黏膜黏附聚合物在阴道给药系统中的应用

目的：系统介绍了黏膜黏附聚合物在阴道给药系统各方面的应用，为阴道给药开发新的应用途径提供参考。方法：对近期的文献进行分类、整理和总结。结果：黏膜黏附聚合物通过阴道给药用于改善阴道干燥、避孕、抗感染、免疫治疗、治疗不孕症、抗病毒治疗等。结论：黏膜黏附聚合物已广泛地应用于阴道给药系统中，有较好的应用前景。     

壳聚糖在黏膜给药系统中的应用

目的壳聚糖应用于黏膜给药上的新进展.方法根据国内外近几年来的文献资料,进行整理归纳.结果壳聚糖以其独特的物理化学性质和生物学特征,吸引着人们的注意力,成为一种应用日渐广泛的药用辅料.结论壳聚糖可以在黏膜的控,缓释给药方面发挥重要的作用.     

壳聚糖在黏膜给药系统中的应用

目的壳聚糖应用于黏膜给药上的新进展。方法根据国内外近几年来的文献资料，进行整理归纳。结果壳聚糖以其独特的物理化学性质和生物学特征，吸引着人们的注意力，成为一种应用日渐广泛的药用辅料。结论壳聚糖可以在黏膜的控，缓释给药方面发挥重要的作用。     

壳聚糖在黏膜给药系统中的应用

目的壳聚糖应用于黏膜给药上的新进展。方法根据国内外近几年来的文献资料，进行整理归纳。结果壳聚糖以其独特的物理化学性质和生物学特征，吸引着人们的注意力，成为一种应用日渐广泛的药用辅料。结论壳聚糖可以在黏膜的控，缓释给药方面发挥重要的作用。     

阴道黏膜给药系统的研究进展

目的:综述阴道黏膜给药系统的最新应用进展。方法:根据国内外发表的文献,对阴道黏膜给药系统的应用加以分析和讨论。结果:阴道黏膜给药安全、有效、能避免首关效应、渗透性能强,延长药物滞留时间,提高生物利用度,可以改善患者用药顺应性。结论:阴道黏膜给药系统已成为目前研究的热点,它是传统给药方式的补充,具有广阔的应用前景。     

口腔黏膜黏附制剂的研究概况

口腔黏膜黏附制剂是一种新的药物释放系统,系利用生物黏附材料与口腔黏膜间的生物黏附力,延长制剂在口腔中的滞留时间,控制药物的释放速度和释药量,使制剂产生最佳疗效.该文作者就口腔黏膜黏附制剂的特点、生物黏附材料的选择及近年来的口腔黏膜黏附制剂的研究概况作一综述,并展望了其发展前景.     

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.     

口腔黏膜黏附制剂研究概况

口腔黏膜黏附制剂是一种新的药物释放系统,系利用生物黏附材料与口腔黏膜间的生物黏附力,延长制剂在口腔中的滞留时间、控制药物的释放速度和释药量,使制剂产生最佳疗效.本文就口腔黏膜黏附制剂的特点、生物黏附材料的选择及近年来口腔黏膜黏附制剂的研究概况作一综述,并展望了其发展前景.     

正交试验优选壳聚糖阴道生物黏附膜处方

目的:优选壳聚糖阴道生物黏附膜的最佳处方.方法:通过自制黏附力测定装置以垂直黏附力和切向黏附力为考察指标,利用L9(34)正交试验对处方组成进行优选.结果:各因素的影响大小顺序为:酸性壳聚糖浓度(A)>甘油浓度(C)>药物含量(D)>明胶浓度(B),优选的最佳处方为A2B2C2D3,即酸性壳聚糖浓度为1.0%,明胶浓度为1.5%,甘油浓度为8.0%,药物含量为1.0%.结论:优选的处方具有较好的黏附力和体外释放度.     

眼黏膜黏附聚合物凝胶给药系统简介

任何一种聚合物溶液或混悬液滴入眼部后，若能与角膜和结膜表面的黏蛋白结合，则这种相互作用过程称为黏膜黏附。黏膜黏附可以实现释药体系在特定部位的定位释放。有研究表明，黏膜黏附聚合物与被吸附组织的紧密接触可以提高大分子药物如蛋白质类和多肽类药物的透过性。     

The use of mucoadhesive polymers in vaginal delivery

The vagina is an important area of the reproductive tract and serves as a potential route of drug administration. Beside locally acting drugs it is also of importance for systemic drug delivery, uterine targeting or even vaccination. Currently available dosage forms have several limitations, therefore novel concepts and dosage forms are needed. In this field mucoadhesive polymers will play a major role. After discussion of the anatomy and physiology of the vagina this review highlights the most important studies based on mucoadhesive polymer-systems like poly(acrylates), chitosan, cellulose derivatives, hyaluronic acid derivatives, pectin and traganth, starch, poly(ethylene glycol), sulfated polysaccharides, carrageenan, Na-alginate and gelatine.     

