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.
Highlights
Acne, a multifactorial pathology that affects skin follicles in areas such as face, upper chest and back, is the most common dermatologic disorder, affecting approximately 85% of teenagers [1]
The polydispersity indexes (PDI) were all less than 0.3, indicating that the vesicle population was relatively homogeneous in size
Epidermis thicknesses had no significant difference with those of normal skin (Fig 3A). These results indicate that CPT loaded ethosomal gel had better anti-acne effects
Summary
A multifactorial pathology that affects skin follicles in areas such as face, upper chest and back, is the most common dermatologic disorder, affecting approximately 85% of teenagers [1]. Acne is a chronic inflammatory follicular disorder of the skin, occurring in specialized pilosebaceous units that consist of the follicular canal with its rudimentary hair and a group of sebaceous glands that surround the opening of the follicle [2]. Several molecules are available for acne treatment, the majority fail to tackle all the pathogenic factors and may cause side effects including dryness, skin irritation and photosensitivity [4]. CPT is effective for the clinical treatment of acne vulgaris [6]. The mechanism of CPT in treating acne may be attributed to its anti-bacterial [7, 8], anti-inflammatory [9, 10] and PLOS ONE | DOI:10.1371/journal.pone.0159967 July 21, 2016
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