Ethosomes Loaded with Cryptotanshinone for Acne Treatment through Topical Gel Formulation

Abstract

The aim of this study was to develop ethosomes loaded with cryptotanshinone (CPT) and formulate them as a topical gel for the treatment of acne. Ethosomes were prepared and evaluated for vesicle size, CPT loading and encapsulation efficiency. Optimized ethosomes were formulated as Carbomer 974 gels and compared with conventional hydroethanolic gels for transdermal permeation and skin deposition in vitro. The anti-acne activity and skin irritation of the gel was investigated in rabbits. Optimized ethosomes had an average vesicle size of 69.1 ± 1.9 nm with CPT loading and encapsulation efficiency of 0.445 ± 0.007 mg/mL and 40.31 ± 0.67%, respectively. The transdermal flux and skin deposition of the optimized ethosomal gel were 2.5- and 2.1-times those of conventional gels. The ethosomal gel revealed better anti-acne effect with only slight skin irritation. This study demonstrates that ethosomal formulation is an effective dermal delivery system for CPT, and that CPT ethosomal gels are promising future acne treatments.

<p>Novel Drug Delivery Systems for Loading of Natural Plant Extracts and Their Biomedical Applications</p>

“…110 More examples of herbal loaded NE are presented in Table 1. 88,111,112 Dendrimer A dendrimer is a tree-like synthesized polymer that was characterized as having a single central core that gives frequent branches of variously armed macromolecules (external capping and multifunctional groups) ( Figure 6) to achieve better targeting to specific sites. Generally, they are made up of natural or synthetic components such as sugars, nucleotides and amino acids.…”

Mechanism of transdermal permeation promotion of lipophilic drugs by ethosomes

“…19 However, the mechanisms by which ethosomes promote skin penetration of drugs remain elusive. 20,21 Therefore, the following three key questions are critical: Which key ingredient(s) in ethosomes is responsible for their excellent properties in promoting percutaneous penetration? Can ethosomes penetrate into the skin with an intact vesicle structure?…”

“…[29][30][31] In terms of possible mechanisms for ethosomes to promote percutaneous permeation of drugs, two viewpoints have been presented: the first one is that ethanol is a known penetration enhancer, which can disturb the multilamellar and ordered lipid domain, lower the structure density, and enhance the fluidity of the stratum corneum, thus providing the vesicles with flexible characteristics that allow them to penetrate easily into deeper layers of the skin; 32,33 the second one is that phospholipids between the stratum corneum and ethosomal vesicle fuse easily, thus changing the transition temperature, leading to enhanced drug penetration. 34 In our research, we interestingly found that even though the lipid content in the liposomes and the ethanol content in the hydroethanolic solution were equal with those in the ethosomes, after percutaneous penetration, a greater fluorescence intensity in the skin of the ethosomal system was observed, compared with that in the hydroethanolic solution and liposomes (P,0.05; Figure 2B).…”

Nanosized ethanol based malleable liposomes of cytarabine to accentuate transdermal delivery: formulation optimization,in vitroskin permeation andin vivobioavailability

“…The skin deposition and permeation studies on pig skin show that ethosomal gel was significantly superior to conventional hydroethanolic gel. Reports suggested that ethosomal gel are efficient vesicles for cryptotanshinone dermal delivery for acne treatment, which efficiently permeates the drug across rat skin and target pilosebaceous unit for baldness [12][13][14]. Mechanistically, ethosomes have a synergistic effect of their ingredients with skin lipids and showed transdermal superiority over liposomes and hydroethanolic solution.…”