Solid Lipid Microparticles by Spray Congealing of Water/Oil Emulsion: An Effective/Versatile Loading Strategy for a Highly Soluble Drug

Spray congealing technique was exploited to produce solid lipid microparticles (SLMp) loaded with a highly water-soluble drug (metoclopramide hydrochloride) dissolved in the aqueous phase of a water in oil (W/O) emulsion. The use of an emulsion as starting material for a spray congealing treatment is not so frequent. Moreover, for this application, a W/O emulsion with a drug dissolved in water is a totally novel path. A ternary diagram was built to optimize the emulsion composition, a factorial design was used to identify the factors affecting the properties of the microparticles and a Design of Experiment strategy was applied to define the impact of process conditions and formulation variables on the SLMp properties.

SLMp were characterized by particle size distribution, morphology, residual moisture, drug content, release behavior, FT-IR analysis and XRPD. The obtained microparticles presented a spherical shape, particle size distribution between 54–98 µm depending on atomizing pressure used during the production step and 2–5% residual moisture 4 days after the preparation. XRPD analysis revealed that lipid polymorphic transition alfa-beta occurs depending on the presence of water. In vitro drug release tests highlighted that all the formulations had a reduced release rate compared to the drug alone. These results suggest that spray congealing of a W/O emulsion could be proposed as a good strategy to obtain SLMp with a high loading of a hydrophilic drug and able to control its release rate.

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Materials

Metoclopramide hydrochloride (MCP, batch 100220002) was purchased from AMSA (Milan, Italy) and used “as received”. Softisan 154 (SFT, hydrogenated palm oil, batch 001296) and Imwitor 600 (IMW, polyglyceryl‐3 poly‐ricinoleate, batch 003153) were kindly donated by IoI Oleo GmbH (Witten, Germany). All other chemicals were of analytical grade.

Candiani, A.; Milanesi, A.; Foglio Bonda, A.; Diana, G.; Bari, E.; Segale, L.; Torre, M.L.; Giovannelli, L. Solid Lipid Microparticles by Spray Congealing of Water/Oil Emulsion: An Effective/Versatile Loading Strategy for a Highly Soluble Drug. Pharmaceutics 2022, 14, 2805. https://doi.org/10.3390/pharmaceutics14122805