生物粘附给药系统的研究进展

本文阐明了生物粘附给药系统的概念，讨论了影响生物粘附性的因素，综述了生物粘附性的体内，体外研究方法，并对常见的剂型及给药途径进行了概述。     

生物粘附给药系统进展概况

目的：介绍生物粘附给药系统国内的研究状况。方法：收集国内近年来有关文献，内容包括生物粘附给药系统的作用机理、常用粘附剂的制剂、质量评价、测定方法等。结果：生物粘附给药系统作用机理比较明确，不同部位不同作用特点的粘膜制剂已有较多的报道和应用。结论：生物粘附给药系统具有较高的生物利用度，应用前景较好。     

生物粘附与粘膜粘贴剂的进展

凡能与生物组织粘膜粘附的高分子化合物称生物粘附剂,其作用产生的现象即称生物粘附(Bioadhesion)。近年来利用生物粘附作用的粘膜粘贴剂发展迅速。粘膜粘贴剂可应用于口腔、鼻腔、眼眶、阴道及胃肠道的特定区段,通过该处上皮细胞粘膜输送药物,由于剂型特点加强药物与粘膜接触的紧密性及持续性,因而有利于药物的吸收。而且利用粘膜粘贴剂很容易控制药物吸收的速率及吸收量。生物粘附定义两种物质中有一种或两种均为生物属     

生物粘附性给药系统的研究

生物粘附性给药系统是年年来药剂学的研究热点,它以特有的缓、控释优势而成为很有前途的剂型。本文对生物粘附作用原理、生物粘附性制剂的给药特点、剂型及发展趋向等进行综述。     

生物粘附给药系统研究进展

本文收集了国内近年来有关生物粘附给药系统研究状况的文献,对生物粘附给药系统的作用机理、常用粘附材料、生物粘附制剂技术的应用等进行了综述,表明生物粘附给药系统具有较高的生物利用度,应用前景广阔。     

口服特异性生物粘附给药系统常用材料的研究进展

根据目前国内外相关文献报道，对口服特异性生物粘附给药系统的常用材料及其制备方法进行了综述，并对它们在口服给药系统中的潜在应用进行了探讨，旨在为研究开发新型口服给药系统提供新的思路和方法。     

生物粘附凝胶剂的研究进展

天然或合成的大分子亲水凝胶与机体组织产生长时间的粘附作用称为生物粘附作用，在此基础上研制出来的一种新型药物释放系统被叫作生物粘附释放系统。生物粘附释放系统的作用部位可以是各种腔道的表皮黏膜或皮肤表层．其剂型可以是片剂、膜剂、棒剂、粉剂、软膏等。生物粘附凝胶剂(Bioadhesive Gels)是近年发展较快的一种新型生物粘附释药系统．为一种半固体制剂．除了具有药效持久、应用方便、可避开首过效应等生物粘附剂的特性外．还具有分散性好、粘附力强、稳定性好、给药部位局部浓度高等特点．因而国内外对它的研发相当重视．已有不少品种问世。     

生物粘附制剂的进展

生物粘附制剂是应用于组织粘膜的一类新型制剂。本文综述了生物粘附机理、常用的生物粘附材料以及生物粘附制剂的进展。     

胃粘附片及粘附辅料的体外评价

用改良的粘附力测定法,测定了片剂中常用的添加剂对几种辅料粘附性的影响,并以阿莫西林为模型药物进行了体外粘附性及药物释放的研究。     

Innovations in bioadhesive vaginal drug delivery system

Introduction: Vagina, due to its anatomical position and physiological characteristics is increasingly being explored as a site for drug delivery in recent years. This route coupled with bioadhesion phenomena has born fruitful results in delivering drugs both locally as well as systemically.

Areas covered: Bioadhesive vaginal drug delivery system has been used for the treatment of local diseases affecting the vagina like candidiasis, STD, vaginal dryness, and so on. Also, research has demonstrated that drugs can be successfully delivered to systemic circulation via vaginal mucosa for treatment of various diseases like migraine and osteoporosis. Besides, this vaginal route has also been used for uterine targeting of drugs. This review focuses on these recent innovations that have been patented in the area of bioadhesive vaginal drug delivery systems. The review also highlights certain physicochemical characteristics of bioadhesive polymers that affect drug delivery through this route.

Expert opinion: An in-depth study of this review will give an insight into the potential areas that can be explored while designing a bioadhesive vaginal drug delivery system. Also, the in vitro and in vivo experimental results discussed in the review will help stimulate research in development and optimization of newer formulations.     

灌流冲洗法评价阴道用凝胶的生物粘附性能

目的 采用灌流冲洗法评价阴道用凝胶的生物粘附性能.方法 采用单因素实验,考察了冲洗速度、冲洗液、温度、样品管材料对灌流冲洗速度的影响,确定灌流冲洗条件.结果 灌流冲洗条件:流速为0.5 ml·min-1;灌流冲洗介质为水;温度为37℃;样品管为软质硅胶管.结论 可以采用灌流冲洗方法评价阴道用凝胶的生物粘附性能.     

胃肠道生物黏附给药系统研究进展

胃肠道生物黏附给药系统(GBDDS)是指利用聚合物与胃、肠黏膜黏液层/上层细胞表面之间的生物黏附,延长药物制剂在胃肠道停留时间或特定部位作用时间的给药系统,在缓控释给药系统中占重要地位.现对胃肠道生物黏附作用的机制、影响因素、生物黏附材料的种类和生物黏附制剂的体内外评价方法进行综述,旨在为研究开发新型口服给药系统提供新的思路和方法.     

