Oral mixed micelle formulations – a novel phospholipid-based platform for safe and effective pediatric drug delivery

Prof. Dr. S. Klein1), University of Greifswald/Germany

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Prof. Dr. Sandra KleinDepartment of Biopharmaceutics and Pharmaceutical Technology, Institute of Pharmacy, University of Greifswald, Greifswald/Germany

People involved

Dr. Frank Karkossa (Postdoc fellow sponsored by the PRC) - Department of Biopharmaceutics and Pharmaceutical Technology, University of Greifswald/Germany (frank.karkossa@uni-greifswald.de)


Oral drug delivery is the most preferred and convenient route of drug administration. Due to high patient compliance, cost-effectiveness, flexibility in formulation design, and the ease of production, over the past decades, solid oral drug products emerged as the most popular dosage forms for adult patients. Whereas in the past particularly in very young children liquid dosage forms were the formulations of choice in oral pediatric drug administration, currently there is also a strong interest in developing solid oral dosage forms for pediatric patients. Although they have an excellent safety profile, to date little attention has been paid to the evaluation of phospholipids in pediatric formulation development. However, this patient group could highly benefit from novel phospholipid-based dosage forms. Besides ensuring patient adherence and allowing for the administration of flexible doses, pediatric formulation concepts should ensure that the drug is sufficiently bioavailable, and the pediatric dosage form is made of excipients that are proven to be non-toxic in this vulnerable patient group. These requirements are a challenge when an enabling formulation is required to guarantee a robust solubilization in the gastrointestinal environment of the target patient group. The combination of natural phospholipids and bile salts in designing mixed micelle formulations represents an interesting formulation approach for developing oral pediatric dosage forms for poorly soluble drugs.1)2)3)4)5) Thus, natural phospholipids will specifically be screened for their applicability in oral pediatric mixed micelle formulations.

The focus of the project is to establish a new phospholipid-based platform by designing a safe and effective oral pediatric dosage form which will close an important gap in oral pediatric drug delivery and promote the use of phospholipids in pediatric formulation development.

Benefit for the community

Even though natural phospholipid excipients derive from renewable sources, represent environmentally friendly excipients and can be considered as non-toxic after oral administration, to date they are unexplored for the applicability in solid oral pediatric drug formulations containing drugs with poor aqueous solubility. The project will help to better understand if and how phospholipids could be used to improve the bioavailability of poorly soluble APIs in pediatric patients. The project is supposed to deliver a new platform for safe and effective oral pediatric dosage forms based on phospholipids. In future projects, this platform approach could also be applied to other patient groups. Since this novel formulation approach might also be an alternative for circumventing existing patents or pending patent application in the field of enabling formulations, it will be of great interest for both industry and academia.

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J. Pharm. Pharmacol. 40, 85-88
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