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Article

Liquid Lipids Act as Polymorphic Modifiers of Tristearin-Based Formulations Produced by Melting Technologies

Department of Pharmacy and BioTechnology, University of Bologna, Via S. Donato 19/2, 40127 Bologna, Italy
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Author to whom correspondence should be addressed.
Academic Editor: Maria Camilla Bergonzi
Pharmaceutics 2021, 13(7), 1089; https://doi.org/10.3390/pharmaceutics13071089
Received: 16 June 2021 / Revised: 13 July 2021 / Accepted: 14 July 2021 / Published: 16 July 2021
(This article belongs to the Special Issue Pharmaceutics and Drug Delivery in Italy)
Despite the growing interest in lipid-based formulations, their polymorphism is still a challenge in the pharmaceutical industry. Understanding and controlling the polymorphic behavior of lipids is a key element for achieving the quality and preventing stability issues. This study aims to evaluate the impact of different oral-approved liquid lipids (LL) on the polymorphism, phase transitions and structure of solid lipid-based formulations and explore their influence on drug release. The LL investigated were isopropyl myristate, ethyl oleate, oleic acid, medium chain trigycerides, vitamin E acetate, glyceryl monooleate, lecithin and sorbitane monooleate. Spray-congealing was selected as an example of a melting-based solvent-free manufacturing method to produce microparticles (MPs) of tristearin (Dynasan®118). During the production process, tristearin MPs crystallized in the metastable α-form. Stability studied evidenced a slow phase transition to the stable β-polymorph overtime, with the presence of the α-form still detected after 60 days of storage at 25 °C. The addition of 10% w/w of LL promoted the transition of tristearin from the α-form to the stable β-form with a kinetic varying from few minutes to days, depending on the specific LL. The combination of various techniques (DSC, X-ray diffraction analysis, Hot-stage polarized light microscopy, SEM) showed that the addition of LL significantly modified the crystal structure of tristearin-based formulations at different length scales. Both the polymorphic form and the LL addition had a strong influence on the release behavior of a model hydrophilic drug (caffeine). Overall, the addition of LL can be considered an interesting approach to control triglyceride crystallization in the β-form. From the industrial viewpoint, this approach might be advantageous as any polymorphic change will be complete before storage, hence enabling the production of stable lipid formulations. View Full-Text
Keywords: spray congealing; lipid microparticles; triacylglycerol; drug release; stability; polymorphism spray congealing; lipid microparticles; triacylglycerol; drug release; stability; polymorphism
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MDPI and ACS Style

Bertoni, S.; Passerini, N.; Albertini, B. Liquid Lipids Act as Polymorphic Modifiers of Tristearin-Based Formulations Produced by Melting Technologies. Pharmaceutics 2021, 13, 1089. https://doi.org/10.3390/pharmaceutics13071089

AMA Style

Bertoni S, Passerini N, Albertini B. Liquid Lipids Act as Polymorphic Modifiers of Tristearin-Based Formulations Produced by Melting Technologies. Pharmaceutics. 2021; 13(7):1089. https://doi.org/10.3390/pharmaceutics13071089

Chicago/Turabian Style

Bertoni, Serena, Nadia Passerini, and Beatrice Albertini. 2021. "Liquid Lipids Act as Polymorphic Modifiers of Tristearin-Based Formulations Produced by Melting Technologies" Pharmaceutics 13, no. 7: 1089. https://doi.org/10.3390/pharmaceutics13071089

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