Microparticles derived from marine sponge collagen (SCMPs): preparation, characterization and suitability for dermal delivery of all-trans retinol.

Collagen microparticles were prepared using marine sponge collagen. For this purpose a previous method by R?ssler et al. (J. Microencapsul. 12 (1995) 49) of emulsification and cross-linking of native calf collagen was modified. The modified method for sponge collagen microparticles (SCMPs) achieved a yield of 10%. Scanning electromicroscopic photographs showed spherical particles with a diameter of 120-300 nm and photon correlation spectroscopic measurements indicated particle size range from 126 (+/-2.9) to 2179 (+/-342) nm. This broad size distribution was caused by some agglomerates that could not be destroyed by ultrasonication. The surface charge was measured as a function of pH. At pH 2.8 the particles were nearly uncharged, at pH 9.0 the particles showed a strong negative charge of about -60 mV. The preformed SCMPs were loaded by adsorption of all-trans retinol. A loading of up to 8% was obtained. Retinol-loaded SCMPs were incorporated into hydrogels and drug stability was investigated. The in vitro penetration of retinol into hairless mice skin in this formulation was compared to retinol formulations without microparticles. The SCMPs had no influence on the chemical stability of retinol in the hydrogel. The dermal penetration of retinol into the skin increased significantly by approximately two-fold.