Abstract
Ketoprofen (KET) represents one of the most common drugs used in the topical treatment of pain and inflammations. However, its potential is rather limited due to the very low solubility and photochemical instability. The local administration of KET by conventional products, such as gels, emulgels, creams, and foams, does not guarantee an efficacious and safe treatment because of its low absorption (due to low solubility) and its sensitivity to UV rays. The photodegradation of KET makes many photoproducts responsible for different adverse effects. In the present work, KET was intercalated into the lamellar anionic clay ZnAl-hydrotalcite (ZnAl-HTlc), obtaining the hybrid ZnAl-KET with improved stability to UV rays and water solubility in comparison to the crystalline form (not intercalated KET). The hybrid was then formulated in autoadhesive patches for local pain treatment. The patches were prepared by casting method starting from a hydrogel based on the biocompatible and bioadhesive polymer NaCMC (Sodium carboxymethycellulose) and glycerol as a plasticizing agent. The introduction of ZnAl-KET in the patch composition demonstrated the improvement in the mechanical properties of the formulation. Moreover, a sustained and complete KET release was obtained within 8 h. This allowed reducing the frequency of anti-inflammatory administration, compared to the conventional formulations.
Highlights
Ketoprofen (KET) is one of the most common NSAIDs (Nonsteroidal anti-inflammatory drugs) used for relieving pain in many acute and chronic conditions as musculoskeletal, tendinitis, strain, sprain, trauma, and arthritis [1,2]
The hybrid ZnAl-KET was obtained by ion exchange mechanism (Scheme 1) using ZnAl-NO3, having the following formula obtained by ICP-OES analysis: [Zn0.70 Al0.30 (OH)2](NO3)0.30·0.4 H2O
The hybrid pattern showed a reflection at 2.19 nm, which was increased in comparison to pristine ZnAl-NO3 that shows a reflection at 0.89 nm, typical of nitrate anion (Figure 1A)
Summary
Ketoprofen (KET) is one of the most common NSAIDs (Nonsteroidal anti-inflammatory drugs) used for relieving pain in many acute and chronic conditions as musculoskeletal, tendinitis, strain, sprain, trauma, and arthritis [1,2]. KET exposition to UV radiations, especially UVA, is responsible for phototoxic and photoallergic reactions [5,6]. These reactions are due to radical intermediates generated by KET-UV rays interactions responsible for DNA damage, mitochondria depolarization, and lysosomes destabilization [6,7,8]. KET topical administration by conventional formulations, such as gels, emulgels, creams, sprays, and foams, does not guarantee protection from UV radiation, exposing the patient to serious health problems [9]. Conventional formulations are responsible for a limited residence time of the drug in the application site
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