PubMed · 13369312
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M L QUARTI. 1956-07-28. [Cutaneous staphylococci].. https://pubmed.ncbi.nlm.nih.gov/13369312/
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Percutaneous penetration enhancers (PPEs) are chemicals used to enhance the transdermal delivery of drugs. Fifty-eight of the approximately 150 PPEs used for the transdermal delivery of drugs have been reported in cigarette mainstream smoke (MS). MS is a complex aerosol of minute liquid droplets (termed the particulate phase) suspended within a mixture of gases (CO(2), CO, NO(x), etc.) and semi-volatile compounds. The gases and many of the semi-volatiles are termed the vapor phase. Twenty-nine of the 58 PPEs have been identified in MS vapor phase, 15 in the particulate phase and 14 in both the vapor and particulate phases. There is a tendency for MS PPEs to be hydrophobic, with 40 of the 58 compounds (69%) being either hydrophobic or strongly hydrophobic, and only 24% being hydrophilic. Many of the 4800 known constituents of MS are hydrophilic and would not be expected to readily cross cell membranes or penetrate tissue when delivered as single compounds. The in vivo effect on biological activity of the juxtaposition within the cigarette smoke aerosol of the large number of hydrophilic constituents with the 58 PPEs is currently unknown. As an initial step in understanding this potential complex interaction, the 58 PPEs in MS have been identified and a number of molecular parameters related to the ability to penetrate tissue have been calculated, including MS concentration, measured and calculated base ten logarithm of the octanol-water partition coefficient (Mlog P and Clog P), molecular volume (MgVol) and calculated molar refractivity (CMR).
Cannabidiol (CBD) is a new drug candidate for treatment of rheumatic diseases. However, its oral administration is associated with a number of drawbacks. The objective of this study was to design a transdermal delivery system for CBD by using ethosomal carriers. CBD ethosomes were characterized by transmission electron microscopy, confocal laser scanning microscopy and differential scanning calorimetry. Results indicated that CBD and phosphatidylcholine form an eutectic mixture. In vivo application of ethosomal CBD to CDI nude mice produced a significant accumulation of the drug in the skin and in the underlying muscle. Upon transdermal application of the ethosomal system to the abdomen of ICR mice for 72 h, steady-state levels were reached at about 24 h and lasted at least until the end of the experiment, at 72 h. Furthermore, transdermal application of ethosomal CBD prevented the inflammation and edema induced by sub-plantar injection of carrageenan in the same animal model. In conclusion, ethosomes enable CBD's skin permeation and its accumulation in a depot at levels that demonstrate the potential of transdermal CBD to be used as an anti-inflammatory treatment.
OBJECTIVE: To investigate short-term and long-term effects of combined hormone replacement therapy (HRT) on C-reactive protein (CRP) and fibrinogen plasma concentrations in healthy postmenopausal women. METHODS: In this cross-sectional study 241 healthy postmenopausal women were enrolled. A total of 81 women were receiving the following treatments for 3 months; transdermal 17beta-estradiol (17beta-E2) + medroxyprogesterone acetate (MPA) (n = 21), oral 17beta-E2 + norethisterone acetate (NETA) (n = 27), and conjugated equine estrogens (CEE) + MPA (n = 33). The same combined therapies were implemented in another 58 women for 12 months; transdermal 17beta-E2 + MPA (n = 10), oral 17beta-E2 + NETA (n = 16), and CEE + MPA (n = 32). Control group included 102 healthy postmenopausal women not receiving HRT. The effect of the type and the duration of HRT regimens on plasma levels of CRP, fibrinogen and lipids were investigated. RESULTS: Median CRP concentrations were significantly higher in women receiving oral 17beta-E2 + NETA (P = 0.037) and CEE + MPA (P = 0.0001) for 3 months than in women taking the same types of HRT for 12 months and of those were not on HRT. Median CRP levels were similar in women taking transdermal 17beta-E2 + MPA for 3 and 12 months, compared with controls. Fibrinogen levels were not different between nonusers and any group of HRT users. CONCLUSIONS: These elevated levels of CRP, which appears very recently as a crucial marker for cardiovascular disease, may be responsible for the early increased cardiovascular risk after starting oral combined HRT. But this increased risk in the early period seems to decrease with long-term use. Transdermal 17beta-E2 + MPA had insignificant effect on CRP both in short-term or in long-term use.