betadex and octylmethoxycinnamate

Topical commercial formulations containing diclofenac (DC) were submitted to photostability tests, according to the international rules, showing a clear degradation of the drug. The degradation process was monitored by applying the multivariate curve resolution technique to the UV spectral data from samples exposed to stressing irradiation. This method was able to estimate the number of components evolved as well as to draw their spectra and concentration profiles. Three photoproducts (PhPs) were resolved by the analysis of photodegradation kinetics, according to two consecutive reactions with a mechanism postulated as DC>PhP₁>PhP₂ and PhP₃. Photodegradation rate of DC in gel was found to be very fast, with a residual content of 90% only after 3.90 min under a radiant exposure of 450 Wm(-2). Because of a very slow skin uptake of DC, a prolonged time of exposure to light could lead to a significant decrease of drug available or the uptake of undesired photoproducts. New gel formulations were designed to increase the photostability of DC by incorporating chemical light-absorbers or entrapping the drug into cyclodextrin. Drug photostability resulted increased significantly in comparison with that of the commercial formulations. The gel containing the light-absorbers such as octisilate, octyl methoxycinnamate and a combination thereof showed a residual DC of 90% up to 12.22 min, 13.75 min and 15.71 min, respectively, under the same irradiation power. The best results were obtained by incorporating the drug in β-cyclodextrin with a degradation of 10% after 25.01 min of light exposure.

Topics: Absorption, Radiation; Administration, Cutaneous; Anti-Inflammatory Agents, Non-Steroidal; beta-Cyclodextrins; Chemistry, Pharmaceutical; Cinnamates; Diclofenac; Drug Stability; Excipients; Gels; Kinetics; Least-Squares Analysis; Models, Chemical; Multivariate Analysis; Photolysis; Salicylates; Technology, Pharmaceutical

Awareness of the harmful effects of ultraviolet radiation has led to the increasing use of sunscreens, thus, the development of safe and effective antisolar preparations is important. The inclusion of sunscreen molecules in different release systems, like liposomes (lipo) and cyclodextrins (CD) is therefore required.. The in vivo sun protection factor (SPF), water resistance, and in vitro transdermal penetration test of octyl p-methoxycinnamate (OMC) in different dispersions, such as OMC encapsulated in liposomes (lipo/OMC), OMC encapsulated in β-cyclodextrins (β-CD/OMC), OMC encapsulated in both release systems (lipo/OMC and β-CD/OMC), and an OMC-free formulation were determined.. Although the formulation containing only the lipo/OMC system revealed high value of in vivo SPF (11.0 ± 1.3) and water resistance (SPF = 10.3 ± 2.2), the formulation containing both release systems (lipo/OMC + β-cyclodextrin/OMC) showed the best result in the in vivo SPF test (11.6 ± 1.6). In the penetration test, the formulation containing the lipo/OMC system had better performance, since a high amount of OMC in the epidermis (18.04 ± 1.17 μg) and a low amount of OMC in the dermis (9.4 ± 2.36 μg) were observed. These results suggest that liposomes interact with the cells of the stratum corneum, promoting retention of OMC in this layer.. According to our study, the lipo/OMC system is the most advantageous release system, due to its ability to both increase the amount of OMC in the epidermis and decrease the risk of percutaneous absorption.

Topics: Adult; Analysis of Variance; Animals; beta-Cyclodextrins; Cinnamates; Female; Histocytochemistry; Humans; Liposomes; Skin; Skin Absorption; Sun Protection Factor; Sunscreening Agents; Swine; Ultraviolet Rays

The aim of the study was to investigate the incorporation of the sunscreen agent, octyl methoxycinnamate into cyclodextrin cavities covalently bound to cloth fibres. Tencel, a cellulosic fabric, was grafted with beta-cyclodextrin molecules through reaction with monochlorotriazinyl-beta-cyclodextrin (beta-CDMCT). The finished and untreated textiles were soaked in water-methanol mixtures containing 2% (v/v) of sunscreen agent and subsequently subjected to several washing cycles. The unmodified and modified fabrics were characterized by UV spectrophotometry and thermogravimetric analysis. The level of octyl methoxycinnamate entrapped in the Tencel tissue was determined by high-performance liquid chromatography and was found to be much higher (0.0203%, w/w) for the textile functionalised with beta-CDMCT compared to the unmodified fabric (0.0025%, w/w). In addition, spectrophotometric assessment of UV transmission through the fabric samples using the Transpore test showed that the in vitro sun protection factor of the textile support was markedly enhanced (3.2-fold increase) by impregnation with octyl methoxycinnamate of the beta-CDMCT grafted textile. Hence, even after repeated washings, the beta-CD finished fabric exhibits higher sunscreen agent retention and photoprotective properties than the unmodified textile material.

Topics: beta-Cyclodextrins; Cellulose, Oxidized; Chromatography, High Pressure Liquid; Cinnamates; Clothing; Spectrophotometry, Ultraviolet; Sunscreening Agents; Textiles; Thermogravimetry; Ultraviolet Rays