Formulation, Characterisation, and in Vitro Skin Diffusion of Nanostructured Lipid Carriers for Deoxyarbutin Compared to a Nanoemulsion and Conventional Cream

Abstract

The long-term use of topical hydroquinone as an anti-hyperpigmentation treatment has well-known, unwanted effects. Deoxyarbutin (4-[(tetrahydro-2H-pyran-2-yl)oxy]phenol) is a relatively new tyrosinase inhibitor, with stronger inhibitory potency than hydroquinone, that exhibited decreased cytotoxicity against melanocytes and other cells. This study developed novel nanostructured lipid carriers (NLCs) for improved topical delivery of deoxyarbutin (dArb), leading to improved depigmenting efficacy. dArb is a hydrophobic substance, but it easily degrades in aqueous medium and is thermolabile. Screening and optimisation of the solid lipid, liquid lipid, surfactant, co-surfactant and production methods were performed to choose the optimum particle size and stability for NLCs. One percent dArb NLCs were obtained from a combination of cetyl palmitate (CP) and caprylic/capric tryglicerides (Myr) in 12% total lipids using poloxamer 188 (P-188) and polyethylene glycol (PEG) 400 as a surfactant and co-surfactant, respectively, with a particle diameter of approximately 500 nm and a polydispersity index (PI) <0.4. These NLCs were produced using the simple method of high-shear homogenisation (10,000 rpm, 5 minutes) and ultrasonication (3.5 min). The compatibility between the substances in the formula was evaluated using Fourier Transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). The morphology of the NLCs was observed using transmission electron microscopy (TEM). In vitro penetration of dArb NLCs was evaluated and compared to the nanoemulsion (NE) and conventional emulsion (CR) delivery methods across Spangler’s membrane (SS). Delivery improvement was clearly observed, and after 8 h of application, dArb gel-NLCs showed the highest dArb penetration, followed by liquid NLCs, NE, and CR.

New Preparation Method Using Microwave, Kinetics, In Vitro Dissolution‐Diffusion, and Anti‐Inflammatory Study of Diclofenac‐ Proline Co–Crystal

“…The MW method require solvent with a high value for this parameter in order to support the rapid nature of this process. Commonly organic solvents are classified according to their heating efficiency in the MW field, with the heating efficiency of ethanol 0.941, followed by methanol at 0.659, and water at 0.123 . In this case, the hydroxyl group of the ethanol bridges the formation of hydrogen bonds, which are supported by the increasing rotational energy from the molecules of both components and is faster than methanol and water.…”

“…In addition to the highest rotation energy of methanol and ethanol compared with the other materials used, the volatility/penetration of these solvents is appropriate to reach the deepest layer of the solid molecules . Furthermore, the dielectric constant is congenial to the DPC binary system . Finally, other variables are affected by different factors, including the powder‘s charge, moisture content, and frequency of rotational energy.…”

Natural and Bioinspired Phenolic Compounds as Tyrosinase Inhibitors for the Treatment of Skin Hyperpigmentation: Recent Advances

“…Reference compounds commonly used as positive controls in the mushroom tyrosinase inhibition assay are kojic acid and β-arbutin (Figure 3), which however are very poor inhibitors (IC 50 > 500 µM) of human tyrosinase [9,47]. Deoxyarbutin has been recently described as a novel tyrosinase inhibitor, with increased skin penetration and binding affinity to human tyrosinase [48][49][50].…”

The Properties and Application of Argan Oil in Cosmetology

“…[102,117,118] Nanostructured lipid carriers with the addition of argan oil in work [119,120] were used to produce semisolidgels, which were tested to determine their textural and sensory properties. [122] The Liposomes are natural carriers of cosmetic and medicinal substances. NLC formulations are also used for the formation of silver nano lipid carriers (sNLC) in form of creams and lotions to treat atopic dermatitis (AD).…”