Immediate-Release Nifedipine Binary Dry Powder Mixtures with Nanocellulose Featuring Enhanced Solubility and...

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Biomedical Engineering

Background:

• Nifedipine (NIF), a calcium channel blocker, exhibits poor solubility and variable bioavailability dependent on formulation.
• Developing effective formulations for poorly soluble drugs like NIF is crucial for therapeutic success.

Purpose of the Study:

• To investigate the potential of dry powder formulations using high surface area nanocellulose (Cladophora cellulose, CLAD) to enhance NIF solubility and dissolution.
• To compare the performance of nanocellulose with conventional microcrystalline cellulose (MCC).

Main Methods:

• Dry powder mixtures of NIF with MCC and CLAD cellulose were prepared by heating at NIF's melting temperature.
• Solid-state properties were analyzed using SEM, DSC, and XRD.
• Drug release was evaluated in biorelevant media: simulated gastric fluid (SGF), fasted-state simulated intestinal fluid (FaSIF), and fed-state simulated intestinal fluid (FeSIF).

Main Results:

• Heated NIF-CLAD mixtures demonstrated significantly enhanced apparent solubility and faster dissolution rates in all tested biorelevant media.
• NIF amorphization within the high surface area nanocellulose powder was identified as the mechanism for improved performance.
• Conventional MCC did not yield comparable improvements in NIF solubility and dissolution.

Conclusions:

• Dry powder formulation with high surface area nanocellulose presents a facile and effective strategy for enhancing the bioavailability of poorly soluble drugs like NIF.
• This approach offers a potentially viable alternative to existing liquid-filled soft gel capsules for calcium channel blockers.