Emerging role of nanocrystals in pharmaceutical applications: A review of regulatory aspects and drug development process

A significant majority of the 20 approved nanoformulations consist predominantly of nanocrystals (NCs). NCs are nanosized drug moieties comprising 100 % of the drug with insignificant amounts of stabilizer. Their nanoscale dimensions bestow upon them key attributes such as improved dissolution rate due to increased surface area, and increased permeability due to increased adhesion, which contributes to improved bioavailability. Recent advancements, including crystal composition modifications for tailored release profiles and the incorporation of targeting moieties through the coating, have expanded the applicability of NCs across diverse administration routes for various diseases.

Highlights

Nanocrystals are nanosized particles composed of 100 % drug in crystalline form formulated along with a stabilizer.

The methodologies employed for the production of nanocrystals can be categorized as either top-down or bottom-up, depending on the nature of the drug material.

Nanocrystals possess remarkable bio-adhesive properties which improve dissolution, solubility and bioavailability of poorly soluble drugs.

Over 30 % of all drug product applications involving nanomaterials are submitted for products containing nanocrystals.

Although, nanocrystals have penetrated the health care market to a great extent, bottlenecks associated with the manufacturing and processing still prevail.

This review aims to provide a comprehensive understanding of NC fabrication methods and elucidate the favorable traits inherent in NCs that facilitate temporospatial drug delivery. Furthermore, the regulatory aspects governing the development and approval of nanocrystal-based formulations, highlighting the key considerations and challenges in compliance with pharmaceutical regulations are also reviewed. Additionally, it delves into the integration of nanocrystals in the drug development process, exploring their potential to revolutionize formulation strategies and improve therapeutic efficacy. Through a comprehensive examination of recent advancements and regulatory frameworks, this review provides insights into the evolving landscape of nanocrystals in pharmaceutical applications, emphasizing their transformative impact on drug development and regulatory compliance.

Padakanti Sandeep Chary, Samia Shaikh, Valamla Bhavana, Naveen Rajana, Ravindra Vasave, Neelesh Kumar Mehra, Emerging role of nanocrystals in pharmaceutical applications: A review of regulatory aspects and drug development process, Applied Materials Today, Volume 40, 2024, 102334, ISSN 2352-9407,
https://doi.org/10.1016/j.apmt.2024.102334.

excipients formulation