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Development and Characterization of Nano-Sized Emulsion Systems Incorporated Polyphenolic Compound for Application Through the Skin

Year 2022, Volume: 1 Issue: 47, 57 - 72, 01.03.2022
https://doi.org/10.55262/fabadeczacilik.1078888

Abstract

In addition to having strong anti-oxidant properties, resveratrol has anti-cancer, anti-angiogenic, cardioprotective, anti-diabetic, antiviral, and neuroprotective activities. Despite its rapid absorption, first-pass effect and intestinal metabolism reduce the bioavailability of resveratrol. Moreover, the lipophilic property of resveratrol reduces its water solubility and metabolized in high incidence reduces its oral bioavailability. Therefore, it was aimed to develop an optimum formulation for the skin application of resveratrol to overcome the
negatives after oral administration.Since their easy formulation, thermodynamically stable properties, and facilitating the delivery of both lipophilic and hydrophilic active ingredients, loading resveratrol to microemulsions (MEs) will be a suitable delivery system to overcome the drawback of stability problems and skin bioavailability of resveratrol. A Triangle phase diagram was constructed, and the MEs region was determined by points studies. Subsequently, some formulations were selected within the transparent region by
considering characteristics required to achieve optimized transdermal drug delivery. Chosen formulations were exposed to pre-stability tests such as centrifuge and thermal stress tests. Characterization studies such as droplet size, size distribution, zeta potential, viscosity, pH measurement were performed on remained intact formulations after pre-stability tests. In terms of the characterization test results such as pH, viscosity, conductivity, there wasn’t found significant difference observed between formulations. However, polydispersity index and zeta potential values provided to choosing optimal formulation.

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Deriden Uygulama İçin Polifenolik Bileşik İçeren Nano Boyutlu Emülsiyon Sistemlerinin Geliştirilmesi ve Karakterizasyonu

Year 2022, Volume: 1 Issue: 47, 57 - 72, 01.03.2022
https://doi.org/10.55262/fabadeczacilik.1078888

Abstract

Resveratrol güçlü bir antioksidan özelliğe sahip olmasının yanı sıra antikanser, anti-anjiyojenik, kardiyoprotektif, anti-diyabetik, anti-viral ve nöroprotektif aktivitelere sahiptir. İnsan vücudunda hızlı emilime uğramasına rağmen, bağırsak ve karaciğer metabolizması, resveratrolün sistemik biyoyararlanımı için hız sınırlayıcıdırlar. Ayrıca, resveratrolün yüksek lipofilikliği, suda çözünürlüğünü ve oral yoldan yüksek oranda metabolize edilmesi nedeni ile oral biyoyararlanımını azaltır. Bu nedenle, oral uygulama ile görülen olumsuzlukların üstesinden gelmek için resveratrolün deri uygulaması için optimum bir formülasyon geliştirilmesi amaçlanmıştır.Kolay formüle edilebilmeleri, termodinamik olarak kararlı
olmaları ve hem lipofilik hem de hidrofilik etkin maddelerin vücuda verilmesini kolaylaştırmalarından dolayı, resveratrolün mikroemülsiyonlara (ME’ler) yüklenmesi, stabilite sorunları ve deriden emiliminin zor olması gibi dezavantajlarının üstesinden gelmek için uygun bir ilaç taşıyıcı sistemi olacaktır.Bu çalışmada önce üçgen faz diyagramı oluşturularak MEs bölgesi noktasal çalışma ile belirlendi. Daha sonra optimize edilmiş formülasyonu elde etmek için gerekli özellikler göz önünde bulundurularak ME sistemleri oluşturan bölge içinde bazı formülasyonları seçildi. Seçilen formülasyonlar, santrifüj ve termal stres testleri gibi ön stabilite testlerine tabi tutuldu. Damlacık boyutu, damlacık boyut dağılımı, zeta potansiyeli, viskozite, pH ölçümü gibi karakterizasyon çalışmaları, ön stabilite testlerinden sonra fiziksel olarak bozulmadan kalan formülasyonlar üzerinde gerçekleştirildi. Viskozite, pH, iletkenlik gibi karakterizasyon testleri sonuçları açısından formülasyonlar transdermal uygulamalar için kabul edilebilir aralıktaydı. Ancak damlacık boyutu, polidispersite indeksi ve zeta potansiyel değerleri optimal formülasyonun belirlenmesini sağlamıştır.

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There are 80 citations in total.

Details

Primary Language English
Subjects Pharmacology and Pharmaceutical Sciences
Journal Section Research Articles
Authors

Bülent Samancı

Fatma Gülgün Yener This is me

İsmail Tuncer Değim This is me

Publication Date March 1, 2022
Submission Date July 27, 2021
Published in Issue Year 2022 Volume: 1 Issue: 47

Cite

APA Samancı, B., Gülgün Yener, F., & Değim, İ. T. (2022). Development and Characterization of Nano-Sized Emulsion Systems Incorporated Polyphenolic Compound for Application Through the Skin. Fabad Journal of Pharmaceutical Sciences, 1(47), 57-72. https://doi.org/10.55262/fabadeczacilik.1078888