TOPICALLY ADMINISTERED, SKIN-PENETRATING GLYCOSAMINOGLYCAN FORMULATIONS SUITABLE FOR USE IN COSMETIC AND PHARMACEUTICAL APPLICATIONS

摘要

The present invention relates to topical glycosaminoglycan compositions, particularly hyaluronan compositions, that facilitate the penetration of modified glycosaminoglycans through the skin barrier into the epidermal and dermal layers of the skin, thereby allowing for the dermal administration of a glycosaminoglycan, such as hyaluronan, without requiring an injection. Through their ability to deliver hyaluronan to the epidermal and dermal layers, the present formulations are therefore suitable for use in dermal rejuvenation, enhancement, hyaluronan replenishment and protection therapy. The glycosaminoglycan compositions are also useful as delivery devices to facilitate the dermal and transdermal delivery of cosmetically and pharmaceutically active substances, including pharmaceuticals, polypeptides, proteins and similarly sized biomacromolecules, through the skin barrier.

主权项

1. A glycosaminoglycan composition comprising a glycosaminoglycan modified through the covalent linkage of a lipid moiety to about 1-15% of the repeating disaccharide monomer units of the glycosaminoglycan wherein:
the glycosaminoglycan to be modified is hyaluronan, a hyaluronan derivative, a polysaccharide comprised of repeating disaccharide units of an uronic acid or hexose linked to a hexosamine, or derivatives thereof; the glycosaminoglycan to be modified has a molecular weight in the range of about 2 kDa to about 2,500 kDa; the lipid moiety comprises one or more naturally-occurring or synthetically-derived fatty acids, glycerolipids, phospholipids, sphingolipids, sterol lipids, prenol lipids, or derivatives thereof, provided that the lipid moiety contains a functional group on its polar head-group to allow for covalent linkage of the lipid to the glycosaminoglycan; and the modified glycosaminoglycan is able to penetrate the skin barrier or a mucous membrane when applied thereto, whereby the modified glycosaminoglycan is formed by the reaction of the glycosaminoglycan with the lipid moiety.