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Int J Pharm. 2010 Nov 15;400(1-2):1-7. doi: 10.1016/j.ijpharm.2010.07.028. Epub 2010 Jul 27.

Benzophenone-3 entrapped in solid lipid microspheres: formulation and in vitro skin evaluation.

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  • 1Laboratoire de Chimie Analytique, Faculté de Pharmacie, Université de Montpellier 1, 15 Avenue C. Flahault, BP 14491, 34093 Montpellier, Cedex 5, France.


Solid lipid microspheres (SLM), lipid-in-water formulations made from oil-and-wax mixtures, were studied concerning feasibility. SLMs were then loaded with a benzophenone-3, water insoluble UVAB-filter intended for dermal application. Microspheres were prepared by dispersion with homogenisers and investigated by polarizing micrography and scanning electron micrography. For the selected formulations, investigations on percutaneous penetration of B-3 capacity were performed "in vitro" using Franz cells. Microspheres, 5-50 μm in size, and a spherical shape were obtained from several mixtures. B-3 was added and the loading capacity of this drug in the SLM was obtained for a maximum of 5% when the lipophilic phase was 18%. The lipophilic mixture with non-ionic surfactants in the selected formulation of lipid microspheres has a favorable effect on size. The selected formulation is also cosmetically adapted and it is composed of physiological and biodegradable lipids. B-3 was released and penetrated into skin more quickly and in greater quantity than in SLM form, from vehicles containing free B-3. This work has shown that SLM is an excellent carrier for lipophilic sunscreens like B-3 in order to decrease the release and penetration rate of this UV absorber compared with B-3 in oily solution.

Copyright © 2010 Elsevier B.V. All rights reserved.

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