Abstract
In this paper, the optimal composition of a paeonol temperature-sensitive in situ gel composed of poloxamer 407 (P407) was determined, and a preliminary study of its effect on allergic rhinitis was performed. The optimal composition of the paeonol temperature-sensitive in situ gel included 2% paeonol inclusion, 22% P407, 2% poloxamer 188 (P188) and 2% PEG6000, as assessed by thermodynamic and rheological studies. The toad palate model was employed to study the toxicity of the paeonol temperature-sensitive in situ gel on the nasal mucosa. The result of this experiment showed low toxicity to cilia, which allows the gel to be used for nasal administration. The Franz diffusion cell method was used to study the in vitro release of paeonol and suggested that the in vitro release was in line with the Higuchi equation. This result suggests that the paeonol could be absorbed into the body through mucous membranes and had some characteristics of a sustained effect. Finally, the guinea pig model of ovalbumin sensitized allergic rhinitis was used to evaluate the preliminary efficacy of the gel, with the paeonol temperature-sensitive in situ gel showing a significant effect on the guinea pig model of sensitized allergic rhinitis (AR).
Highlights
Allergic rhinitis (AR), known as hyperaesthetic rhinitis, is an allergic inflammatory disease that is caused by a variety of allergens
Nasal toxicity and in vitro release were investigated, and the results of these studies showed that the paeonol thermosensitive gel had low ciliary toxicity and could be used for intranasal administration
The in vitro release data were in line with the Higuchi equation, indicating that the paeonol could be absorbed into body through the mucous membranes and have some sustained effect
Summary
Allergic rhinitis (AR), known as hyperaesthetic rhinitis, is an allergic inflammatory disease that is caused by a variety of allergens. The intranasal administration of drugs has long been used for the treatment of rhinitis and nasal congestion. Intranasal administration can overcome the side effects that occur in the gastrointestinal tract and the hepatic first-pass effect. Drugs are absorbed better, because of the abundant blood and lymphatic capillaries under the nasal mucosa. Because of these properties, intranasal administration can effectively improve the bioavailability of drugs. The scavenging effect of nasal cilia leads to a very short drug residence time on the human nasal mucosal surface (only 15–30 min) [3], which affects the clinical efficacy to some extent. A high research value and various application prospects surround the development of clinically efficacious and safe nasal preparations
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