Targeted delivery of anti-inflammatory drugs in lower parts of gastrointestinal tract: Conventional and novel approaches

Abstract

The therapy of inflammatory bowel diseases can be improved by development of new effective and selective biological drugs and efficiency improvement of existing, traditional anti-inflammatory drugs via targeting sites of inflammation. Targeted drug delivery upon peroral administration results in improved therapeutic efficacy, reduction of systemic side effects, decreases risk of drug to drug interactions, and in case of prolonged-release systems improves compliance/adherence by reduced frequency of drug intake. This article describes two approaches for targeted delivery of anti-inflammatory drugs in lower parts of gastrointestinal tract: conventional, based on specific physiological conditions of different parts of gastrointestinal tract (pH, enzymatic activity of intestinal flora and transit time) and novel, based on micro- and nanoencapsulation (e.g. polymeric and lipid micro- and nanoparticles, liposomes), with focus on the anti-inflammatory drugs intended for targeted delivery in lower parts of gastrointestinal tract available on market of Republic of Serbia.

Poboljšanje efikasnosti terapije inflamatornih bolesti creva postiže se razvojem novih, efikasnih i selektivnih bioloških lekova, ali i unapređenjem efikasnosti postojećih, tradicionalnih antiinflamatornih lekova, putem ciljane isporuke na mesto inflamacije. Ciljanom isporukom na mesto inflamacije nakon peroralne primene postiže se veća terapijska efikasnost, smanjuju sistemski neželjeni efekti leka i rizik od interakcije sa drugim lekovima, a kod sistema sa produženim oslobađanjem poboljšava i komplijansa/adherenca usled smanjenja učestalosti doziranja. U ovom radu su opisane dve grupe pristupa za postizanje ciljane isporuke antiinflamatornih lekova u donje delove gastrointestinalnog trakta: konvencionalni, zasnovani na fiziološkim specifičnostima različitih delova gastrointestinalnog trakta (pH vrednost, enzimska aktivnost crevne flore i tranzitno vreme, odnosno njihova kombinacija) i savremeni, koji se zasnivaju na inkapsulaciji lekovitih supstanci u mikro- i nanonosače (npr. polimerne i lipidne mikro- i nanočestice i liposome), sa posebnim osvrtom na antiinflamatorne lekove za ciljanu isporuku u donje delove gastrointestinalnog trakta prisutne na tržištu Republike Srbije.