Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Development of a Versatile Lipid Core for Nanostructure Lipid Carriers (NLC) Using Design of Experiments (DoE) and Raman Mapping

Version 1 : Received: 5 January 2024 / Approved: 6 January 2024 / Online: 8 January 2024 (06:27:32 CET)

A peer-reviewed article of this Preprint also exists.

Rios, C.A.; Ondei, R.; Breitkreitz, M.C. Development of a Versatile Lipid Core for Nanostructured Lipid Carriers (NLCs) Using Design of Experiments (DoE) and Raman Mapping. Pharmaceutics 2024, 16, 250. Rios, C.A.; Ondei, R.; Breitkreitz, M.C. Development of a Versatile Lipid Core for Nanostructured Lipid Carriers (NLCs) Using Design of Experiments (DoE) and Raman Mapping. Pharmaceutics 2024, 16, 250.

Abstract

In the study, a lipid mixture was developed and optimized using a broad range of excipients of different po-larities. Initially, the excipients were classified according to their behavior in water. Then binary mixtures were prepared using cetyl palmitate (Crodamol™ CP pharma) as the solid lipid. The miscibility between the excipients was evaluated using Raman chemical images obtained by classical least squares (CLS). Based on the results, the excipients Crodamol™ CP pharma (cetyl palmitate, hydrophobic), Super Refined™ DMI (di-methyl isosorbide; hydrophilic) and Super Refined™ Lauryl Lactate (medium polarity) were chosen to com-pose the lipid core. The ideal proportion of these excipients was determined using a Mixture Design and the standard deviation of image histograms as responses. The main goal was to develop a versatile lipid core for ‘brick-dust type of drugs’. After statistical evaluation of the DOE results, the final composition was deter-mined and drugs with different logP (0 to 10) and physiochemical characteristics were evaluated in the opti-mized mixture. The drugs butamben, tacrolimus, atorvastatin calcium and resveratrol presented a homoge-neous distribution in the optimized lipid core, indicating that the core has indeed the capability to be used in NLC formulations of such type of drugs.

Keywords

Nanostructured Lipid Carriers; Raman Mapping; Design of Experiments; Classical Least Squares

Subject

Medicine and Pharmacology, Pharmacy

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