Deriye İlaç Uygulanması için Transetozomların Formülasyonu ve İn vitro Karakterizasyonu

Year 2019, , 51 - 59, 06.09.2019

Aslı Gürbüz Sevgi Güngör Meryem Sedef Erdal

https://doi.org/10.26650/JARHS2019-616323

Abstract

Deriye ilaç taşınmasını modifiye eden topikal taşıyıcılara olan ilgi son dönemlerde oldukça artmıştır. Etken maddelerin penetrasyonunda, derinin en dış tabakası olan stratum corneum önemli bir bariyer oluşturmaktadır. Bu bariyeri aşmaya yönelik birçok formülasyon yaklaşımı denenmiştir. Bu yaklaşımlar arasında veziküler taşıyıcılar olan lipozom, etozom, transferzom ve son dönemlerde transetozomların kullanılması ile özellikle lipofilik etken maddelerin derideki lokalizasyonunun iyileştirilmesi hedeflenmektedir. Fosfolipit, yüzey etken madde ve yüksek oranda etanol içeren transetozomlar, transferzom ve etozomların avantajlarını kombine eden sistemlerdir. Bu çalışmada, model lipofilik etken madde olarak fluvastatin ile yüklenmiş transetozomlar geliştirilmiş ve karakterize edilmiştir. Fluvastatinin domuz derisine in vitro penetrasyonu oklüzif olan ve oklüzif olmayan koşullar altında çalışılarak bantla soyma yöntemi ile kantitatif tayin gerçekleştirilmiştir. Transetozomların deri ile etkileşimi ATR-FTIR spektroskopisi kullanılarak araştırılmıştır. Sonuç olarak, oklüzif olmayan koşullarda uygulandığında derideki etken madde lokalizasyonunu iyileştiren bir transetozom formülasyonu hazırlanmıştır. 

Keywords

Transetozom, veziküler ilaç taşıyıcı sistem, fluvastatin, deriye ilaç uygulanması

Formulation and in vitro Characterization of Transethosomes for Dermal Drug Delivery

Abstract

There has been increased interest during recent years in the use of topical vehicles that may modify drug penetration into the skin. However, the complex structure of the skin and especially its uppermost layer, the stratum corneum, function as a rate limiting barrier for topical drug delivery. Various strategies have been employed to achieve the delivery of drugs into the skin. Among these strategies, vesicular carriers such as liposomes, ethosomes, transfersomes, and, more recently, transethosomes have been suggested to serve as efficient promoters of drug localization within the skin. Transethosomes contain phospholipids, surfactants, and a high percentage of ethanol. They have shown to enhance the skin penetration of lipophilic drugs. In this study, transethosomes have been developed, characterized, and loaded with a model lipophilic drug, fluvastatine. The in vitro pig skin penetration of fluvastatine from transethosome dispersion under occlusive and non-occlusive conditions have been determined quantitatively by using the tape stripping method. An ATR-FTIR spectroscopy has been used to study the interaction of transethosomes with the skin lipids. As a result, a topical transethosomal carrier which optimizes drug localization within the skin when applied under non-occlusive conditions has been developed. 

Keywords

Transethosome, vesicular drug carrier system, fluvastatin, drug delivery to skin

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