The use of mucoadhesive polymers in buccal drug delivery

Buccal delivery of the desired drug using mucoadhesive polymers has been the subject of interest since the early 1980s. Advantages associated with buccal drug delivery have rendered this route of administration useful for a variety of drugs. This review highlights the use of mucoadhesive polymers in buccal drug delivery. Starting with a review of the oral mucosa, mechanism of drug permeation, and characteristics of the desired polymers, this article then proceeds to cover the theories behind the adhesion of bioadhesive polymers to the mucosal epithelium. Additionally, we focus on the new generation of mucoadhesive polymers such as thiolated polymers, followed by the recent mucoadhesive formulations for buccal drug delivery.     

The use of mucoadhesive polymers in ocular drug delivery

In the present update on mucoadhesive ocular dosage forms, the tremendous advances in the biochemistry of mucins, the development of new polymers, the use of drug complexes and other technological advances are discussed. This review focusses on recent literature regarding mucoadhesive liquid (viscous solutions, particulate systems), semi-solid (hydrogel, in situ gelling system) and solid dosage forms, with special attention to in vivo studies. Gel-forming minitablets and inserts made of thiomers show an interesting potential for future applications in the treatment of ocular diseases.     

Engineering design and molecular dynamics of mucoadhesive drug delivery systems as targeting agents

The goal of this critical review is to provide a critical analysis of the chain dynamics responsible for the action of micro- and nanoparticles of mucoadhesive biomaterials. The objective of using bioadhesive controlled drug delivery devices is to prolong their residence at a specific site of delivery, thus enhancing the drug absorption process. These mucoadhesive devices can protect the drug during the absorption process in addition to protecting it on its route to the delivery site. The major emphasis of recent research on mucoadhesive biomaterials has been on the use of adhesion promoters, which would enhance the adhesion between synthetic polymers and mucus. The use of adhesion promoters such as linear or tethered polymer chains is a natural result of the diffusional characteristics of adhesion. Mucoadhesion depends largely on the structure of the synthetic polymer gels used in controlled release applications.     

Development of mucoadhesive dosage forms of buprenorphine for sublingual drug delivery

The development of mucoadhesive formulations of buprenorphine for intended sublingual usage in the treatment of drug addiction is described. The formulations include mucoadhesive polymer films, with or without plasticizers, and mucoadhesive polymer tablets, with or without excipients that enhance drug release and/or improve tablet compaction properties. The mucoadhesive polymers studied include carbomers such as Carbopol 934P, Carbopol 974P, and the polycarbophil Noveon AA-1, with excipients chosen from pregelatinized starch, lactose, glycerol, propylene glycol, and various molecular weights of polyethylene glycol. The development of plasticizer-containing mucoadhesive polymer films was feasible; however, these films failed to release their entire drug content within a reasonable period. Thus, they were not determined suitable for sublingual usage because of possible loss by ingestion during routine meal intakes. The mucoadhesive strength of tablet formulations containing Noveon AA-1 appears to be slightly superior to the Carbopol-containing tablets. However, the Carbopol 974P formulations exhibited superior drug dissolution profiles while providing adequate mucoadhesive strength. The tablet formulations containing Carbopol 974P as mucoadhesive polymer, lactose as drug release enhancer, and PEG 3350 as compaction enhancer exhibited the best results. Overall, the mucoadhesive tablet formulations exhibited superior results compared with the mucoadhesive film formulations.     

Development of a mucoadhesive nanoparticulate drug delivery system for a targeted drug release in the bladder

Purpose

Purpose of the present study was the development of a mucoadhesive nanoparticulate drug delivery system for local use in intravesical therapy of interstitial cystitis, since only a small fraction of drug actually reaches the affected site by conventional treatment of bladder diseases via systemic administration.

Methods

Chitosan-thioglycolic acid (chitosan-TGA) nanoparticles (NP) and unmodified chitosan NP were formed via ionic gelation with tripolyphosphate (TPP). Trimethoprim (TMP) was incorporated during the preparation process of NP. Thereafter, the mucoadhesive properties of NP were determined in porcine urinary bladders and the release of TMP among simulated conditions with artificial urine was evaluated.

