Oleic acid (OA) is a kind of fatty acid occurring naturally in various animal and vegetable fats and oils. It is an odorless and colorless oil. In chemical terms, OA is classified as a monounsaturated omega-9 fatty acid, abbreviated with a lipid number of 18:1 cis-9. It has the formula CH3(CH2)7CH=CH(CH2)7COOH.
Fig.1 Chemical structure of OA.
Vesicles were prepared with OA as fatty material. Clotrimazole-loaded OA vesicles were prepared by the membrane hydration method. The size, size distribution, shape, thermal behavior, release in vitro, antifungal activity in vitro, skin penetration and retention in vitro, and antifungal activity in vivo of vesicles were characterized. OA vesicles have high drug entrapment efficiency, the best particle size, and good colloidal properties. The in vitro drug release study showed that the drug had the sustained-release effect of vesicle dispersion. Studies on skin penetration and skin retention showed that drugs accumulated in the epidermis of the skin. In vivo studies confirmed that the drug can prolong the release time of OA vesicles up to 5 days, indicating that it can be used for long-term treatment. Therefore, OA vesicles can be used as an effective carrier of antifungal drugs for the treatment of localized fungal infections.
Fig.2 Transmission electron microscopic (TEM) image of optimized clotrimazole-loaded OA vesicles at 80 kV and 50,000×. (Verma, 2014)
Scientists found that an unsaturated fatty acid in the LNP formulation, including OA, can significantly improve the delivery effect for siRNA and miRNA. Compared with the commercial transfection agent Lipofectamine 2000, LNPs containing OA delivered microRNA-122 more efficiently, with a 1.8-fold increase in mature miR-122 expression and a 20% decrease in microRNA-122 target Bcl-w. LNPs containing OA have comparable liver accumulation and in vivo transport efficiency compared to a commercial transfection agent Invivofectamine that was specifically designed for liver transport. The DOTMA-OA LNP formulation showed great advantages for siRNA/miRNA delivery both in vitro and in vivo. The DOTMA-OA LNPs provide a means for delivering pathogenic protein-specific siRNAs/miRNA to hepatocytes. The incorporation of unsaturated fatty acids OA into DOTMA based LNPs showed potent delivery efficacy. The enhanced pH sensitivity, smaller particle size, and surface charge close to neutral could be the main reasons for the observed high delivery efficacy.
Fig.3 Mechanisms of siRNA delivery by DOTMA-OA LNPs. (Wang, 2013)
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