最新发表的相关文献,对壳聚糖及其衍生物作为相关药物载体的应用以及作用机制进行分析讨论,并对其作为抗肿瘤药物靶向载体、缓控释药物载体、眼用药物载体、基因载体和凝胶基质的应用及研究进展进行综述。     

D-Optimal Design in the Development of Rheologically Improved In Situ Forming Ophthalmic Gel

In situ forming ophthalmic gels need to be fine tuned considering all the biopharmaceutical challenges of the front of the eye in order to increase drug residence time at the application site resulting in its improved bioavailability and efficacy. The aim of this study was to develop in situ forming ophthalmic poloxamer P407/poloxamer P188/chitosan gel fine tuned in terms of polymer content, temperature of gelation, and viscosity. Minimizing the total polymer content while retaining the advantageous rheological properties has been achieved by means of D-optimal statistical design. The optimal in situ forming gel was selected based on minimal polymer content (P407, P188, and chitosan concentration of 14.2%, 1.7%, and 0.25% w/w, respectively), favorable rheological characteristics, and in vitro resistance to tear dilution. The optimal in situ forming gel was proved to be robust against entrapment of active pharmaceutical ingredients making it a suitable platform for ophthalmic delivery of active pharmaceutical ingredients with diverse physicochemical properties.     

眼用凝胶剂研究进展

凝胶剂因其优良的成型性、黏弹性、载药量、生物相容性好和眼部滞留时间长的优点,已广泛应用于眼部给药系统.根据国内外眼用凝胶剂的研究现状,本文简要综述了眼用凝胶剂的性质、分类、常用的聚合物及应用情况等.     

Pharmacokinetics and in vivo fate of drug loaded chitosan nanoparticles

Chitosan is a natural polysaccharide which is generally biodegradable, biocompatible and mucoadhesive, thus, attracting considerable interest of scientific researchers. The application of chitosan as nanocarriers for drug delivery thrived. And some of their pharmacokinetics and biodistribution profiles were studied, which are crucial to develop a promising drug delivery system. In this article, we will first give an introduction for the chitosan as drug delivery system, especially as nanoparticles. Then, we focus on pharmacokinetics studies of various chitosan nanoparticles both in vitro and in vivo. In a following part, we refer to researches on biodistribution properties of chitosan nanoparticles. Here we crucially discuss the in vivo fate of chitosan nanoparticles. And finally, toxicity issue is discussed and conclusions are drawn.     

Potential applications of chitosan in veterinary medicine

Chitosan is a partially deacetylated polymer obtained from the alkaline deacetylation of chitin which is a glucose-based unbranched polysaccharide widely distributed in nature as the principal component of exoskeletons of crustaceans and insects as well as of cell walls of some bacteria and fungi. Chitosan exhibits a variety of physicochemical and biological properties resulting in numerous applications in fields such as waste and water treatment, agriculture, fabric and textiles, cosmetics, nutritional enhancement, and food processing. In addition to its lack of toxicity and allergenicity, and its biocompatibility, biodegradability and bioactivity make it a very attractive substance for diverse applications as a biomaterial in pharmaceutical and medical fields, where it has been used for systemic and local delivery of drugs and vaccines. It also has bioactive properties in its own right. This paper reviews current veterinary applications for chitosan including wound healing, bone regeneration, analgesic and antimicrobial effects. It also discusses the potential application of chitosan to drug and vaccine delivery in veterinary species. Given the restrictions imposed by financial and animal restraint considerations, especially in farming applications, the veterinary drug delivery areas most likely to benefit from chitosan are the delivery of chemotherapeutics such as antibiotics, antiparasitics, anaesthetics, painkillers and growth promotants to mucosal epithelium for absorption for local or systemic activity, and the delivery of immunomodulatory agents to the mucosal associated lymphoid tissue for induction or modulation of local immune responses. The properties of chitosan expected to enhance these functions are discussed, and the future research directions in this field are indicated.     

凝胶材料及其在经皮给药系统中的应用与研究进展

凝胶材料具有触感舒适、透气性好、高粘弹性等其他材料所无法比拟的优势,在经皮给药系统中备受青睐,被广泛应用于现代经皮给药制剂如贴剂、贴膏剂、凝胶剂、膜剂当中。随着医药材料的创新发展,许多具有优异功能的新型凝胶材料涌现,使经皮给药制剂的应用范围得到扩大,性能得以优化。通过综述凝胶材料的分类、性能及其在经皮给药系统中的应用,总结最新研究进展,为凝胶材料在经皮给药系统的创新应用提供借鉴和参考。