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Studying the Complex Formation of Sulfonatocalix[4]naphthalene and Meloxicam towards Enhancing Its Solubility and Dissolution Performance

Research Authors
Tayel A. Al Hujran, Mousa K. Magharbeh, Samer Al-Gharabli, Rula R. Haddadin, Manal N. Al Soub and Hesham M. Tawfeek
Research Date
Research Department
Research Journal
Pharmaceutics
Research Publisher
MDPI
Research Vol
13
Research Website
https://doi.org/10.3390/pharmaceutics13070994
Research Year
2021
Research_Pages
994-1012
Research Abstract

The interaction between meloxicam and sulfonatocalix [4] naphthalene was investigated
to improve the meloxicam solubility and its dissolution performance. Solubility behavior was investigated
in distilled water (DW) and at different pH conditions. Besides, solid systems were prepared
in a 1:1 molar ratio using coevaporate, kneading, and simple physical mixture techniques.
Further, they were characterized by PXRD, FT-IR, DCS, and TGA. In vitro dissolution rate for coevaporate,
kneaded, and physical mixture powders were also investigated. Solubility study revealed
that meloxicam solubility significantly increased about 23.99 folds at phosphate buffer of pH
7.4 in the presence of sulfonatocalix [4] naphthalene. The solubility phase diagram was classified as
AL type, indicating the formation of 1:1 stoichiometric inclusion complex. PXRD, FT-IR, DCS, and
TGA pointed out the formation of an inclusion complex between meloxicam and sulfonatocalix [4]
naphthalene solid powders prepared using coevaporate technique. In addition, in vitro meloxicam
dissolution studies revealed an improvement of the drug dissolution rate. Furthermore, a significantly
higher drug release (p ≤ 0.05) and a complete dissolution was achieved during the first 10
min compared with the other solid powders and commercial meloxicam product. The coevaporate
product has the highest increasing dissolution fold and RDR10 in the investigated media, with average
values ranging from 5.4–65.28 folds and 7.3–90.7, respectively. In conclusion, sulfonatocalix [4]
naphthalene is a promising host carrier for enhancing the solubility and dissolution performance of
meloxicam with an anticipated enhanced bioavailability and fast action for acute and chronic pain
.disorders