İntestinal Absorpsiyonu Artırmak Amacıyla Kullanılan Permeasyon Artırıcı Ajanlar

Abstract

Sistemik etki elde etmek amacıyla ilaçlar farklı yollarla uygulanmaktadır. Bu uygulama yolları arasında en yaygın olarak kullanılanı oral yoldur. Oral yolla verilen bir ilaç etki edeceği bölgeye ulaşana kadar çeşitli biyolojik membranlardan geçmek zorundadır. Bu membranların en önemlilerinden biri de barsak epitelidir. Barsak epitelinden absorpsiyon başlıca iki mekanizma ile gerçekleşmektedir. Bunlar epitel hücre membranlarından absorpsiyon transselüler yol ve epitel hücreler arasındaki sıkı kavşaklar tight junction ’dan absorpsiyondur. Moleküllerin hücreler arasındaki sıkı kavşaklardan geçmesi paraselüler interselüler transport olarak adlandırılmaktadır. Paraselüler permeabilitenin düzenlenerek ilaç absorpsiyonunu artırmak için en etkili yol sıkı kavşakların yapısal olarak düzenlenmesidir. Polimer ve yüzey etkin özellikteki bazı maddelerin membranlardan paraselüler yolla geçen ilaçların absorpsiyonunu çeşitli mekanizmalarla artırdığı belitilmiştir. Bu maddeler permeasyon artırıcılar olarak da bilinmektedir. Bu derlemede, permeasyon artırıcıların fizikokimyasal özellikleri ve intestinal absorpsiyonu artırma mekanizmalarından bahsedilmektedir. Ayrıca permeasyon artırıcılara çeşitli örnekler verilerek, ve bu maddelerle yapılmış çalışmalar değerlendirilmiştir.

Keywords

• Permeasyon artırıcılar,Paraselüler absorpsiyon,Permeabilite

Permeability enhancers used to increase intestinal absorption

Abstract

Drugs are administered through various routes to obtain systemic effect. Of these, the most commonly used route of administration is the oral route. Following oral administration, the drug has to pass through several biological membranes until it reaches the site of effect. The most important one among these membranes is the intestinal epithelium. Absorption through the intestinal epithelium occurs mainly by two mechanisms. These mechanisms are absorption through the epithelial cell membranes transcellular route and absorption through the tight junctions between epithelial cells. Transport of molecules through the tight junctions is called as paracellular intercellular transport. The most effective way to improve drug absorption by regulating paracellular permeability is the structural organization of tight junctions. It is reported that some substances such as polymers, surfactants increase the absorption of paracellulary transported drugs across membranes by means of various mechanisms. These substances are also known as permeation enhancers. In this review, physicochemical peroperties of permeability enhancers and their mechanism of effect to increase intestinal absorption were discussed. Also various examples were given for these permeability enhancers and the studies counducted using these substances were evaluated.

Keywords

• Permeation enhancers,Paracellular absorption,Permeability

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