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Maria Grazia Saita, Danilo Aleo, Barbara Melilli, Sergio Mangiafico, Melina Cro, Sebastiano Mangiafico; HP-GUAR-LIPID BASED NANOCARRIER FOR TOPICAL OCULAR DELIVERY OF EPA AND DHA. Invest. Ophthalmol. Vis. Sci. 2015;56(7 ):4142.
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© ARVO (1962-2015); The Authors (2016-present)
The greatest difficulties in the development of ophthalmic formulations based on polynsaturated fatty acids (PUFAs), such as EPA and DHA are derived mainly from their water solubility as well as their poor stability to oxidation. The objective of our work was to develop a new drug delivery system able to solubilize and stabilize EPA and DHA both chemically and physically.
EPA and DHA in oil solution were mixed with an Oxygen Blocker Substance (OBS) and nanodispersed in a carbopol / hyaluronic acid / hydroxypropilguar hydrogel to form a lipid based nanocarrier for PUFAs delivery to the ocular surface (FH0114).<br /> Osmolality, pH, droplet size as well as ocular biocompatibility (Corneal Epithelim Cells-HCE test) were evaluated. The chemical stability of EPA and DHA in the final formulation (FH0114) was evaluated with HPLC and compared with that of FH0114 without the OBS (FH0214) under different ICH recommended conditions.
FH0114 nanoparticles size was stable and showed a narrow range of distribution (size: 400-600 nm with an average of 440+20nm). Osmolality ranged from 300-310 mOsm/Kg and pH=6.8-7.2.<br /> EPA and DHA have maintained a concentration higher than 90% after 24 months at room temperature (25°+/- 2° and 60%+/- 5% R.H.). Concentrations of EPA and DHA at the same ICH conditions in the FH0214 were lower than 25% after 3 months.<br /> Ocular biocompatibility (ocular irritation and cytotoxicity tests) evaluated on Human Corneal Epithelium Cells, was good.
The new HP-Guar-Lipid-Based vehicle maintains EPA and DHA chemically and physically stable. The new FH0114 formulation was showed biocompatible with HCE cells and may represents a potentially new therapeutic tool in corneal wound healing as well as in dry eye patients.
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