Oya KERİMOĞLU, Setenay ÖZER, Timuçin UĞURLU

Nanotaşıyıcılar: Oral İnsülin Tedavisine Yeni Yaklaşımlar

Dünya üzerinde en fazla üyeye sahip kronik hastalıklardan biri olan diyabet için, özellikle tip 1 diyabetli hastalarda, vücutta üretilen insülinin görevlerini tam olarak karşılayabilen tedavi yöntemi henüz bulunamamıştır. Peptid yapılı bir makromolekül olan insülin, farklı uygulama yollarıyla verildiğinde enzimatik bozunmaya uğraması veya yeterince emilememesi sebebiyle çoğunlukla subkutan olarak uygulanır. Ancak rutin olarak subkutan ilaç uygulamak hastalarda birtakım immünolojik problemlere, yağ dokusu bozulduğundan lipodistrofi şikayetlerine sebep olabilmektedir. Ayrıca doğal olarak üretilen insülinle farmakokinetik özellikleri tam olarak uyuşmadığından hiperinsülinemi görülebilmektedir. Son yıllarda yapılan klinik çalışmalara göre hatırı sayılır oranda diyabet hastası insulinin enjeksiyonla yapılan tedavisine uyunç sağlayamadığından uzun vadede glisemik kontrol de sağlanamamaktadır. Oral dozaj şekilleri ile ilaç tedavisi uyunç ve uygulama kolaylığı sebebiyle en fazla tercih edilen sistemler olduğundan, subkutan insülin tedavisinin zorluklarına alternatif olarak oral insülin uygulanmasının yolu açılmaya çalışılmış ve formülasyonun uygulanması için öne çıkan problemlere çözüm aranmaya başlanmıştır. Nanoteknoloji, pek çok alanda olduğu gibi ilaç teknolojisinde de dikkat çekmeye başlamıştır. Nanofarmasötik sistemler geleneksel ilaçlara göre absorpsiyonu ve etkin madde için koruyuculuğu yüksek, terapötik seviyeye ulaşmak için gerekli doz miktarını azaltan, biyoyararlanımı artıran, kontrollü salım ve hedeflendirme yapabilme avantajlarını sağlayan, ilacın etki süresini azaltan sistemlerdir. Tüm bu avantajlar düşünüldüğünde, insülinin oral yoldan verilebilmesi için nanofarmasötiklerin uygunluğu in vitro ve in vivo deneylerle araştırılmaktadır.

Anahtar Kelimeler:

Nano sistemler, insülin, oral uygulama, diyabet, biyoyararlanım, oral peptidler

Nanocarriers: Novel Approaches to Oral Delivery of Insulin

Diabetes is among the major chronic diseases at present, and no medication has been developed that can replace the roles of endogenous insulin, especially for type 1 diabetes patients. However, insulin can be frequently administered by the subcutaneous route as a protein macromolecule because enzymatic and absorption-associated problems. It leads to immunogenic symptoms, adipose tissue complaints such as lipodystrophy, and hyperinsulinemia risks because of pharmacokinetic properties that do exactly overlap with those of endogenous insulin. In a remarkable number of patients, failure to attain permanent glycemic control by subcutaneous insulin treatment has shown by clinical trials based on noncompliance. Oral drug administration has always been the most preferred administration pathway for drugs with high patient compliance and convenience. Difficulties in the use of subcutaneous insulin have prompted scientists to find solutions for the oral administration of insulin. Similar to many other fields, nanotechnology has recently come to the fore in the pharmaceutical field. Compared with conventional systems, nanopharmaceuticals are drug delivery systems that enable promoted absorption, protection of the active ingredient from the external environment, lower dose applications, higher bioavailability, controlled release, and prolonged residence time. In vitro and in vivo studies have been performed with varied nanopharmaceutical systems in order to administer insulin orally for this purpose.

Keywords:

Nanosystems, insulin, oral delivery, diabetes, bioavailability, oral peptides,

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