Background:
Allergic Rhinitis (AR) is a kind of systemic inflammatory response caused by a variety of allergic sources, which is mediated by immunoglobulin IgE. The major clinical manifestations including nasal congestion, itchy, runny nose, sneezing and so on. It affects the patient's normal life seriously. Using the nasal spray is the main way to treat and relieve symptoms allergic rhinitis. Triamcinolone acetonide was the first choice for treatment of allergic rhinitis medicine[1], because it has a very good treatment effect and less adverse reactions, but the solubility is poor[2], so we prepared it into supramolecular inclusion to increase the solubility[3], then promote the absorption of triamcinolone in the nasal cavity, and improving the bioavailability of the drug.
Objective:
The aim of the study was to improve triamcinolone acetonide solubility, So we prepared it into supramolecular inclusion to promote the absorption of triamcinolone in the nasal cavity, and improving the bioavailability of the drug.
Methods:
The supramolecular inclusion solids of triamcinolone cyclodextrin were prepared by freeze-drying method[4], and the preparation conditions of triamcinolone acetonide- hydroxypropyl -β -cyclodextrin supramolecular inclusion was as follows: the feed ratio of host to guest was 12:1, the inclusion time was 2h, and the temperature was 50℃.
Results:
The supramolecular inclusion complex was characterized by differential scanning calorimetry and scanning electron microscopy to verify that the supramolecular inclusion complex had been formed[5]. The results of infrared spectrum showed that triamcinolone acetonide molecules had entered the cavity of the cyclodextrin to form the supramolecular inclusion complex with the cyclodextrin[6], and phase solubility experiment showed that HP-β-CD had solubilization effect on triamcinolone acetonide. The mean particle size measured values of triamcinolone-HP-β-CD supramolecular inclusion compound is 13.61±1.03nm, much less than triamcinolone acetonide nasal spray, and the triamcinolone-HP-β-CD supramolecular inclusion nasal spray is 1.09±0.01, whith is smaller than triamcinolone acetonidewhich, too. This means triamcinolone-HP-β-CD supramolecular inclusion nasal spray has more uniform contact with the nasal cavity, which is better for absorption greatly improved its bioavailability and provided a new therapeutic agent for patients with allergic rhinitis.
Discussion:
In this study, triamcinolone acetonid-hydroxypropyl-β-cyclodextrin supramolecular inclusion complex was successfully synthesized, and then triamcinolone acetonide cyclodextrin nasal spray was successfully developed. Data shows that the mean particle size measured values and the ellipticity of triamcinolone-HP-β-CD supramolecular inclusion nasal spray are much less than triamcinolone acetonide nasal spray, this means triamcinolone-HP-β-CD supramolecular inclusion nasal spray has more uniform contact with the nasal cavity, so, triamcinolone-HP-β-CD supramolecular inclusion nasal spray is better for absorption, can greatly improved its bioavailability, also, provided a new therapeutic agent for patients with allergic rhinitis. In addition, the experimental results of nasal spray on guinea pig AR model showed that triamcinolone-HP-β-CD supramolecular inclusion nasal spray nasal spray had a significant inhibitory effect on guinea pig allergic rhinitis, and the effect was most obvious in the medium-dose and high-dose groups.