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Phytosomes as Novel Carriers of Herbal Extracts
Published in Madhu Gupta, Durgesh Nandini Chauhan, Vikas Sharma, Nagendra Singh Chauhan, Novel Drug Delivery Systems for Phytoconstituents, 2020
Sevgi Güngör, Özlem Akbal-Dağıstan, Evren Algın Yapar, Murat Kartal, Yıldız Özsoy
Flavonoids are generally defined as polyphenolic compounds, which are commonly found in edible plants and mainly used for their antioxidant, antithrombotic, and anti-inflammatory properties. Quercetin and Rutin are the most abundant flavonoids and have a larger structure among others; their phytosomal formulations become markedly available (Panche et al., 2016). Terpenoids are widely distributed natural compounds, which are derived via biogenesis through isoprene units. Gingko biloba L. and Cannabis L. are the most commonly used plant for their terpenoid compounds. Both terpenoids and sub-groups of terpenoids, such as carotenoids and isoprenoids, are mainly formulated in phytosomes (Pattanaik and Lindberg, 2015). Terpenes are a class of hydrocarbons of biological origin derived from isoprene and have been utilized due to their pharmacological activities and for antimalarial, fungal and bacterial infections, against depression, the inhibition of cholesterol synthesis, anxiety and addiction, and currently many researchers are focused on cancer therapy as well (Aldred et al., 2009).
Phytochemicals: Some Basics
Published in Scott Mendelson, Herbal Treatment of Major Depression, 2019
Terpenes are common in plants. They are hydrocarbons synthesized from various combinations of the 5-carbon molecular building block isoprene. They are often aromatic, and may serve plants by deterring herbivores or attracting pollinators. They are responsible for the pleasant fragrances of pine and citrus fruits, the floral aroma of lavender, and the pungent odors of marijuana. Terpenes can be simple in structure, such as the hemiterpene isovaleric acid, a four-carbon chain with a methyl group attached. They can also be large and complex, multi-ringed, steroid-like molecules. Terpenes, as a class, are highly lipophilic and penetrate the brain where they can manifest psychiatrically significant effects.
Why Terpenes Matter—The Entourage Effect
Published in Betty Wedman-St Louis, Cannabis as Medicine, 2019
There is a lot more to cannabis than its cannabinoid content. Other therapeutic compounds in cannabis contribute to its smell and aromatic diversity. Terpenes have garnered increased attention as a result of the “entourage effect” which emphasizes that the therapeutic benefits of cannabis are improved when full spectrum compounds—multiple cannabinoids + terpenoids + flavonoids—are used instead of single cannabinoids. The terms terpene and terpenoid are frequently used interchangeably, but they have different meanings. Terpenes are hydrocarbons (the only elements present are hydrogen and carbon), whereas terpenoids have been denatured by oxidation—drying and curing the flowers or chemically modified.
Design, biological evaluation, and molecular modelling insights of cupressic acid derivatives as promising anti-inflammatory agents
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Amal F. Soliman, Diaaeldin M. Elimam, Fardous F. El-Senduny, Manal A. Alossaimi, Mubarak Alamri, Fatma M. Abdel Bar
Since ancient times, plant-derived products have been used to reduce inflammation or inflammation-associated conditions 1. Araucaria trees are coniferous trees grown as ornamental plants, which upon injury, exudate an oleogum resin that protects against invading pathogens2. Few studies reported the biological activities of the oleogum resin of Araucaria heterophylla; mainly as an antiulcerogenic, cytotoxic, and antibacterial agent3. The oleogum resins, containing mainly labdane diterpenes, have been employed topically to treat bruises and dermal inflammation4. Diterpenes are natural products known to exert potent anti-inflammatory activities through various mechanisms4. Labdane-diterpenes were reported to exhibit anti-inflammatory activities in several animal and cell-based bioassays3,4. In addition, the analgesic and anti-inflammatory effects of semisynthetic terpene derivatives were previously described4. Cupressic acid derivatives are the major labdane diterpenes of the oleogum resin of Araucaria heterophylla. Previous studies by our research group reported the antiprotozoal activity of resin-isolated cupressic acids and the anti-inflammatory activities of their microbially transformed metabolites2,5.
Utilization of experimental design in the formulation and optimization of hyaluronic acid–based nanoemulgel loaded with a turmeric–curry leaf oil nanoemulsion for gingivitis
Published in Drug Delivery, 2023
Amal M. Sindi, Khaled M. Hosny, Waleed Y. Rizg, Fahad Y. Sabei, Osama A. Madkhali, Mohammed Ali Bakkari, Eman Alfayez, Hanaa Alkharobi, Samar A Alghamdi, Arwa A. Banjar, Mohammed Majrashi, Mohammed Alissa
For formulation NG4, which contained oleic acid instead of CrO in the developed nanoemulsion, the permeation parameters were also much lower than those of NG1, which contained CrO among its components. For example, NG4 had a Q24 value of 5986 ± 101 µg/cm2 compared with the NG1 value of 7530 ± 215 µg/cm2. Such a reduction in drug permeation affirmed the importance of CrO in improving drug permeation. Its better action might have been due to its terpene content. The presence of terpene compounds increased the drug solubility in membrane lipids and the lipid/protein arrangement was disrupted during permeation enhancement (Sapra et al., 2008). Therefore, there seems to be a lot of potential for the usage of terpenes in topical and buccal formulations.
Development of invaethosomes and invaflexosomes for dermal delivery of clotrimazole: optimization, characterization and antifungal activity
Published in Pharmaceutical Development and Technology, 2023
Sureewan Duangjit, Kozo Takayama, Sureewan Bumrungthai, Jongjan Mahadlek, Tanasait Ngawhirunpat, Praneet Opanasopit
Invaethosomes (I-ETS) and invaflexosomes (I-FXS) are a new combination of invasomes-ethosomes and invasomes-flexosomes, respectively, which are being introduced for the first time in this study. The combination of ethanol and/or polysorbate 20 and d-limonene as potential penetration enhancers was demonstrated in this study. Several types of terpenes were varied. The lipid constituents of the CZ-loaded nanovesicles and their characteristics were defined as causal factors (Xi) and response variables (Yi), respectively. CZ-loaded nanovesicles with a constant concentration of 0.025% w/v CZ, phosphatidylcholine, cholesterol, and various concentrations of ethanol (X1), d-limonene (X2), and polysorbate 20 (X3) were prepared as penetration enhancers. The physicochemical characteristics (e.g. vesicle size, size distribution, zeta potential, and CZ concentration), skin permeation, and antifungal activity of the CZ-loaded I-ETS/I-FXS formulations were characterized. Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction were used to screen and investigate the mechanism of action of various terpenes. The correlation between the causal factors and the response variables was estimated using Design Expert®. The reliability and accuracy of the optimal I-ETS/I-FXS were experimentally evaluated and confirmed. The objective of this study was to develop novel I-ETS and I-FXS to enhance the dermal delivery of CZ. I-ETS and I-FXS were successfully used for dermal delivery of 0.025% w/v CZ.