Benzophenone-3 entrapped in solid lipid microspheres: formulation and in vitro skin evaluation.
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.
Mestres
J P
JP
Laboratoire de Chimie Analytique, Faculté de Pharmacie, Université de Montpellier 1, 15 Avenue C. Flahault, BP 14491, 34093 Montpellier, Cedex 5, France.
Duracher
L
L
Baux
C
C
Vian
L
L
Marti-Mestres
G
G
D000279:Administration, Cutaneous; D000818:Animals; D001577:Benzophenones / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D004337:Drug Carriers / Q000737:chemistry*; D004355:Drug Stability; D004431:Ear, External; D066298:In Vitro Techniques; D008055:Lipids / Q000737:chemistry*; D008863:Microspheres; D010316:Particle Size; D010539:Permeability; D012867:Skin / Q000187:drug effects* / Q000378:metabolism; D012869:Skin Absorption / Q000187:drug effects; D013473:Sunscreening Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D013552:Swine
D001577:Benzophenones; D004337:Drug Carriers; D008055:Lipids; D013473:Sunscreening Agents; C005290:oxybenzone