In vivo and in vitro evaluation of octyl methoxycinnamate liposomes

Abstract

Solar radiation causes damage to human skin, and photoprotection is the main way to prevent these harmful effects. The development of sunscreen formulations containing nanosystems is of great interest in the pharmaceutical and cosmetic industries because of the many potential benefits. This study aimed to develop and evaluate an octyl methoxycinnamate (OMC) liposomal nanosystem (liposome/OMC) to obtain a sunscreen formulation with improved safety and efficacy by retaining OMC for longer on the stratum corneum. Methods: The liposome/OMC nanostructure obtained was tested for enzymatic hydrolysis with lipase from Rhizomucor miehei and biodistribution with liposomes labeled with technetium-99m. The liposome/OMC formulation was then incorporated in a gel formulation and tested for ocular irritation using the hen's egg test-chorio-allantoic membrane (HET-CAM) assay, in vitro and in vivo sun protection factor, in vitro release profile, skin biometrics, and in vivo tape stripping. Results: The liposome/OMC nanosystem was not hydrolyzed from R. miehei by lipase. In the biodistribution assay, the liposome/OMC formulation labeled with technetium-99m had mainly deposited in the skin, while for OMC the main organ was the liver, showing that the liposome had higher affinity for the skin than OMC. The liposome/OMC formulation was classified as nonirritating in the HET-CAM test, indicating good histocompatibility. The formulation containing liposome/OMC had a higher in vivo solar photoprotection factor, but did not show increased water resistance. Inclusion in liposomes was able to slow down the release of OMC from the formulation, with a lower steady-state flux (3.9 ± 0.33 µg/cm 2 /hour) compared with the conventional formulation (6.3 ± 1.21 µg/cm 2 /hour). The stripping method showed increased uptake of OMC in the stratum corneum, giving an amount of 22.64 ± 7.55 µg/cm 2 of OMC, which was higher than the amount found for the conventional formulation (14.57 ± 2.30 µg/cm 2 ). Conclusion: These results indicate that liposomes are superior carriers for OMC, and confer greater safety and efficacy to sunscreen formulations.

Nuclear imaging of liposomal drug delivery systems: A critical review of radiolabelling methods and applications in nanomedicine

“…In dermatology, liposomes and other nanoparticulate formulations have been explored as vehicles, usually to increase transdermal drug delivery, with mixed results [293]. On the other hand, one study used 99m Tc-labelled liposomes to show an increased skin retention and reduced liver uptake of octyl methoxycinnamate, a photoprotective compound widely used in sunscreens [294].…”

Nanomaterials for Skin Delivery of Cosmeceuticals and Pharmaceuticals

“…Another clinical study has shown that flexible liposomes help in wrinkle reduction, have decreased the efflorescence in the treatment of acne and increase skin smoothness [86]. Liposomes have been formulated with chemical (benzophenone-3 [12], octyl methoxy cinnamate [87]) and physical (ZnO and TiO2 [88]) sunscreens to offer UV protection in cosmetic formulations. Liposomes are reported for the delivery of vitamins, mainly in anti-aging creams, moisturizing cream, sunscreens, and for the treatment of hair loss [89].…”

Multidynamic Liposomes in Nanomedicine: Technology, Biology, Applications, and Disease Targeting

“…Octyl methoxycinnamate (OMC) liposomal nanosystem (liposome/OMC) was used successfully as a safe and effective sunscreen formulation [68].…”