Koenzim Q10'un biyoyararlanımını arttırmak için proniozomal formülasyonların geliştirilmesi: İn vitro ve in vivo değerlendirilmeleri
Küçük Resim Yok
Tarih
2023
Yazarlar
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Trakya Üniversitesi
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
Koenzim Q10 vücudun ürettiği en önemli antioksidanlardan biridir. Ayrıca elektron taşıyıcı olarak da görev alır, genel olarak oral olmakla birlikte vücuda transdermal, oküler yollarla da uygulanmaktadır. Koenzim Q10, oksijen kaynaklı serbest radikaller ile etkileşerek biyomoleküllerin zarara uğramasını önlemektedir. Bundan dolayı vücutta güçlü bir antioksidan olarak görev alarak diğer antioksidanların yenilenmesinde, hücre sinyalinde, hücre büyümesinde ve gen ekspresyonunda görev alır, membran stabilitesinde, enerji dönüşümünde ve ATP üretiminde de önemli rol oynar. Koenzim Q10 düşük çözünürlük ve düşük biyoyararlanımı gösterdiğinden kullanımı sınırlanmaktadır. Yaptığımız tez çalışması kapsamında proniozomlardan elde edilen niozomal formülasyonları üzerinde karakterizasyon çalışmaları yapılmış ve belirlenen formüller in vivo farmakokinetik çalışmalara tabi tutulmuştur. Saf koenzim Q10 ve koenzimQ10 yüklü proniozomlar uygulandıktan sonra sıçanlardan 24 saat boyunca belli saatlerde kan örnekleri alınıp gerekli ölçümler yapılmıştır. Farmakokinetik parametreler incelendiğinde görüleceği üzere proniozom formülasyonu saf etkin maddeye göre etkili bir biyoyararlanım göstermiştir. Miktar tayinleri yapılırken ICH referans alınarak HPLC'de analitik metot yöntemi geliştirilmiş ve bu yöntemin validasyonu yapılmıştır. Yapılan bu çalışmada koenzim Q10 proniozomlara yüklenmiş, in vitro ve in vivo deneyler sonucunda etkin maddenin biyoyararlanımının arttığı gözlemlenmiştir. Sonuç olarak proniozom formülasyonlarının biyoyararlanımı arttırmada etkili bir taşıyıcı olduğu çalışmamızda gösterilmiştir. Anahtar kelimeler: Bulamaç yöntemi, koenzim Q10, proniozom, biyoyararlanım, farmakokinetik.
Coenzyme Q10 is one of the most important antioxidants produced by the body. It also functions as an electron carrier and is generally administered orally, but can also be applied to the body transdermally, orally, and ocularly. Coenzyme Q10 interacts with oxygen-derived free radicals to prevent damage to biomolecules. Therefore, it serves as a potent antioxidant in the body, contributing to the renewal of other antioxidants, cell signaling, cell growth, and gene expression. Additionally, it plays a significant role in membrane stability, energy conversion, and ATP production. Due to its low solubility and low bioavailability, the use of coenzyme Q10 is limited. As part of our thesis work, characterization studies were conducted on niosomal formulations obtained from proniosomes, and the identified formulas were subjected to in vivo pharmacokinetic studies. After the application of pure coenzyme Q10 and coenzyme Q10 -loaded proniosomes, blood samples were collected from rats at specified intervals over 24 hours, and the necessary measurements were performed. When pharmacokinetic parameters were examined, it was observed that the proniosome formulation exhibited effective bioavailability compared to the pure active substance. Quantitative determinations were carried out by developing an analytical method using the ICH reference in HPLC, and the validation of this method was performed. In this study, coenzyme Q10 was loaded into proniosomes, and because of in vitro and in vivo experiments, it was observed that the bioavailability of the active substance increased. In conclusion, our study has demonstrated that proniosome formulations are effective carriers in increasing bioavailability. Keywords: Slurry method, coenzyme Q10, proniosome, bioavailability, pharmacokinetics.
Coenzyme Q10 is one of the most important antioxidants produced by the body. It also functions as an electron carrier and is generally administered orally, but can also be applied to the body transdermally, orally, and ocularly. Coenzyme Q10 interacts with oxygen-derived free radicals to prevent damage to biomolecules. Therefore, it serves as a potent antioxidant in the body, contributing to the renewal of other antioxidants, cell signaling, cell growth, and gene expression. Additionally, it plays a significant role in membrane stability, energy conversion, and ATP production. Due to its low solubility and low bioavailability, the use of coenzyme Q10 is limited. As part of our thesis work, characterization studies were conducted on niosomal formulations obtained from proniosomes, and the identified formulas were subjected to in vivo pharmacokinetic studies. After the application of pure coenzyme Q10 and coenzyme Q10 -loaded proniosomes, blood samples were collected from rats at specified intervals over 24 hours, and the necessary measurements were performed. When pharmacokinetic parameters were examined, it was observed that the proniosome formulation exhibited effective bioavailability compared to the pure active substance. Quantitative determinations were carried out by developing an analytical method using the ICH reference in HPLC, and the validation of this method was performed. In this study, coenzyme Q10 was loaded into proniosomes, and because of in vitro and in vivo experiments, it was observed that the bioavailability of the active substance increased. In conclusion, our study has demonstrated that proniosome formulations are effective carriers in increasing bioavailability. Keywords: Slurry method, coenzyme Q10, proniosome, bioavailability, pharmacokinetics.
Açıklama
Yüksek Lisans
Anahtar Kelimeler
Eczacılık ve Farmakoloji, Pharmacy and Pharmacology