Results

The particles size ranged from 183 nm to 266 nm with a positive zeta potential of +7 to +13 mV. Under optimized conditions the encapsulation efficiency of TMP was 37%. The adhesion of prehydrated chitosan-TGA NP on the urinary bladder mucosa under continuous urine voiding was 14-fold higher in comparison to unmodified chitosan NP. Release studies indicated a more sustained TMP release from covalently cross linked particles in comparison to unmodified chitosan-TPP NP over a period of 3 h in artificial urine at 37 °C.

Conclusion

Utilizing the method described here, chitosan-TGA NP might be a useful tool for local intravesical drug delivery in the urinary bladder.     

The use of the InteliSite Companion device to deliver mucoadhesive polymers to the dog colon

The aims of this study were two-fold; first to report on the use of the novel InteliSite^® Companion device to deliver material to the colon, and second to use this new technology to assess the potential of mucoadhesive polymers to be retained in the large intestine. In this three-way crossover study in beagle dogs, two mucoadhesive polymers and a non-mucoadhesive polymer were remotely delivered in powder form to the colon. The retention of 150 mg doses of the radiolabelled mucoadhesive polymers Carbopol 980 and polycarbophil AA-1, and the retention of ethylcellulose (control) in the colon of three canines was examined using gamma scintigraphy. The InteliSite^® Companion device had a mean gastric emptying time of 1.0 ± 0.8 h and a mean caecal arrival time of 2.3 ± 1.0 h. The device was remotely activated to expel the polymers at the caecum. Although incomplete release was noted with all polymers, Carbopol 980 was found to have increased retention in the proximal colon of all three dogs. The mean retention time within the proximal colon for Carbopol 980 (15.3 ± 1.4 h) was significantly higher than that of polycarbophil AA-1 (10.0 ± 5.7 h) and the control (7.1 ± 1.4 h) (p < 0.05). The increased colon retention time demonstrated by Carbopol 980 may be suggestive of a mucoadhesive effect.     

High efficiency entrapment of superoxide dismutase into mucoadhesive chitosan-coated liposomes

Superoxide dismutase (SOD), antioxidative enzyme and potential anti-inflammatory agent, was encapsulated into mucoadhesive chitosan-coated liposomes in order to increase its releasing time and to facilitate its cellular penetration. Positively, neutrally and negatively charged liposomes were prepared using soybean lecithin, stearylamine, phosphatidyl glycerol and cholesterol. The effects of liposomal lipid composition and protein to lipid ratio on the encapsulation parameters were studied in three preparation methods: dehydration–rehydration, hydration and proliposome methods. The highest efficiency of SOD entrapment, 39–65%, was achieved by the proliposome method. Vesicles prepared by the hydration method entrapped 1–13% and vesicles prepared by dehydration–rehydration entrapped 2–3% of SOD. Stability tests for SOD-loaded liposomes prepared by the proliposome method showed no significant loss of the enzyme activity within 1 month at 4 °C or within 2 days at 37 °C. Positively, neutrally and negatively charged liposomes, prepared by the proliposome method, were successfully coated with two types of low and medium molecular weight chitosans. Both types of chitosan coating increased the mucoadhesive characteristics of all three types of vesicles. Using the proliposome method and subsequent chitosan coating, highly efficient SOD-loaded vesicles for drug targeting on mucosal tissues could be produced.     

Positively charged gelatin microspheres as gastric mucoadhesive drug delivery system for eradication of H. pylori

Gastric mucoadhesive drug delivery systems are very promising for eradication of Helicobacter pylori (H. pylori), a spiral bacterium that resides in the gastric mucus layer and at the mucus- epithelial cell interface. New positively charged biodegradable microspheres were prepared using aminated gelatin by surfactantfree emulsification in olive oil, followed by a cross-linking reaction with glutaraldehyde. The amino group contents of the modified gelatin and the microspheres were determined using a 2,4,6-trinitrobenzenesulfonic acid method. With the increase of glutaraldehyde concentration, the amino group content of the microspheres decreased accordingly. The influence of glutaraldehyde concentration, cross-linking reaction time, drug-loading patterns, and type of release media on the in vitro release characteristics of amoxicillin from the microspheres was investigated. Amoxicillin release rate from the modified gelatin microspheres was significantly reduced compared with that from gelatin microspheres. Furthermore, the release was decreased with the increase of glutaraldehyde concentration and/or cross-linking time. On the other hand, a faster release was observed in a lower pH release medium and/or using a lower pH solution for amoxicillin loading. The gastric mucoadhesive properties of the microspheres were evaluated using RITC-labeled microspheres in an isolated rat stomach. The gastric mucoadhesion of the modified gelatin microspheres was markedly improved compared with that of gelatin microspheres. The modified gelatin microsphere proves to be a possible candidate delivery system for the effective eradication of H. pylori.