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SHR Neuro Krebs Kardio Lipid Stoffw Microb

Salar-Behzadi, S; Corzo, C; Gomes Lopes, D; Meindl, C; Lochmann, D; Reyer, S.
Novel approach for overcoming the stability challenges of lipid-based excipients. Part 2: Application of polyglycerol esters of fatty acids as hot melt coating excipients.
Eur J Pharm Biopharm. 2020; 148(3):107-117 Doi: 10.1016/j.ejpb.2020.01.009
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Co-Autor*innen der Med Uni Graz

Meindl Claudia

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Abstract:

The application of hot melt coating (HMC) as an economic and solvent-free technology is restricted in pharmaceutical development, due to the instable solid-state of HMC excipients resulting in drug release instability. We have previously introduced polyglycerol esters of fatty acids (PGFAs) with stable solid-state (Part 1). In this work we showed a novel application of PGFAs as HMC excipients with stable performance. Three PGFA compounds with a HLB range of 5.1-6.2 were selected for developing immediate-release formulations. The HMC properties were investigated. The viscosity of molten lipids at 100 °C was suitable for atomizing. The DSC data showed the absence of low solidification fractions, thus reduced risk of agglomeration during the coating process. The driving force for crystallization of selected compounds was lower and the heat flow exotherms were broader compared to conventional HMC formulations, indicating a lower energy barrier for nucleation and lower crystallization rate. Lower spray rates and a process temperature close to solidification temperature were desired to provide homogeneous coating. DSC and X-ray diffraction data revealed stable solid state during 6 months storage at 40 °C. API release was directly proportional to HLB and indirectly proportional to crystalline network density and was stable during investigated 3 months. Cytotoxicity was assessed by dehydrogenase activity and no in vitro cytotoxic effect was observed. Copyright © 2020 Elsevier B.V. All rights reserved.

Find related publications in this database (using NLM MeSH Indexing)

Calorimetry, Differential Scanning -

Chemistry, Pharmaceutical -

Crystallization -

Drug Stability -

Drug Storage -

Esters - chemistry

Excipients - chemistry

Fatty Acids - chemistry

Glycerol - chemistry

Hot Temperature -

Lipids - chemistry

Polymers - chemistry

Technology, Pharmaceutical -

X-Ray Diffraction -

Find related publications in this database (Keywords)

Polyglycerol esters of fatty acids

Hot melt coating

Lipid-based excipients

Solid-state

Stability

Stable release profile

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