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The design of novel delivery systems to treat vaginal fungal infections is a topic of high interest. Chitosan, being itself antimicrobial and having good mucoadhesive properties, is an excellent candidate as a delivery matrix for active compounds. In this work, chitosan microcapsules containing dry extracts of Argentinean medicinal plants with proved biological properties (Larrea divaricata, L. cuneifolia, L. nitida, Zuccagnia punctata and Tetraglochin andina) were developed through electrospraying and compared with conventionally used tablets containing the same extracts. Total phenolics, loading efficacy, physical properties, morphology and particle size, molecular organization, water sorption capacity, release of bioactive compounds and biological properties were assessed. The encapsulation process or the inclusion in tablets did not degrade the bioactive compounds of the extracts. The release of phenolic compounds from chitosan microcapsules was faster than from tablets. The fingerprint of released phenolic compounds from microcapsules and tablets was similar to that from the dry extracts and the antioxidant and antifungal capacity remained unchanged. The FT-IR analysis suggested interactions between the chitosan and the extracts, which explained why the microcapsules kept the integrity in slightly acidic media. Increased solubility of the extracts when incorporated in the microcapsules was seen in simulated vaginal fluid, potentially increasing the bioavailability of bioactive compounds in the vaginal environment. This work highlights the potential of the chitosan-based delivery systems for phytomedicines with antifungal and antioxidant activity to be used in vulvovaginal candidiasis.

Larrea divaricata (Ld), Larrea cuneifolia (Lc) and Larrea nitida (Ln) are shrubs occurring in Northwestern Argentina used in traditional medicine to treat fungal and bacterial infections and as anti-inflammatory. Antibacterial and antifungal activity of several Larrea species has been reported. However, their potential use in vaginal infections has been so far not assessed. The aim of this work was to determine the botanical difference between Larrea species, the chemical composition and the activity of Larrea dry extracts (DE) on Candida species isolated from vaginal infections and to assess their potential as antioxidant agents because infections are usually associated with oxidative processes. The main botanical difference between Larrea species resides in the morphology and shape of leaf, leaflets and stipules, presence or absence of mucron and rachis, percentage of coalescence of the leaflets. The position and abundance of the sclerenchymatic tissue at the mind vein and petiole transection allows the differentiation of the three species. The profile of phenolic compounds in the Larrea DE was determined. HPLC-ESI-MS/MS analysis of DE allowed the identification of 2 flavonoids and 10 lignans. Trihydroxy-6,7′cyclolignan was found only in L. divaricata and dihydroxy-methoxy-epoxylignan in L. cuneifolia and L. nitida, nordihydroguaiaretic acid (NDGA) was found in the three species. All extracts showed antioxidant capacity. The DE showed to be effective against Candida albicans and non-albicans strains. According to our results, the local vaginal use of Larrea DE in the concentration range of MIC values for Candida species does not affect the Lactobacillus normal vaginal microbiota. This work adds evidence to the potential use of Larrea DE as phytomedicine in vulvovaginal candidiasis with multiple effects, including antifungal and antioxidant activity.

The flowers and leaves of Ageratina havanensis (Kunth) R. M. King & H. Robinson are traditionally used as a tea to cure several diseases. The production of active secondary metabolites can be affected by several environmental factors such as climate, altitude, rainfall, phenological stage and other conditions that may influence the growth of plants. In this sense, the development of a methodology to compare the chemical composition of plant extracts is needed. The qualitative chemical composition of the ethyl acetate extracts of flowers and leaves, collected in both reproductive and non-reproductive season, was determined by flow injection analysis-electrospray ionization-ion trap tandem mass spectrometry (FIA-ESI-IT-MS n) and ultra-high-performance liquid chromatography coupled to electrospray negative ionization mass spectrometry (UPLC/ESI-MS n). The qualitative chemical composition of the ethyl acetate extracts of flowers and leaves was very similar in all cases. Also the antiviral activity of flowers against human herpes simplex viruses type 1 and 2 (HSV-1, HSV-2) (Herpesviridae) was analyzed. Three glucoside flavonoids were isolated from the ethyl acetate extract of the leaves of A. havanensis collected in flowering season using chromatographic methods and their structures were elucidated by physical and spectroscopic data measurements, and by comparing the obtained data with previously published values. The compounds were identified as 3-O-β-D-glucosyl-7-methoxyaromadendrin (5), 7-O-β-D-glucosyl-4'dihydroxy-5-methoxyflavanone (6) and 5-O-β-D-glucosylsakuranetin (7); this is the first report of the isolation of these compounds in the Asteraceae family. Since the qualitative composition of the extracts of A. havanensis was similar in all cases, it can be expected that the ethyl acetate extract of the leaves collected in the non-reproductive season has anti-herpetic activity similar to that obtained in the reproductive season.