Cerasomes (CS), evolved from liposomes, are novel drug-delivery systems that have potential medical application as carriers for drugs or active ingredients. Although many studies have been conducted on the pharmaceutical and physicochemical properties of CS, the role of CS in influencing the in vivo plasma and topical pharmacokinetics and efficacy of topical drug delivery remain unclear. In this context, we chose cryptotanshinone (CTS) as a model drug for the preparation of CTS-CS by means of the ethanol injection method to investigate their in vitro/in vivo drug-release behavior and in vivo efficacy. (1) In in vitro studies, CTS-CS gel was proven to be capable of achieving a higher permeation rate and significant accumulation in the dermis of isolated rat skin using Franz diffusion cells. (2) In in vivo studies, microdialysis experiments used to measure the plasma and topical pharmacokinetics demonstrated that the CS had a high drug concentration, short peak time, and slow elimination. Meanwhile, the plasma area under the concentration–time curve of CTS-CS gel was less than half that for the CTS gel in 12 h, which indicates that the drug bioavailability dramatically increased in the experiments. (3) In in vivo efficacy studies, we duplicated a rat acne model and performed antiacne efficacy experiments. The CTS-CS gel improved the antiacne efficacy compared to that of ordinary CTS gel. Moreover, it inhibited the expression of interleukin-1α and androgen receptors effectively. All of these results show that CTS-CS gel has significant potential for the treatment of acne induced by inflammation and excessive secretion of androgen, suggesting that CS formulations were designed as a good therapeutic option for skin disease.
Cancer is a major cause of morbidity and mortality all over the world and a promising area of cancer research is concentrated on chemoprevention by nutritional compounds. Capsaicin, traditionally used as a food additive and an analgesic, is one of the main pungent ingredients in chili peppers. Recent studies have shown that capsaicin has anti-cancer effects in various types of cancer model. The purpose of this review is to outline the anticarcinogenic effect of capsaicin and its mechanism.
Glycyrrhiza flavonoids and its major component, licochalcone A, inhibit melanogenesis through MAPK/ERK pathway by activating ERK phosphorylation Dear Editor, Melanin is synthesized mainly by melanocytes that are located in the basal layer of the epidermis and its formation is associated with tyrosinase and dopachrome tautomerase activities [1]. And tyrosinase plays an important role in melanogenesis which can catalyze the hydroxylation of tyrosine to 3, 4-L-dihydroxyphenylalanine (DOPA) and further oxidation of DOPA to dopaquinone [2]. Microphthalmia-associated transcription factor (MITF) is a basic helix-loop-helix leucine zipper transcription factor, which can control the expression of various genes for normal melanin synthesis in melanocytes [3]. Recently, it was reported that melanogenesis was regulated by the MAP kinase family, phosphorylated p38 can activate MITF, promoting melanin synthesis, whereas phosphorylated ERK can inhibit the activation of MITF [1]. When the skin is exposed to ultraviolet radiation (UVR), keratinocytes secrete hormones, such as adrenocorticotropic hormone (ACTH), endothelin-1 (ET-1), and alpha-melanocytestimulating hormone (a-MSH). Subsequently, the melanocortin 1 receptor (MC1R) binds to a-MSH, activating MITF and enhancing the expression of tyrosinase [4].Since 2005, whitening cosmetics and medicines have been developed rapidly, such as kojic acid, arbutin, hydroquinone, and vitamin C, however, these components of whitening cosmetics proved unsatisfactory in clinical applications [5]. Therefore, there is a large demand for new skin-whitening components. In addition, people prefer to use whitening cosmetics that are derived from herbaceous natural sources, to reduce skin irritation. Glycyrrhiza flavonoids(GF) are extracted and separated from the dry roots and rhizomes of Glycyrrhiza and its basic constituents are 2-phenyl chromone compounds. GF inhibit tyrosinase activity and reduce melanin synthesis [6,7], they have been widely used in whitening cosmetics. However, the component of GF that is mainly responsible for whitening and its mechanism of action are still unclear. In the current study, we investigated the inhibitory effects of GF and licochalcone A(lic-A) on tyrosinase in vivo and in vitro, and the possible mechanism for whitening activity in B16 mouse melanoma cells.Firstly, we found that lic-A is one of the main constituents of GF, and its content was approximately 26% of all constituents (Fig. 1A-B). Next, we found that neither GF nor lic-A displayed no observable cytotoxicity below 800 mg/mL and 208 mg/mL, respectively (Fig. 1C), and the result can provide an evidence to select the appropriate drug concentration for subsequent determination of melanin content and tyrosinase activity.Subsequently, we discovered that GF and lic-A both reduced the content of melanin (Fig. 1D) and tyrosinase activity (Fig. 1E) in cultured B16 cells. Furthermore, after treating with the drugs for 24 h, the expression of tyrosinase in the B16 cells was significantly inhibited, 400 mg/mL GF a...
Abbreviations: TDDS, transdermal drug delivery system; FDA, food and drug administration; EC, ethyl cellulose; BPO, benzoyl peroxide; SEM, scanning electron microscopy; AUC, area under the curve; EE, entrapment efficiency; DSC, differential scanning calorimetry; MED, minimal erythemal dose; SPF, sun protection factor IntroductionCompared with drug dosage forms for oral and parenteral administration, Transdermal drug delivery system (TDDS) can minimize and avoid some restrictions relating to dosage forms effectively. Due to the conventional delivery systems suffering from certain restrictions like Peak and Valley phenomenon i.e., they show fluctuations in plasma drug concentration and cannot render sustained effect.1 However, the TDDS can meet the requirement to keep relatively stable plasma drug concentration and prolong delivery of drug, in a steady-state profile and minimizes the peak-associated side effects, which thus ensures the level of the drug is effective for treatment on the minimal therapeutic concentration. In general, Transdermal drug delivery system, as a controlled drug delivery system, is exceedingly humanized, commodious and prolong the period of time of release of drug, if need arises (e.g. systemic toxicity) with less pain sensation while administrating drug candidates. Additionally, TDDS permits the permeation of drugs across the skin and into the systemic circulation which avoids the hepatic first-pass effect observed in the course of oral administration and inconvenience of frequent parenteral administration. As a new drug carrier of TDDS, Microsponges are mostly used for topical 4-10 and oral administration. 11-15 For other topical delivery systems, the traditional delivery systems are required of frequent dosing to keep relatively stable local concentrations of effective constituent for therapeutic effectiveness because of low effectiveness.Thus to avoid this defect it is indispensable to design a new drug delivery system to prolong the residual time of drug in the epidermis or the dermis, while reduce its penetration into the body. For this reason, as a porous polymeric microsphere, Microsponges can fulfill such aims uniquely.4 Microsponges are porous, polymeric microspheres (Figure 1) which are invariably used for topical delivery system; 4-5,7-10 its inside are full of lacunas and its particle size is 5~300μm in diameter. AbstractTransdermal drug delivery system (TDDS) is a dosage form designed to deliver drug through skin by topical route of administration to the systemic circulation or for local treatment. As a new type of dosage form, TDDS has a number of special merits, but inevitably at the same time it possess some distinct disadvantages, such as low permeability and the drug mostly enter the systemic vascular. Microsponges are a kind of micro-sized and polyporous particles which can entrap effective constituents, and are biologically safe. And Microsponges also exhibit distinctive advantage at the aspect of drug release. The TDDS can enhance drug stability, decrease side effec...
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.