Replacement of Extrusion by Temperature-Controlled Ultrasonication in Emulsome Production

Year 2021, Issue: 28, 584 - 589, 30.11.2021

Mehmet Hikmet Üçışık

https://doi.org/10.31590/ejosat.1009437

Abstract

Emulsomes are lipid-based drug delivery systems comprising of a solid fat core surrounded by phospholipid multi-layers. Stability, prolonged release profile, biocompatibility and high encapsulation capacity for lipophilic compounds are their most prominent features. This study investigates the suitability of a temperature-controlled ultrasonication procedure to replace extrusion step that is widely applied for production and homogenization of emulsomes. In this study, emulsomes homogenized through ultrasonication were evaluated based on physicochemical properties including size, morphology and zeta potential. Temperature-controlled ultrasonication yielded production of tripalmitin-based emulsomes with size 285.6 ± 68.7 nm and zeta potential 31.6 ± 9.3 mV in average. Hexadecylamine in the phospholipid composition conferred the formulation a net positive surface charge. The morphology of emulsomes were investigated with scanning electron microscope. To further investigate whether ultrasonication alters the encapsulation capacity of emulsomes for lipophilic compounds, curcumin was added to the formulation as a model lipophilic substance. The physicochemical features as well as loading capacity of emulsomes produced with the introduced approach were compared with the values in the literature, where emulsomes of the same composition were homogenized through extrusion during their production. The results suggested that the control on temperature at ultrasonication benefited on emulsome production with high reproducibility in size and zeta potential and regarded as the solid feature of the proposed approach. In conclusion, the study provides evidence that the temperature-controlled ultrasonication methodology can safely replace the extrusion step as a robust, reliable approach for production of emulsomes.

Keywords

Emulsome, Ultrasonication, Homogenization, Lipid-based drug delivery systems.

Supporting Institution

Tübitak 2232

Project Number

115C022

Thanks

The author thanks The Scientific and Technological Research Council of Turkey (TÜBİTAK) for support under 2232 Postdoctoral Reintegration Fellowship Program with project number 115C022. The author also thanks to Dr. Hasan Kurt and Sabancı University Nanotechnology Research and Application Center (SUNUM) for providing support to SEM imaging.

Emülzom Üretimindeki Ekstrüzyon Uygulamasının Sıcaklık Kontrollü Ultrasonikasyon ile Değiştirilmesi

Abstract

Emülzomlar, birden çok fosfolipid katmanı ile çevrili katı bir yağ çekirdeğinden oluşan lipit-bazlı ilaç iletim sistemleridir. Stabilite, uzun süreli salım profili, biyouyumluluk ve lipofilik bileşikler için yüksek yükleme kapasitesi en belirgin özellikleridir. Çalışma, emülzomların üretimi ve homojenizasyonu için yaygın olarak kullanılan ekstrüzyon basamağı yerine sıcaklık kontrollü bir ultrasonikasyon prosedürünün uygunluğunu araştırmaktadır. Bu çalışmada ultrasonikasyon ile homojenize edilen emülzomlar, boyut, morfoloji ve zeta potansiyeli gibi fizikokimyasal özelliklere göre değerlendirilmiştir. Sıcaklık kontrollü ultrasonikasyon yöntemi ile, ortalama olarak 285.6 ± 68.7 nm ve zeta potansiyeli 31.6 ± 9.3 mV olan tripalmitin-bazlı emülzomların üretimi sağlanmıştır. Fosfolipid bileşimindeki heksadesilamin, formülasyona net bir pozitif yüzey yükü kazandırmıştır. Emülzomların morfolojisi taramalı elektron mikroskobu ile incelenmiştir. Ultrasonikasyonun emülzomlara yüklenen lipofilik bileşiklerin miktarını değiştirip değiştirmediğini araştırmak için formülasyona lipofilik bileşik olarak kurkumin ilave edilmiştir. Bu şekilde üretilen emülzomların fizikokimyasal özellikleri ve yükleme kapasitesi, aynı bileşime sahip emülzomların üretimleri sırasında ekstrüzyon yoluyla homojenize edildiği literatürdeki değerlerle karşılaştırılmıştır. Sonuçlar, ultrasonikasyonda sırasında sıcaklık üzerindeki kontrolün, boyut ve zeta potansiyeli açısından yüksek tekrarlanabilirlik ile emülzom üretimine uygulanan metodun önemli bir özelliği olarak katkı sağladığı görülmüştür. Netice itibariyle elde edilen sonuçlar, sıcaklık kontrollü ultrasonikasyon metodolojisinin, emülzom üretimi için kullanılan ekstrüzyon uygulamasının yerini güvenle alabileceğine dair kanıt sunmaktadır.

Keywords

Emülzom, Ultrasonikasyon, Homojenizasyon, Lipit-bazlı ilaç iletim sistemleri

Project Number

115C022

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