Biyouyumlu Polimerik Kürelerden 5-Fluorourasilin Kontrollü Salımı

Primidin analoğu olan 5-Fluorourasil (5-FU) çok çeşitli kanserlerin (meme, kolorektal, gastrointestinal vb.) tedavisinde kullanılan bir kemoterapi ajanıdır. Ancak, plazma yarı ömrünün kısa olması, kanser hücrelerine karşı düşük seçiciliği ve ciddi yan etkilere sebep olması klinik kullanımını sınırlandırmıştır. Bu çalışmada 5-FU’nun kontrollü salım teknolojisi ile olumsuz özelliklerinin en aza indirilmesi hedeflendi. Bu amaçla 5-FU yüklü poli (vinil alkol)/sodyum aljinat (PVA/NaAlg) küreleri FeCl3 kullanılarak iyonik çapraz bağlanma yöntemiyle hazırlandı ve Fourier transform infrared spektroskopi (FTIR), taramalı elektron mikroskopi (SEM) ve diferansiyel taramalı kalorimetri (DSC) ile karakterize edildi. İn vitro salım çalışmaları 2’şer saat süre ile 3 farklı pH (1.2, 6.8 ve 7.4) değerinde toplam 6 saat olacak şekilde gerçekleştirildi. PVA/NaAlg (m/m) oranı, ilaç/polimer (m/m) oranı, çapraz bağlama süresi ve çapraz bağlayıcı derişiminin 5-FU salımı üzerine etkisi araştırıldı. Kürelerde PVA miktarının artmasıyla 5-FU salımının arttığı buna karşın çapraz bağlama süresinin ve çapraz bağlayıcı derişimin artmasıyla 5-FU salımının azaldığı belirlendi.

Controlled Release of 5-Fluorouracil from Biocompatible Polymeric Beads

5-Fluorouracil (5-FU), a pyrimidine analog, is a chemotherapy agent used in the treatment of a wide variety of cancers (breast, colorectal, gastrointestinal, etc.). However, its short plasma half-life, low selectivity against cancer cells and serious side effects limited its clinical use. In this study, it was aimed to minimize the negative properties of 5-FU with controlled release technology. For this purpose, 5-FU loaded poly(vinyl alcohol)/sodium alginate (PVA/NaAlg) beads were prepared by ionic crosslinking method using FeCl3 and beads were characterized by Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM) and differential scanning calorimetry (DSC). In vitro release studies were carried out for 2 hours at 3 different pH values (1.2, 6.8 and 7.4) for a total of 6 hours. The effects of PVA/NaAlg (w/w) ratio, drug/polymer (w/w) ratio, crosslinking time and crosslinker concentration on 5-FU release were investigated. It was determined that 5-FU release increased with increasing PVA amount in the beads, whereas 5-FU release decreased with increasing crosslinking time and crosslinker concentration.

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