Research ArticlesEvaluation of spray congealing as technique for the preparation of highly loaded solid lipid microparticles containing the sunscreen agent, avobenzone
Section snippets
INTRODUCTION
The topical use of sun protective products represents one of the most widespread strategy for protecting human skin against the well-documented damaging effects (erythema, cutaneous photoaging, immune suppression, and various forms of skin cancers) of solar UV radiation (290–400 nm).1, 2, 3 The active ingredients in these products, referred to as UV filters or sunscreen agents, decrease the dose of UV light reaching the skin by absorbing, reflecting, or scattering the radiation.1
While the
Materials
Butyl methoxydibenzoylmethane (avobenzone) was supplied by Merck (Darmstadt, Germany). Hydrogenated soybean phosphatidylcholine (PC) was a gift by Cargill (Hamburg, Germany). Carnauba wax was from Polichimica (Bologna, Italy). The excipients for the cream preparations were from Sigma–Aldrich (Steinheim, Germany) and Henkel (Fino Mornasco, Italy). Methanol, acetonitrile, and water were high-performance liquid chromatography (HPLC)-grade from Merck. All other reagents and solvents were of
Lipid Microparticle Preparation and Characterization
Lipid microparticles with high avobenzone loadings were developed using a conventional melt dispersion method (based on emulsion formation)24 and a spray congealing technique with a novel pneumatic atomizer which enables the nebulization of highly concentrated fluids.27 Both procedures exhibited the advantage of circumventing the use of organic solvents; additionally, spray congealing based on the atomization of a drug dispersion/solution in the molten carrier, is completely solvent free.
CONCLUSIONS
The results reported in this study indicated that the entrapment of avobenzone in lipid microparticles at high loading levels (>40%), represents an effective strategy to reduce the photolability of this UVA filter, while limiting the quantity of SLMs to be introduced in the sunscreen formulation. This is important, since topical products do not support high amount of powder components. Moreover, the spray congealing technique was found to be superior to the traditional method for the
Acknowledgements
The authors are grateful to MIUR (Ministero dell'Istruzione, dell'Università e della Ricerca, Rome, Italy) for financial support.
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