Development of Standard Test Methods for Lipid Quantitation in Liposomal Drug Products

S. Majumdar, G. Palui, A. Raghavendra, A.K. Patri
U.S. Food and Drug Administration,
United States

Keywords: nanoparticle, drug delivery,

Summary:

Over the last two decades, there has been a steady increase in submissions to FDA of products containing nanomaterials for drug delivery, gene delivery, and medical devices; however, there is a lack of appropriate documentary and reference material standards to assess the critical quality attributes that facilitate regulatory review and market entry of safe and effective products. The Global Summit on Regulatory Science (GSRS16) brought together international regulators, industry stakeholders, and standards development organizations to identify and prioritize the reference material and documentary standards needs in nanotechnology.1 For drug products containing nanomaterial, especially for liposomes, several standards were identified and slated for collaborative development. Lipid composition and quantitation are critical quality attributes that influence the quality and efficacy of a liposomal drug product, as they affect the stability of liposomes, drug encapsulation and release, and pharmacokinetic properties. Three methods were developed for lipid quantitation in liposomal formulations consisting of cholesterol, 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy (polyethylene glycol)-2000] (DSPE-PEG 2000) and hydrogenated (soy) L-α-phosphatidylcholine (HSPC) employing hyphenation of high-performance liquid chromatography with three different detectors, viz. triple quadrupole mass spectrometer, evaporative light scattering detector, and charged aerosol detector. The methods were validated for robust and reproducible quantitation of the analytes and are currently approved ASTM Standards after significant testing in the laboratory and rigorous review process through FDA and external stakeholders. These standards will benefit the pharmaceutical industry in ascertaining quality assessment and for regulatory submission. This presentation will highlight the development of three ASTM International Standards for liposomal lipid quantitation.2 Reference: [1] Report on the 2016 Global Summit on Regulatory Science (GSRS16) Nanotechnology Standards and Applications (2016). www.astm.org/COMMIT/GSRS16%20Final%20Report.pdf [2] ASTM International E56.08 Sub-committee https://www.astm.org/get-involved/technical-committees/committee-e56/subcommittee-e56/jurisdiction-e5608. Acknowledgements: This work was supported by an Interagency Agreement (IAG) between the U.S. Food and Drug Administration/NCTR and the National Institute of Environmental Health Sciences/NTP (FDA IAG No. 75F40120S05000/NIEHS IAG No. AES17011). Disclaimer: The views expressed are of the presenter and should not be construed to represent FDA’s views or policies.