Influence of solid lipid microparticle carriers on skin penetration of the sunscreen agent, 4-methylbenzylidene camphor.
The objective of this study was to prepare lipid microparticles (LMs) loaded with the sunscreen agent, 4-methylbenzylidene camphor (4-MBC), to achieve decreased skin penetration of this UV filter. The microparticles were produced by the melt dispersion technique using tristearin as lipidic material and hydrogenated phosphatidylcholine as the surfactant. The obtained microparticles were characterized by scanning electron microscopy and differential scanning calorimetry. Release of 4-MBC from the LMs was found to be slower than its dissolution rate. The influence of the LMs' carrier system on percutaneous penetration was evaluated after their introduction in a model topical formulation (emulsion). In-vitro measurements were performed with cellulose acetate membranes in Franz diffusion cells. The 4-MBC release and diffusion was decreased by 66.7-77.3% with the LM formulation, indicating that the retention capacity of the microparticles was maintained after incorporation into the emulsion. In-vivo human skin penetration of 4-MBC was investigated by tape stripping, a technique for selectively removing the upper cutaneous layers. The amount of sunscreen penetrating into the stratum corneum was greater for the emulsion containing non-encapsulated 4-MBC (36.55% of the applied dose) compared with the formulation with the sunscreen-loaded microparticles (24.57% of the applied dose). The differences between the two formulations were statistically significant in the first (2-4) horny layer strips. Moreover, the LMs' effect measured in-vivo was less pronounced than in-vitro. The increased 4-MBC retention on the skin surface achieved by its incorporation in the LMs should enhance its efficacy and reduce the potential toxicological risk associated with skin penetration.
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, via Fossato di Mortara 17, 44100 Ferrara, Italy. sls@unife.it
Santo
S
Scalia
Matteo
M
Mezzena
Valentina
V
Iannuccelli
D000279:Administration, Cutaneous; D000328:Adult; D002164:Camphor / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid; D004337:Drug Carriers / Q000737:chemistry; D004655:Emulsions; D005260:Female; D006801:Humans; D008055:Lipids / Q000737:chemistry*; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D009824:Ointments; D010316:Particle Size; D012867:Skin / Q000378:metabolism*; D012869:Skin Absorption; D013473:Sunscreening Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D013817:Thermography / Q000379:methods
D004337:Drug Carriers; D004655:Emulsions; D008055:Lipids; D009824:Ointments; D013473:Sunscreening Agents; D002164:Camphor; C038939:enzacamene