LIQUID AND SOLID SELF-EMULSIFYING DRUG DELIVERY SYSTEMS (SEDDS) CONTAINING VALSARTAN: STABILITY ASSESSMENT AND PERMEABILITY STUDIES

Gülbeyaz Yıldız Türkyılmaz; Mine Diril; Eda Gülmezoğlu; Yesim Karasulu

Article Details

LIQUID AND SOLID SELF-EMULSIFYING DRUG DELIVERY SYSTEMS (SEDDS) CONTAINING VALSARTAN: STABILITY ASSESSMENT AND PERMEABILITY STUDIES

Authors:

Gülbeyaz Yıldız Türkyılmaz | Mine Diril | Eda Gülmezoğlu | Yesim Karasulu

Publisher:

Ankara University

Main Topics:

İlaç Dağıtım Teknolojileri

Journal:

Ankara Üniversitesi Eczacılık Fakültesi Dergisi Vol.48 Issue 2, pp.525-534

Document Type:

Article

Publication Date:

5/2024

Document Language:

English

Document ID (Org No.):

2001311401

pISSN:

1015-3918

Keywords:

Abstract:

 Objective: Valsartan VST is a Biopharmaceutical classification system BSC class II active ingredient with a bioavailability of approximately 25 and is utilized to treat high blood pressure hypertension. This study aimed was to showcase the stability and increase the permeability of VST by developing self-emulsifying drug delivery systems SEDDS and solidified SEDDS S-SEDDS formulations. Material and Method: The ratios of the components were determined by the pseudo-ternary phase diagram, and the characterization studies were conducted in the previous study. Stability was performed in long-term 252C, 605 relative humidity and accelerated 402C, 755 relative humidity conditions. The intestinal permeability of SEDDS formulations was evaluated by Caco-2 cells. Result and Discussion: Formulations for 12 month, droplet sizes were found to be 67.52  5.26 nm and 176.93  17.34 nm for SEDDS of VST VST-SEDDS and S-SEDDS of VST VST-S-SEDDS, respectively. During this period, polydispersity indexes were: VST-SEDDS, 0.560.1; VST-S-SEDDS, 0.580.05. Both formulations increased VST permeability across Caco-2 cells: VST-SEDDS by 2.32x powder and 2.18x commercial; VST-S-SEDDS by 1.38x powder and 1.30x commercial. The formulation components did not have cytotoxic effects. These results demonstrated that newly developed VST-SEDDS and VST-S-SEDDS formulations with high permeability may be a desirable approach for antihypertensive therapy.

 Objective: Valsartan VST is a Biopharmaceutical classification system BSC class II active ingredient with a bioavailability of approximately 25 and is utilized to treat high blood pressure hypertension. This study aimed was to showcase the stability and increase the permeability of VST by developing self-emulsifying drug delivery systems SEDDS and solidified SEDDS S-SEDDS formulations. Material and Method: The ratios of the components were determined by the pseudo-ternary phase diagram, and the characterization studies were conducted in the previous study. Stability was performed in long-term 252C, 605 relative humidity and accelerated 402C, 755 relative humidity conditions. The intestinal permeability of SEDDS formulations was evaluated by Caco-2 cells. Result and Discussion: Formulations for 12 month, droplet sizes were found to be 67.52  5.26 nm and 176.93  17.34 nm for SEDDS of VST VST-SEDDS and S-SEDDS of VST VST-S-SEDDS, respectively. During this period, polydispersity indexes were: VST-SEDDS, 0.560.1; VST-S-SEDDS, 0.580.05. Both formulations increased VST permeability across Caco-2 cells: VST-SEDDS by 2.32x powder and 2.18x commercial; VST-S-SEDDS by 1.38x powder and 1.30x commercial. The formulation components did not have cytotoxic effects. These results demonstrated that newly developed VST-SEDDS and VST-S-SEDDS formulations with high permeability may be a desirable approach for antihypertensive therapy.

 Objective: Valsartan VST is a Biopharmaceutical classification system BSC class II active ingredient with a bioavailability of approximately 25 and is utilized to treat high blood pressure hypertension. This study aimed was to showcase the stability and increase the permeability of VST by developing self-emulsifying drug delivery systems SEDDS and solidified SEDDS S-SEDDS formulations. Material and Method: The ratios of the components were determined by the pseudo-ternary phase diagram, and the characterization studies were conducted in the previous study. Stability was performed in long-term 252C, 605 relative humidity and accelerated 402C, 755 relative humidity conditions. The intestinal permeability of SEDDS formulations was evaluated by Caco-2 cells. Result and Discussion: Formulations for 12 month, droplet sizes were found to be 67.52  5.26 nm and 176.93  17.34 nm for SEDDS of VST VST-SEDDS and S-SEDDS of VST VST-S-SEDDS, respectively. During this period, polydispersity indexes were: VST-SEDDS, 0.560.1; VST-S-SEDDS, 0.580.05. Both formulations increased VST permeability across Caco-2 cells: VST-SEDDS by 2.32x powder and 2.18x commercial; VST-S-SEDDS by 1.38x powder and 1.30x commercial. The formulation components did not have cytotoxic effects. These results demonstrated that newly developed VST-SEDDS and VST-S-SEDDS formulations with high permeability may be a desirable approach for antihypertensive therapy.

