Abstract
We have previously reported that heated powder mixtures of ibuprofen (IBU) and high surface area nanocellulose exhibit an enhanced dissolution and solubility of the drug due to IBU amorphization. The goal of the present work was to further elaborate the concept and conduct side-by-side in vitro drug release comparisons with commercial formulations, including film-coated tablets, soft gel liquid capsules, and IBU-lysine conjugate tablets, in biorelevant media. Directly compressed tablets were produced from heated mixtures of 20% w/w IBU and high surface area Cladophora cellulose (CLAD), with 5% w/w sodium croscarmelose (AcDiSol) as superdisintegrant. The side-by side studies in simulated gastric fluid, fasted-state simulated intestinal fluid, and fed-state simulated intestinal fluid corroborate that the IBU-CLAD tablets show more rapid and less variable release in various media compared to three commercial IBU formulations. On the sidelines of the main work, a possibility of the presence of a new meta-crystalline form of IBU in mixture with nanocellulose is discussed.
Highlights
Ibuprofen (IBU) is the most common non-steroidal anti-inflammatory drug from the class of profens, i.e., arylpropionic acid derivatives
We have previously reported that heated powder mixtures of ibuprofen (IBU) and high surface area nanocellulose exhibit an enhanced dissolution and solubility of the drug due to IBU amorphization
CLAD is a special type of nanocellulose powder that features a surface area that is almost two orders of magnitude larger than that of microcrystalline cellulose (MCC), being currently the most common tableting excipient used by the pharmaceutical industry [6]
Summary
Ibuprofen (IBU) is the most common non-steroidal anti-inflammatory drug from the class of profens, i.e., arylpropionic acid derivatives. To avoid the problem of delayed onset, different formulation strategies are currently employed. These include e.g., soft gel liquid capsules filled with solubilized IBU [3] or IBU salt conjugates with aminoacids, e.g., IBU-arginine or IBU-lysine [4,5]. Heated mixtures of 10% w/w IBU with high surface area nanocellulose, such as Cladophora cellulose (CLAD), in a free powder form showed complete IBU amorphisation and thereby augmented IBU dissolution and solubility [6]. It should be noted that the formulation using a heated mixture of 10% w/w IBU with low surface area cellulose, such as MCC, did not result in a similar improvement of dissolution. The observed amorphisation of poorly soluble lipophilic drugs was assigned to high affinity between aromatic organic molecules and cellulose, which is amplified by the available large surface area in CLAD
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