美国药物输送和治疗杂志 开放获取

抽象的

用質構儀評估不同聚合物與黏膜組織的黏膜黏附性能

法特馬努爾·圖古-德米羅斯

黏膜黏附聚合物是用於各種藥物框架的材料的集合。它們的特徵是親水性大分子，含有各種實用的天然聚集體，可與黏膜建立聯繫。這些聚合物的特徵在於它們與黏膜的連結。用於改善黏膜黏附的非共價鍵包括持氫、疏水合作和靜電連接。黏膜黏附聚合物可以是陽離子、陰離子或非離子的。陰離子聚合物，例如聚丙烯酸衍生物，被認為在體液糖蛋白的羧基團和羥基團之間形成低於其pKa的氫鍵。另外也建議，在羧酸鹽中可能會發生粒子偶極子通訊。此外，聚衍生物還可與熱敏聚合物（如泊洛沙姆 407 (P407)）結合使用，以增強維護能力。考慮到在應用於身體後變稠之前穿過器具的截面，熱響應聚合物在基本溫度下從流體變為黏稠凝膠。黏膜黏附的組成部分通常分為兩個階段：接觸階段和結合階段。主要階段是透過黏膜黏附劑與體液膜之間的接觸來描述的，隨著定義的擴展和擴展，開始與體液層的深度接觸。在結合過程中，黏膜黏附材料是由濕氣的接近而產生的。潮濕使框架塑化，使黏膜黏附顆粒自由分裂並透過脆弱的范德華力和氫鍵連接起來。

黏膜表面將鼻腔、視覺、口腔、直腸、陰道和胃腸道區域分佈在身體的不同部位。藥物可以被引導到這些目的地以實現附近的影響，並且它們的高多孔性使它們對基本的藥物運輸有吸引力。儘管如此，來自這些目的地的常規自由工具限制了生活安排時間，減少了藥物吸收或社區影響的範圍。為了克服這些弱點，創建了「黏膜黏附」框架，該框架透過各種誘人的物理化學關聯牢牢地固定在黏膜上，改善維護，透過這種方式，藥物的充分性黏膜黏附是材料黏附在黏膜的能力。此特性已被廣泛用於創建用於口腔、口腔、鼻腔、視覺和陰道藥物傳遞的聚合物劑量結構。具有帶電聚集體和非離子實用聚集體的親水性聚合物具有令人難以置信的黏膜黏附特性，適合與黏膜表面形成氫鍵。本文探討了黏膜黏附和黏膜黏附聚合物研究的最新進展。它給出了黏膜結構、體液凝膠特性和黏膜黏附概念的圖表。使用黏膜黏附藥物輸送設備的主要目的是延遲他們在特定地點的私人時間，使他們的目標明確，並改善藥物攝入過程。沿著這些思路，黏膜黏附性的估計是規劃黏膜黏附藥物輸送框架的關鍵進步。利用黏膜黏附聚合物材料來提高治療藥物的充分性的方法已經提出了一段時間，並且該方法仍然對藥物科學領域充滿熱情。

In vitro or ex vivo procedures are significant in the exhibition testing of mucoadhesive medication conveyance frameworks and are savvy in choosing proficient frameworks when contrasted and in vivo strategies. These techniques can assess mucoadhesive details, without utilizing creature models, and may offer robotic comprehension of mucoadhesion. Various strategies have been created to survey and comprehend the mucoadhesion of medication conveyance frameworks. The advancement of new strategies ought to be approved by correlation with a highest quality level in vitro method, or in vivo execution. New strategies to examine the mucoadhesive profile of semisolid polymer frameworks are commonly evolved in-house on bespoke hardware, and have not experienced approval, which stresses the significance of normalized methods. Besides, every measurements structure may require diverse trial conditions and examination may just be conceivable inside dose structure types. The separation power technique (otherwise called the ductile strategy) is the most broadly utilized technique to explore glue associations between a mucosal film (or other substrate) and a detailing. This strategy can be utilized for strong and semisolid measurement structures and it is realized that instrumental boundaries and analysis configuration impact test results. Different strategies, for example, the rheological strategy, can bring about various reactions and translations relying upon the examination type utilized. In this way, it is imperative to comprehend the factors of the technique for mucoadhesion testing, taking into account that normalized strategies have been required.

Mucoadhesion is a mind boggling process and various speculations have been proposed to clarify the instruments in question. Those are wetting hypothesis, Diffusion hypothesis, Fracture hypothesis, The electronic hypothesis, The adsorption hypothesis. Mucoadhesive conveyance frameworks are being investigated for the confinement of the dynamic specialists to a specific area/site. Polymers have assumed a significant job in structuring such frameworks in order to build the habitation time of the dynamic specialist at the ideal area. Mucoadhesive polymers are water-solvent and water insoluble polymers. Mucoadhesive polymers that hold fast to the mucin-epithelial surface can be helpfully partitioned into three expansive classes:

1.Polymers that become clingy when set in water and owe their mucoadhesion to tenacity.

2. Polymers that follow through vague, non-covalent associations those are essentially electrostatic in nature

3. Polymers that quandary to explicit receptor site on tile self surface.

Every one of the three polymer types can be utilized for medicate conveyance.

在這項研究的背景下，解決了用各種聚合物建立的凝膠定義對各種黏膜組織的黏膜黏附特性。作為聚合物，使用了八種不同的聚合物； Kitosan M、Kitosan H、HPMC K15M、HPMC K100M、瓜爾膠 H、瓜爾膠 S、Carbopol® 974 P 和 Policarbophil® AA-1。利用九種不同的牛樣黏膜組織（陰道、鼻、頰、腸、結腸、胃、子宮和喉嚨）對所排列的凝膠進行黏膜黏附研究。 TA.XT。此外，質地分析儀也用於測量黏膜黏附凝膠定義與黏膜分離的能力以及黏膜黏附過程。此外，將脂質體作為微粒框架添加到凝膠細節中，以觀察鍵結如何受到影響。就整體結果而言，與其他聚合物相比，Kitosan H 和瓜爾膠 H 被認為具有最佳的黏膜黏附性能。