 Amaç: Valsartan VST, biyoyararlanımı yaklaşık 25 olan Biyofarmasötik Sınıflandırma Sistemi BSS sınıf II aktif maddedir ve yüksek kan basıncını hipertansiyon tedavi etmek için kullanılır. Bu çalışmanın amacı, kendi kendine emülsifiye olan ilaç dağıtım sistemleri SEDDS ve katılaştırılmış SEDDS S-SEDDS formülasyonları geliştirerek VSTnin stabilitesini göstermek ve geçirgenliğini artırmaktır. Gereç ve Yöntem: Bir önceki çalışmada bileşenlerin oranları üçgen faz diyagramı ile belirlenmiş olup, karakterizasyon çalışmaları yapılmıştır. Bu çalışmada, uzun süreli 252C, 605 bağıl nem ve hızlandırılmış 402C, 755 bağıl nem koşullarda stabilite çalışmaları gerçekleştirildi. SEDDS formülasyonlarının bağırsak geçirgenliği Caco-2 hücreleri tarafından değerlendirildi. Sonuç ve Tartışma: Formülasyonların 12 ay boyunca partikül boyutları VST içeren SEDDS VST-SEDDS formülasyuonunda 67.52  5.26 nm, VST içeren S-SEDDS VST-S-SEDDS formülasyonunda 176.93  17.34 nm olarak bulundu. Bu süre boyunca VST-SEDDS ve VST-S-SEDDS formülasyonunun polidispersite indeksleri sırasıyla 0.560.1, 0.580.05 olarak bulundu. Her iki formülasyon da Caco-2 hücreleri boyunca VST geçirgenliğini artırdı: VST-SEDDS 2,32 kat toz ve 2,18 kat ticari; VST-S-SEDDS 1,38x toz ve 1,30x ticari. Formülasyonların bileşenlerinde sitotoksik etki görülmedi. Bu sonuçlar, yüksek geçirgenliğe sahip yeni geliştirilen VST-SEDDS ve VST-S-SEDDS formülasyonlarının antihipertansif tedavi için arzu edilen bir yaklaşım olabileceğini gösterdi.

Article Details

LIQUID AND SOLID SELF-EMULSIFYING DRUG DELIVERY SYSTEMS (SEDDS) CONTAINING VALSARTAN: STABILITY ASSESSMENT AND PERMEABILITY STUDIES

Authors:

Gülbeyaz Yıldız Türkyılmaz | Mine Diril | Eda Gülmezoğlu | Yesim Karasulu

Publisher:

Ankara University

Main Topics:

İlaç Dağıtım Teknolojileri

Journal:

Ankara Üniversitesi Eczacılık Fakültesi Dergisi Vol.48 Issue 2, pp.525-534

Document Type:

Article

Publication Date:

5/2024

Document Language:

English

Document ID (Org No.):

2001311401

pISSN:

1015-3918

Caco-2 cell line

permeability

self-emulsifying drug delivery system

solidified self-emulsifying drug delivery system

valsartanCaco-2 hücre hattı

kendi kendine emülsifiye olan ilaç dağıtım sistemleri

katılaştırılmış kendi kendine emülsifiye olan ilaç dağıtım sistemleri

permeabilite

valsartan

Issues

Article Details

Authors: Gülbeyaz Yıldız Türkyılmaz | Mine Diril | Eda Gülmezoğlu | Yesim Karasulu

Publisher: Ankara University

Main Topics: İlaç Dağıtım Teknolojileri

Journal: Ankara Üniversitesi Eczacılık Fakültesi Dergisi Vol.48 Issue 2, pp.525-534

Document Type: Article

Publication Date: 5/2024

Document Language: English

Document ID (Org No.): 2001311401

pISSN: 1015-3918

Issues

Authors:

Gülbeyaz Yıldız Türkyılmaz | Mine Diril | Eda Gülmezoğlu | Yesim Karasulu

Publisher:

Ankara University

Main Topics:

İlaç Dağıtım Teknolojileri

Journal:

Ankara Üniversitesi Eczacılık Fakültesi Dergisi Vol.48 Issue 2, pp.525-534

Document Type:

Article

Publication Date:

5/2024

Document Language:

English

Document ID (Org No.):

2001311401

pISSN:

1015-3918