In vitro evaluation of emulgel formulation for topical application of diclofenac potassium

Year 2024, Volume: 49 Issue: 2, 371 - 381, 30.06.2024

Esra Demirtürk

https://doi.org/10.17826/cumj.1437623

Abstract

Purpose: For superficial pain, nonsteroidal anti-inflammatory medications (NSAIDs) offer sufficient analgesia, particularly in cases of mild to severe dull pain. Diclofenac potassium is one of the most preferred drugs in this group, but its low water solubility and high permeability due to its BCS II class classification makes it a challenging active substance in the formulation process. The aim of this study was to develop and evaluate in vitro of emulgel formulations containing diclofenac potassium.
Materials and Methods: All substances used in the formulation development process were substances in conformity with pharmacope specifications. Emulgel formulations containing diclofenac potassium were prepared and evaluated in terms of pH, conductivity, rheological properties, viscosity, drug release rate and stability.
Results: The method developed and validated for the determination of the active ingredient resulted in a good linear relationship that was established between the peak areas and the concentrations (2.5-40 μg /mL) of diclofenac potassium with the determination coefficient (R2) which equals to 0.9999. F1, F2, F3 and F4 formulations were found to be stable at the end of the 1st and 3rd month when evaluated with the amount of active substance, pH and rheological properties at different temperatures and conditions. Formulations F2 and F4 are more viscous than other formulations F1 and F3. The initial pH values of all prepared formulations were found to be compatible with the skin. When the reological properties of the formulations were studied, they were determined by examining the calculated R2 values of the Herschel-Bulkley reological type (R2 values of F1, F2, F3 and F4 formulations respectively were 0.999045, 0.999301, 0.999650, 0.999631). In the drug release rate studies, the release of active substance from F2 and F4 formulations continued until the 6th hour and reached plateau values.
Conclusion: Diclofenac potassium emulgel can be used as an antiinflammatory analgesic agent for topical drug delivery.

Keywords

Diclofenac potassium, emulgel, topical nonsteroidal anti-inflammatory drug

Project Number

Bulunmamaktadır.

Diklofenak potasyumun topikal uygulaması için emulgel formülasyonunun in vitro değerlendirilmesi

Abstract

Amaç: Yüzeysel ağrılar için nonsteroid antienflamatuvar ilaçlar (NSAİİ), özellikle hafif ve şiddetli donuk ağrı durumlarında yeterli analjezi sağlamaktadır. Diklofenak potasyum bu grupta en çok tercih edilen ilaçlardan biridir, ancak BCS II sınıfı olması nedeniyle düşük suda çözünürlüğü ve yüksek geçirgenliği onu formülasyon sürecinde zorlu bir etken madde haline getirmektedir. Bu çalışmanın amacı diklofenak potasyum içeren emüljel formülasyonları geliştirmek ve bunları in vitro olarak değerlendirmektir.
Gereç ve Yöntem: Formülasyon geliştirme sürecinde kullanılan tüm maddeler farmakope spesifikasyonlarına uygun özellikde maddelerdir. Diklofenak potasyum içeren emülgel formülasyonları pH, iletkenlik, reolojik özellikler, viskozite, salım hızı ve stabilite açısından hazırlanarak değerlendirilmiştir.
Bulgular: Etkin maddenin tayini için geliştirilen ve valide edilen yöntem, pik alanları ile diklofenak potasyumunun konsantrasyonları (2.5-40 μg/mL) arasında iyi bir lineer ilişki sağladığı 0.9999 olarak bulunan tanımlayıcılık katsayısı (R2) ile ortaya konmuştur. F1, F2, F3 ve F4 formülasyonları, etkin madde miktarı, pH ve reolojik özellikleri ile farklı sıcaklıklarda ve koşullarda değerlendirildiğinde 1. ve 3. ayın sonunda stabil olduğu tespit edilmiştir. Formülasyonlardan F2 ve F4 diğerlerinden daha viskozdir. Hazırlanan tüm formülasyonların başlangıç pH değerleri deri ile uyumludur. Formülasyonların reolojik özellikleri incelendiğinde, Herschel-Bulkley tipi sergilediği R2 değerleri incelenerek belirlenmiştir. (R2 değerleri F1, F2, F3 and F4 formülasyonları için sırasıyla 0.999045, 0.999301, 0.999650, 0.999631 olarak bulunmuştur). İlaç salım hızı çalışmaları sırasında, F2 ve F4 formülasyonlarından etkin madde salımı 6. saate kadar artarak devam etmiş ve plato değerlerine ulaşmıştır.
Sonuç: Diklofenak potasyum emüljel, topikal ilaç dağıtımı için antienflamatuar analjezik bir ajan olarak kullanılabilir..

Keywords

Diklofenak potasyum, emüljel, topikal nonsteroidal antienflamatuvar ilaç

Project Number

Bulunmamaktadır.

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