Ethosomes of Phenylethyl Resorcinol as Vesicular Delivery System for Skin Lightening Applications

Abstract

Ethosome formulations containing phenylethyl resorcinol (PR) were developed. The formulation was produced from 0.5% w/v PR, 0.5% w/v cholesterol from lanolin, 3% w/v L-α-phosphatidylcholine from soybean, 30% v/v absolute ethanol, and water up to 100% v/v. It was characterized by a vesicular size of 389 nm, low polydispersity index of 0.266, zeta potential of −34.19 ± 0.44 mV, high PR entrapment efficiency of 71%, and good stability on storage at 4 and 30°C at 75% RH for 4 months. In vitro studies using pig skin revealed that permeation coefficient of PR from ethosomes was significantly higher than that from liposomes. In vitro retention profiles showed that PR accumulation in pig skin following application of ethosome formulations was 7.4-, 3.3-, and 1.8-fold higher than that achieved using liposomes, 20% propylene glycol solution, and 30% hydroethanolic solution, respectively. An inhibition value of around 80% was measured for antityrosinase activity of PR in pig skin. Consistently, ethosomes exhibited higher tyrosinase inhibition activity and melanin content reduction when compared to other formulations in B16 melanoma cells. Ethosomes did not cause acute dermal irritation in albino rabbits. These findings demonstrate that ethosomes are capable of delivering PR into the skin efficiently and hold promise for topical application of skin lightening products.

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

“…On the same line, hybrid poly (lactic-co-glycolic acid) (PLGA) microspheres have been proposed to improve the encapsulation and control the release of amphiphilic compounds such as phenylethyl resorcinol, leading to 40% enhancement of tyrosinase inhibition in mouse melanoma cells [233]. Ethosomes formulations as well as nanostructured lipid carriers (NLCs) with high encapsulation efficiency and stability have also been developed for the delivery of phenylethyl resorcinol into the skin, exhibiting higher tyrosinase inhibition compared to other formulations in B16 melanoma cells [234,235]. Increased loading and chemical stability was achieved also by the use of smartPearls combined with the UV abosorber Tinosorb S [236].…”

Enhanced stability of phenylethyl resorcinol in elastic vesicular formulations

“…In case of transfersomes, the PR was encapsulated at lipid bilayer of the vesicles. In contrast, ethosomes and invasomes which composed of ethanol in the formulation, the PR could be distributed throughout the vesicle [15][16][17]. The encapsulation of PR within the vesicles helps to protect the PR from the degradation by natural light, resulting in the higher stability for long periods of time.…”

“…In this study, the ethosomes, transfersomes and invasomes were selected to study on improving stability of PR. All vesicles were prepared accounting to the method of our previous reports [15][16][17]. The main composition of all vesicles composed of 3 % w/v SPC: 0.5 % w/v CHOL: 0.5 % w/v PR: up to 100 % v/v water phase.…”

“…Finally, the physical property and total active content were evaluated at initial time and after storing at 4 ± 1, 30 ± 1 and 45 ± 1 C at 75 % RH in a Constant Climate Chamber (Model HPP260, Memmert, Schwabach, Germany) for 4 months. In addition, all formulations were prepared for the morphology study according to the method explained by Limsuwan et al and Amnuaikit et al [16,17]. The surface morphology and the structure within the vesicles were observed by scanning electron microscopy (SEM, Quanta 400, FEI, Czech Republic) and transmission electron microscopy (TEM, JEM-2010, JEOL, Japan), respectively.…”

Phenylethyl Resorcinol Loaded in Liposomal Cream Formulation for Cosmeceutical Application

“…Moreover, PR is safe to use as skin lightening agent since it is non-toxic. There were no adverse effects such as oedema, erythema and eschar in rabbits after 72 h, when 0.5% PR solution was applied in a shortterm exposure [9]. The clinical study on human subjects revealed that 0.5% of PR was more effective than 1% Kojic acid in skin lightening [10].…”