Development of Biodegradable Starch Microspheres for Intranasal Delivery

Domperidone microspheres for intranasal administration were prepared by emulsification crosslinking technique. Starch a biodegradable polymer was used in preparation of microspheres using epichlorhydrine as cross-linking agent. The formulation variables were drug concentration and polymer concentration and batch of drug free microsphere was prepared for comparisons. All the formulations were evaluated for particle size, morphological characteristics, percentage drug encapsulation, equilibrium swelling degree, percentage mucoadhesion, bioadhesive strength, and in vitro diffusion study using nasal cell. Spherical microspheres were obtained in all batches with mean diameter in the range of above 22.8 to 102.63 μm. They showed good mucoadhesive property and swelling behaviour. The in vitro release was found in the range of 73.11% to 86.21%. Concentration of both polymer and drug affect in vitro release of drug.     

Cationic lipid emulsions as potential bioadhesive carriers for ophthalmic delivery of palmatine

Palmatine (PM) is a potent anti-infective agent used to treat eye diseases. However, PM is less effective for ocular application due to short residence time within the eyes. This study aimed to develop a cationic lipid emulsions (CLEs) for ophthalmic delivery of PM and evaluate its suitability in infection treatment. PM-loaded CLEs (PM-CLEs) were prepared through emulsifying/high-pressure homogenisation and characterised by particle size, ζ potential and morphology. The resulting PM-CLEs possessed a particle size of 192?nm and ζ potential of 45?mV around. In vitro release illustrated that PM was released less from CLEs. Corneal bioadhesion test showed that PM-CLEs exhibited an enhanced ocular residence time. Improved anti-infective activity was achieved in the model of fungus-induced keratitis. Furthermore, PM-CLEs demonstrated predominant cellular uptake and internalisation in the corneal epithelial cells. These results provide proof of concept that CLEs are promising bioadhesive carriers for ophthalmic delivery of PM.     

放线菌素D阴道生物黏附片的研制

目的：研制一种持续作用时间长，毒副作用小的放线菌素D阴道生物黏附片。方法：以放线菌素D为主药，卡波姆934（CP934）、羟丙基纤维素（HPC）、乳糖、酸碱产气系统（碳酸氢钠和枸橼酸）为辅料。采用正交设计试验制备了不同处方的放线菌素D阴道生物黏附片。同时用自制黏附力测定装置测定了黏附片的黏附力；用桨法测定了体外释药速率。结果：最优处方为CP934：HPC=2：3，乳糖用量20％，酸碱产气系统用量5％。结论：本制剂工艺简单、可行，可通过调节处方配比，获得生物黏附力和体外释药均较理想的处方。     

生物黏附制剂的研究进展

目的对生物黏附制剂研究进展进行综述。方法参考近几年国内外文献30余篇,介绍利用生物黏附材料作为制剂载体,以给药途径的不同阐述生物黏附新剂型的研究进展。结果目前生物黏附制剂给药途径一般分为口腔给药、眼部给药、鼻黏膜给药、胃肠道给药和阴道盆腔给药。利用各种具有生物黏附功能的辅料,制备不同剂型的制剂,给药后黏附于特定给药部位,可以控制释药速率,提高靶部位药物浓度,进而提高疗效。结论归纳总结国内外生物黏附制剂最新研究进展,生物黏附制剂具有良好的缓、控释释药及靶向给药等优势,具有较高的市场开发潜力。     

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。     

Application of pectin in oral drug delivery

Introduction: Biopolymers have been used extensively in the pharmaceutical field. Pectin, a biopolymer, has several unique properties that enable it to be used as an excipient or carrier for oral drug delivery systems. Accordingly, several investigators have identified the benefits of pectin-based delivery systems for oral drug administration.

Areas covered: This review first describes the chemical structure, source and production, degree of esterification and gel formation properties of pectin. The application of pectin in various oral drug delivery platforms is also discussed, that is, controlled release systems, gastro-retentive systems, colon-specific delivery systems and mucoadhesive delivery systems.

Expert opinion: Pectin from different sources provides different gelling abilities, due to variations in molecular size and chemical composition. Like other natural polymers, a major problem with pectin is inconsistency in reproducibility between samples, which may result in poor reproducibility in delivery characteristics. Scintigraphic studies and in vivo studies, in both animals and human volunteers, demonstrate the successful development of a pectin-based colon-specific drug delivery system. Pectin-based controlled release systems, gastro-retentive systems and mucoadhesive systems present promising approaches for increasing the bioavailability of drugs, but are in their infancy. A lack of direct correlation between in vitro release and in vivo absorption studies is a major concern with these systems.     

Mucoadhesion of Hydroxypropylmethacrylate Nanoparticles to Rat Intestinal Ileal Segments in Vitro

The purpose of this study was to evaluate the adhesion of HPMA nanoparticles to mucus using a perfused rat ileum test system. Radiolabeled nanoparticles were prepared and deposited onto rat ileal segments in vitro. The segments were perfused and the perfusate was collected in fractions and assayed for radioactivity. Between 10 and 50% of the radioactivity was eliminated over the first 120-sec perfusion, whereas the remaining activity was firmly attached to the ileum. Among the variables tested, the time interval between nanoparticle deposition and perfusion played the major role, indicating that the mucus-nanoparticle interaction is likely to result from the diffusion of polymers into the mucus and of mucin into the polymeric matrix.