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Dış Akustik Meatus (EAM) Platformu ile Nanoboyutlu Duloksetinin Taşınmasına Yönelik Yenilikçi Bir Yaklaşım

Amaç: Depresyon yaygın fakat ciddi bir duygudurum bozukluğu. Tedavi maliyeti çok yüksektir. Dış kulak yolu, bir tedavi platformu olarak kullanılır ve oral tedaviye bağlı aşırı doz probleminde işe yarar. Mevcut araştırmaların amacı, depresyon üzerinde daha iyi kontrol olanağı sağlayan bir model ilaç olarak duloksetin nano süspansiyonunu kulak yoluyla beyne yönlendiren yeni bir rota keşfetmektir. Gereç ve Yöntemler: Bu düşünce, nöro-boyutlu bir API, yani duloksetin formülasyonu hazırlayarak kanıtlandı ve sonikasyon banyosu yöntemi ile farmakolojik etkilerini gözlemledi. Biyo-nano süspansiyonu, Piper nigrum'un meyvelerinden izole edilen bir biyopolimer kullanılarak hazırlandı. Sekiz formülasyon, 1: 0.5, 1: 1, 1: 2, 1: 3, 1: 4, 1: 5, 1: 7 ve 1:10 gibi hazırlandı. Bulgular: Formülasyonlar, pH, % iletim, İçerik homojenliği, ex-vivo stabilitesi, 36 saatten fazla salınım gibi çeşitli değerlendirmelere tabi tutuldu. Duloksetinin, F1 (1: 0.5) 'in 0.9905 tT80: 22 saatlik r2 değerine sahip en iyi formülasyon olduğu bulunmuş ve en uygun modelin Higuchi matrisi olduğu bulunmuş ve ulaşım mekanizmasının bits yazılımı ile anormal transport olduğu hesaplandı. Sonuç: Elde edilen in-vitro sonuçlara dayanarak, önemli miktarda ilacın dış kulak kanalı yoluyla beyne ulaştığı ve dolayısıyla bu yeni yolla Duloksetin'in verilmesi uygun olduğu sonucuna varılabilir.

An Innovative Approach for Delivery of Nanosized Duloxetine Via External Acoustic Meatus (EAM) Platform

Objective: Depression is a common but serious mood disorder. The treatment cost is very high. The external auditory canal is used as a delivery platform and has overcome the dose dumping problem in the case of oral system. The current research work was to explore a novelistic route for targeting to the brain through ear by formulating nanosuspension using duloxetine as a model drug permitting better control over depression. Method: The concept was proved by preparing a nano-sized formulation of API i.e duloxetine and observed its pharmacological actions by sonication bath method. Bio-nano suspension was prepared by using a biopolymer which was isolated from berries of Piper nigrum. Eight formulations were prepared viz 1:0.5, 1:1, 1:2, 1:3, 1:4, 1:5, 1:7, and 1:10. Results: The formulations were subjected to various evaluations, including pH, % transmittance, content uniformity, ex-vivo stability, release for over 36 hours. Different formulations of duloxetine out of which F1 (1:0.5) was found to be the best formulation having the r2 value of 0.9905 tT80: 22 hrs and the best fit model was found to be Higuchi matrix, and mechanism of transport was anomalous transport which was calculated by bits software. Conclusion: On the basis of the in-vitro results obtained it can be concluded that significant amount of drug reaches the brain via external acoustic meatus and so it is feasible to deliver Duloxetine by this novelistic route.

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