Ethosomal nanocarriers: the impact of constituents and formulation techniques on ethosomal properties, in vivo studies, and clinical trials

Abstract

Ethosomal systems are novel lipid vesicular carriers containing a relatively high percentage of ethanol. These nanocarriers are especially designed for the efficient delivery of therapeutic agents with different physicochemical properties into deep skin layers and across the skin. Ethosomes have undergone extensive research since they were invented in 1996; new compounds were added to their initial formula, which led to the production of new types of ethosomal systems. Different preparation techniques are used in the preparation of these novel carriers. For ease of application and stability, ethosomal dispersions are incorporated into gels, patches, and creams. Highly diverse in vivo models are used to evaluate their efficacy in dermal/transdermal delivery, in addition to clinical trials. This article provides a detailed review of the ethosomal systems and categorizes them on the basis of their constituents to classical ethosomes, binary ethosomes, and transethosomes. The differences among these systems are discussed from several perspectives, including the formulation, size, ζ-potential (zeta potential), entrapment efficiency, skin-permeation properties, and stability. This paper gives a detailed review on the effects of ethosomal system constituents, preparation methods, and their significant roles in determining the final properties of these nanocarriers. Furthermore, the novel pharmaceutical dosage forms of ethosomal gels, patches, and creams are highlighted. The article also provides detailed information regarding the in vivo studies and clinical trials conducted for the evaluation of these vesicular systems.

Preparation and Characterization of Anti-Acne Ethosomes Using Cold and Thin-Layer Hydration Methods

“…The preparation was done at room temperature (25±2°C). The aqueous phase (phosphate buffer pH 7.4) was added dropwise to the organic phase under constant mixing at 700 rpm; the stirring was continued for another 30 min [11]. The ethosomal suspensions were sonicated in 3 cycles for 5 (F2), 10 (F3), or 15 (F4) min, and stored in the refrigerator at 4°C.…”

“…The vesicles produced using the thin-layer hydration method can be categorized as SUVs because they had been sonicated during the formation process. A high ethanol concentration (35% v/v) caused the formation of thin phospholipid bilayers [11]. F4 ethosomes were chosen to be evaluated for the next stage because they had the best characteristics compared to F2 and F3 ethosomes.…”

Untitled

“…Span 80 (Sp-80), sodium cholate (SC) and sodium deoxycholate (SDC) were used as edge activators to enhance the penetrability of vesicles through the skin. In all formulations, cholesterol was added to enhance the stability and entrapment efficiency of drug present in unilamellar or multilamellar vesicles 15 . Functional groups present in all excipients are explained in Table 1, while the FTIR spectra are shown in Table 2, while the FTIR spectra are shown in Fig.…”

Untitled

“…As compared with methyl nicotinate ethosomes, ammonium glycyrrhizinate ethosomes showed better vesicle size ranges were observed between 350 and 100 nm, and entrapment efficiency was found to be 78. 45. Finally, they state that the differences between methyl nicotinate and ammonium glycyrrhizinate in the cumulative amount of drug permeated through human stratum corneum epidermis from the same type of formulations were probably due to the different physicochemical properties of the two molecules because methyl nicotinate erythema depends on two principal factors: Vehicle composition and duration of application.…”