Topical delivery of l -ascorbic acid spanlastics for stability enhancement and treatment of UVB induced damaged skin

Abstract

l -Ascorbic acid (LAA) is considered a powerful antioxidant that protects skin from premature aging. Maintaining the stability of vitamin C remains the biggest challenge in cosmeceuticals. Our main aim is the entrapment of high dose of vitamin C in spanlastic vesicles to provide maximum stability and efficacy. LAA-loaded spanlastics were prepared by ethanol injection method and were characterized for entrapment efficiency (EE%), particles size (PS), polydispersity index (PDI), zeta potential, deformability index (DI) and in vivo skin permeation. Selected spanlastics formula composed of span 60 and tween 60 (5:1) showed highest EE% of 89.77 ± 3.61% (w/w), high deformability of 11.13 ± 1.145 as well as good physical and chemical stability for 6 months. Improved drug penetration into stratum corneum (SC) was obtained from spanlastics compared to topical LAA solution. Quantitative real time PCR revealed that MMP2 and MMP9 levels were significantly suppressed in response to LAA spanlastics treated rats by 30.4% and 65.3%, respectively, when compared to the control group after exposure to UV irradiation. Results were confirmed by western blot analysis. Histopathological study of rat skin after UV irradiation revealed that application of LAA-loaded spanlastics provided the highest skin protection compared to UVB and LAA solution treated group which was evident by the normal thick epidermal morphology and the densely arranged dermal collagen fibers. LAA-loaded spanlastics successfully improved LAA stability, skin permeation and antioxidant protection against skin photodamage.

Rapid determination of L‐ascorbic acid content in vitamin C serums by ultra‐high‐performance liquid chromatography–tandem mass spectrometry

“…Only formulations with a pH of 3.5 or lower assist transport by promoting the uncharged form of L-AA [9]. Furthermore, the product must have an L-AA concentration ranging from 10% to 20% to be effective [7,16]. Low concentrations are ineffective, while higher concentrations are associated with skin irritation [7].…”

“…Furthermore, the product must have an L-AA concentration ranging from 10% to 20% to be effective [7,16]. Low concentrations are ineffective, while higher concentrations are associated with skin irritation [7]. Besides, the L-AA concentration of 20% is related to maximal percutaneous absorption [9].…”

“…Topical L-AA application can improve the health of facial skin [7,8]. However, L-AA can be a problem in vitamin C serums because of its low stability in formulations [4], which can be accelerated depending on cosmetic composition, packaging and storage conditions [10].…”

“…L‐AA is a potent natural antioxidant used as an active ingredient for skincare products [7]. It has several skincare benefits when applied topically, such as anti‐ageing and anti‐wrinkling activity [7], protects human skin against the effects of UV radiation [8] and is also effective in the treatment of hyperpigmentation [9].…”

Facial Treatment with 3-O-Cetyl Ascorbic Acid for Improvement of Skin Texture: Uptake, Effectiveness, and In Vitro Carcinogenicity Assessment

“…AA is unstable and readily oxidized in the formulation of cosmetics, and it is difficult to deliver into the skin in an adequate quantity [16,17]. Consequently, considerable efforts to improve its topical application have been directed toward the development of new synthetic derivatives and novel delivery methods [18][19][20][21][22][23][24][25].…”