A comparative evaluation of coenzyme Q10-loaded liposomes and solid lipid nanoparticles as dermal antioxidant carriers

Abstract

Background:The effective delivery of coenzyme Q10 (Q10) to the skin has several benefits in therapy for different skin pathologies. However, the delivery of Q10 to deeper layers of skin is challenging due to low aqueous solubility of Q10. Liposomes and solid lipid nanoparticles (SLN) have many advantages to accomplish the requirements in topical drug delivery. This study aims to evaluate the influence of these nanosystems on the effective delivery of Q10 into the skin. Methods: Q10-loaded liposomes (LIPO-Q10) and SLNs (SLN-Q10) were prepared by thin film hydration and high shear homogenization methods, respectively. Particle size (PS), polydispersity index (PI), zeta potential (ZP), and drug entrapment efficiency were determined. Differential scanning calorimetry analysis and morphological transmission electron microscopy (TEM) examination were conducted. Biocompatibility/cytotoxicity studies of Q10-loaded nanosystems were performed by means of cell culture (human fibroblasts) under oxidative conditions. The protective effect of formulations against production of reactive oxygen species were comparatively evaluated by cytofluorometry studies. Results: PS of uniform SLN-Q10 and LIPO-Q10 were determined as 152.4 ± 7.9 nm and 301.1 ± 8.2 nm, respectively. ZPs were −13.67 ± 1.32 mV and −36.6 ± 0.85 mV in the same order. The drug entrapment efficiency was 15% higher in SLN systems. TEM studies confirmed the colloidal size. SLN-Q10 and LIPO-Q10 showed biocompatibility towards fibroblasts up to 50 µM of Q10, which was determined as suitable for cell proliferation. The mean fluorescence intensity % depending on ROS production determined in cytofluorometric studies could be listed as Q10 $ SLN-Q10 . LIPO-Q10. Conclusion: The LIPO-Q10 system was able to enhance cell proliferation. On the contrary, SLN-Q10 did not show protective effects against ROS accumulation. As a conclusion, liposomes seem to have advantages over SLN in terms of effective delivery of Q10 to skin for antioxidant purposes.

An Overview on Topical Administration of Carotenoids and Coenzyme Q10 Loaded in Lipid Nanoparticles

“…Coenzyme Q10 (CoQ10), also known as ubiquinone or ubidecarenone, is a liposoluble vitamin-like compound that plays a relevant role in several biochemical processes, such as the production of cellular energy in the form of adenosine triphosphate, the mitochondrial electron transport chain, and the inhibition of cell membrane peroxidation [23,[124][125][126][127]. CoQ10 is part of a homologous series of substances that share a common benzoquinone ring structure, differing in the length of the isoprenoid side chain.…”

“…Different types of antioxidant compounds have been topically administered in the skin, such as carotenoids [9][10][11][12][13], coenzyme Q10 [14][15][16][17][18], essential oils [19][20][21], polyphenols [22][23][24][25][26], and vitamins [27][28][29][30][31]. Since only a few active ingredients are effective after topical application due to the barrier function of the skin, lipid nanoparticles have been explored as carriers to enhance bioavailability, skin penetration, and retention of the active ingredients [32][33][34].…”

Development and evaluation of coenzyme Q10 loaded solid lipid nanoparticle hydrogel for enhanced dermal delivery

“…Nano-sized particles have some advantages in overcoming the stratum corneum barrier and penetrating into deeper layers of the skin. Nano-size can act in favor of the interaction of solid lipids of the formulation with lipids of the stratum corneum and passing through the pores in the skin (10,19). The smallest and homogenous dispersion was obtained with F3.…”

“…Q10 loaded SLNs were prepared by the high shear homogenization method (19) using two different probes, 8G and 10G, at different concentrations of ingredients (Table I). C888 was employed as the lipid base; Poloxamer 188 (P188) and Tween 80 (Tw 80) were used as surfactant and co-surfactant, respectively.…”

CoQ10-loaded liposomes combined with UTMD prevented early nephropathy of diabetic rats

“…They can accommodate both hydrophilic and lipophilic candidates, and control release of their encapsulated contents [ 17 ]. Encapsulation of CoQ10 by liposomes improved its water solubility and stability in vivo and in vitro , which was considered to be a promising delivery means [ 18 ]. However, CoQ10-loaded liposome was nonspecifically distributed in vivo and exhibited a short half-life in blood [ 19 ].…”