A Comparative Study of Passive and Active Tumor Targeting Using Nanoparticles as Drug Delivery Systems

Year 2018, Volume: 6 Issue: 1, 1 - 7, 31.01.2018

Cenk Dağlıoğlu

https://doi.org/10.21541/apjes.349889

Cited By: 1

Abstract

Nanoparticle-mediated drug targeting is an active
area of cancer research and hold enormous potential in improving anticancer
efficacy by providing tumor tissue specificity.
Herein, tumor targeting capabilities of nanoparticles between passive targeting
approach via the enhanced
permeability and retention (EPR) effect and active
targeting approach via the biotin receptors were compared to determine
targeting efficiency rates. For this reason, Fe₃O₄@SiO₂(FITC)-DOX
(for passive targeting) and Fe₃O₄@SiO₂(FITC)-BTN/DOX
(for active targeting) multifunctional nanoparticles combining imaging and therapy were used. Fluorescence microscopy and
flow cytometry were employed to both visualize and quantify the accumulation of
nanoparticles into the tumor cells. The results demonstrated that active
targeting strategy considerably enhanced nanoparticle accumulation in the cervical carcinoma HeLa cells with
a 2-fold increase in comparison to passive targeting. Targeted nanoparticles
exhibited higher cytotoxicity in cancer cells with an approximately 2.5-fold
better half maximal inhibitory concentration (IC₅₀) value than
untargeted nanoparticles. Moreover, it was found that targeted nanoparticles increased
the number of apoptotic cells by nearly 21.1% as compared to untargeted
nanoparticles. These observations show that active tumor targeting drug
delivery systems could be more promising for enhancing the chemotherapeutic
effects of anticancer drugs as compared to passive tumor targeting drug
delivery systems.

Keywords

Cancer, multifunctional nanoparticles, passive targeting, active targeting

İlaç Taşıma Sistemleri olarak Nanopartiküller kullanılarak Pasif ve Aktif Tümör Hedeflemelerinin Karşılaştırmalı İncelenmesi

Abstract

Nanopartikül-aracılı ilaç
hedefleme kanser araştırmalarının aktif bir alanı olup, tümör dokusuna özgün
antikanser etkinliği artırmada çok önemli bir potansiyele sahiptir. Bu
çalışmada, hedefleme verimlilik oranlarının belirlenmesi için pasif ve aktif
hedefli nanopartiküllerin tümör hedefleme kabiliyetleri, sırasıyla artmış
geçirgenlik ve alıkonma (EPR) etkisi ve biyotin reseptörlerini hedefleme
yaklaşımları karşılaştırılarak incelendi. Bunun için, görüntüleme ve tedavi
edici özellikleri bir arada barından Fe₃O₄@SiO₂(FITC)-DOX (pasif
hedefleme için) ve Fe₃O₄@SiO₂(FITC)-BTN/DOX
(aktif hedefleme için) multifonksiyonel nanopartikülleri kullanıldı. Nanopartiküllerin
tümör hücrelerindeki birikiminin izlenmesi ve miktarsal ölçümü için floresan
mikroskopu ve akım sitometresi kullanıldı. Elde edilen sonuçlar, pasif
hedeflemeyle karşılaştırıldığında aktif hedefleme stratejisinin servikal
karsinoma HeLa hücrelerindeki nanopartikül birikimini 2 kat gibi önemli bir ölçüde
artırdığını gösterdi. Aktif hedefli nanopartiküller, pasif hedefli nanopartikülerden
yaklaşık 2.5 kat daha düşük yarı-maksimum inhibisyon konsantrasyonu (IC₅₀)
değeri ile kanser hücrelerinde daha yüksek sitotoksisite sergiledi. Ayrıca, pasif hedefli
nanopartiküllerle karşılaştırıldığında, aktif hedefli nanopartiküllerin apoptotik
hücre sayısını yaklaşık % 21.1 oranında artırdığı bulundu. Bu gözlemler, aktif tümör
hedefli ilaç taşıma sistemlerinin, pasif tümör hedefli ilaç taşıma sistemleri
ile karşılaştırıldığında, antikanser ilaçların kemoterapötik etkilerini artırmada
daha umut verici olduğunu göstermektedir.

Keywords

Kanser, multifonksiyonel nanopartiküller, pasif hedefleme, aktif hedefleme

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