Delim application of innovative methods for enhanced API bioavailability

Milan, Italy: – Innovative CRO Delim Cosmetics & Pharma s.r.l. has successfully applied leading-edge solid-state transformation methods, such as spray drying amorphization and solvent wetting granulation, to produce API active pharmaceutical ingredients with superior bioavailability and biopharmaceutical characteristics.

By transforming crystalline drugs into their amorphous forms, Delim has succeeded in achieving drug formulations with higher apparent solubility, faster dissolution rates, and improved absorption.

Amorphization methods

Solid-state transformations in APIs play a crucial role in the development of effective drug formulations. These transformations can significantly influence the bioavailability and biopharmaceutical characteristics of a drug.

The process of amorphization is significant in solid-state chemistry, as it facilitates the transformation of crystalline active pharmaceutical ingredients (APIs) into amorphous states, thereby enhancing their bioavailability and biopharmaceutical attributes.

This can be achieved through several methods, including milling, quench cooling, spray drying, and lyophilization. Each method disrupts the orderly arrangement of molecules in the crystalline state, resulting in an amorphous form characterized by a lack of long-range molecular order.

Delim spray drying and solvent wetting

Delim adopted the Spray-Drying technique for its versatility and scalability. In this process, a solution containing the API is atomized into fine droplets, which are then rapidly dried using hot gas. The dried particles are then separated from the air in a cyclone separator and collected. This method produces uniform, fine powders with controlled particle sizes. The rapidity of the drying process prevents the API molecule to organize into a crystal and therefore results in the formation of amorphous particles. Spray drying is particularly suitable for producing amorphous forms on a large scale.

Delim has also mastered the Solvent Wetting granulation technique, in which a minimal amount of solvent is used to dissolve the poorly water-soluble drug and uniformly disperse it onto the solid polymeric carrier in a High-Shear mixer. This approach can provide uniform and free-flowing granules while minimizing granular changes in the polymeric carrier, and thereby has the advantage that the pulverization step of the particulates can be omitted in comparison with the co-precipitation approach, in which there’s the precipitation of the drug and polymer together from a solution.

Advancing amorphization

Amorphization represents a powerful strategy to enhance the bioavailability and biopharmaceutical characteristics of APIs. By transforming crystalline drugs into their amorphous forms, it is possible to achieve higher solubility, faster dissolution rates, and improved absorption. However, the inherent instability of amorphous forms necessitates the use of stabilizing techniques and meticulous control of manufacturing processes.

While amorphization offers significant benefits, it also presents challenges. Amorphous forms are thermodynamically unstable and may recrystallize over time, potentially leading to reduced solubility and bioavailability. Therefore, stabilizing agents such as polymers or surfactants must be used to maintain the amorphous state.

As research in solid-state chemistry and pharmaceutical technology advances, Delim sees amorphization as an increasingly important tool in the development of effective and reliable drug formulations.

About Delim

Headquartered at Vimodrone, in Milan, Delim Cosmetics & Pharma s.r.l., has rapidly established itself as a dynamic and innovative Contract Research Organisation (CRO) specializing in the development of novel drugs formulations and generic pharmaceutical products.

Delim specializes in the design, patenting, and technical transfer of innovative and generic pharmaceutical products in line with its core mission to offer highly advanced B2B services to companies that need innovative technical/scientific support for the development of pharmaceutical products.

Delim services include assistance for: patenting, sourcing of API active ingredients, development of prototypes, clinical trials. Also, assistance for: scale-up of manufacturing methods, tech transfer to GMP facilities, production of pilot, validation and bio batches, regulatory consulting and preparation of dossiers for pharmaceutical products registration.

Delim’s in-house specialist expertise takes in development of semi-solid innovative and generic formulations (Q1, Q2, Q3), solid oral formulations for both immediate release and controlled release through technologies such as fluid bed coating and spray drying, in vitro studies of semi-solid products for topical and ophthalmic use, and development and validation of analytical methods.

Its technology portfolio covers a broad range of therapeutic areas and delivery systems including  dermatology, gynecology, pneumology, oncology, and ophthalmology. It also specializes in formulations for medical device delivery in additional application areas such as orthopedics and aesthetic medicine.

To learn more, visit: https://www.delim.it/en

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