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

• Published in: European journal of pharmaceutics and biopharmaceutics Vol. 54; no. 2; pp. 125 - 133
• Main Authors: Swatschek, Dieter, Schatton, Wolfgang, Müller, Werner E.G, Kreuter, Jörg
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 01.09.2002; Elsevier Science
• Subjects: Administration, Cutaneous; All- trans retinol; Animals; Biological and medical sciences; Collagen - chemistry; Collagen - pharmacology; Dermal drug delivery; Drug Carriers - chemistry; Drug Compounding; Drug Stability; Female; General pharmacology; In Vitro Techniques; Marine sponge collagen; Medical sciences; Mice; Mice, Hairless; Particle Size; Pharmaceutical technology. Pharmaceutical industry; Pharmacology. Drug treatments; Porifera; Skin Absorption; Sponge Chondrosia reniformis; Sponge collagen microparticles; Vitamin A - administration & dosage; Vitamin A - chemistry; Vitamin A - metabolism; Sponge collagen microparticles; Sponge Chondrosia reniformis; Dermal drug delivery; Marine sponge collagen; All- trans retinol; Encapsulation; Particle size; Chemical stability; Drug carrier; Percutaneous route; pH; Microparticle; Chemical properties; Physical structure; Surface charge; Pharmaceutical technology; Control release polymer; Rodentia; Permeation; In vitro; Retinol; Vertebrata; Mammalia; Mouse; Animal; Collagen; Dosage form; Sponge; Skin; Hydrogel; Physicochemical properties
• ISSN: 0939-6411; 1873-3441
• DOI: 10.1016/S0939-6411(02)00046-2

Collagen microparticles were prepared using marine sponge collagen. For this purpose a previous method by Rössler 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.