Protecting Pancreatic β-cells from Metabolic Insults
Christophe Wiart in Medicinal Plants in Asia for Metabolic Syndrome, 2017
Ethylacetate fraction of roots of Acorus calamus L. at a concentration of 25 µg/mL boosted the secretion of insulin by HIT-T15 cells more potently than gliclazide at 10 µmol/L in vitro.471 This fraction inhibited yeast α-glucosidase with an IC50 value of 0.4 mg/mL and this effect was superior to acarbose.471 In ICR mice, the fraction given orally at a single dose of 800 mg/kg lowered glycemia after 1 hour from about 4.8 to 3.2 mmol/L (gliclazide at 100 mg/kg: about 2.5 mmol/L).471 In mice receiving intraperitoneal load of glucose, the extract at 100 mg/kg given orally 1 hour before lowered after 1 hour of glucose injection glucose as potently as gliclazide at 100 mg/kg.471 In mice receiving an oral load of starch, the extract at 100 mg/kg orally lowered 30 minutes postprandial peak.471Acorus calamus L. accumulates β-asarone.472
Vacha
A papaverine-like relaxant, depressant and anti-spasmodic activity has been seen in the essential oil and in its isolated compounds asarone and β-asarone. It inhibited heart rhythms in frogs and dogs and relaxed the tone of isolated intestine. The neuropharmacological action of the oil revealed its sedative and tranquillizing effect. It caused a reduction in anxiety without dullness but with prolonged calming. It enhanced the activity of pentabarbitol and hexobarbital. Asarone antagonized the hyperactive and hallucinogenic effects of mescaline (personal communication). Both asarone and β-asarone are psychoactive, but hallucinogenic in higher doses. The essential oil-free alcohol extract had a sedative and analgesic property. The choloroform extract of the root had a cannabis-like activity, and the intraperitoneal administration of this extract brought about profound behavioural changes in monkeys (Dasgupta et al. 1977). Khare and Sharma (1982) observed anti-epileptic activity in it. Keller et al. (1985) noted that asarone had a spasmolytic activity against histamine. Aqueous alcohol extract reduced the severity of maximum shock-induced seizures but did not exhibit complete protection (Vohora et al. 1990). According to Martis et al. (1991)Acorus may be of use for epilepsy. Prasad and Chakraborty (1992) found it to be less tranquillizing but more hypotensive in nature. Zanoli et al. (1997) studied sedative and hypothermic effects induced by β-asarone and concluded that this compound cannot be considered a direct cannabinomimetic agent.
Apiaceae Plants Growing in the East
Mahendra Rai, Shandesh Bhattarai, Chistiane M. Feitosa in Ethnopharmacology of Wild Plants, 2021
A total of 48 and 46 compounds were identified in the essential oil from leaves and seeds of wild carrot. The seeds essential oil was predominantly composed of oxygenated monoterpens (66.08%) and oxygenated sesquiterpenes (16.41%). The main components were geranyl acetate (52.45%), cedrone S (14.04%), and asarone (11.39%). The oil from leaves is mainly composed of monoterpene hydrocarbons (64.59%) and sesquiterpene hydrocarbons (22.18%) with α-pinene (27.44%), sabinene (25.34%) and germacrene D (16.33%) as its main components (Ksouri et al. 2015). While ninety-one compounds were identified in the essential oil of carrot leaves (Daucus carota L. subsp. sativus) from Iran, the main classes were monoterpenes (30.0%), sesquiterpenes (27.8%) and phenyl propanes (26.4%). The major constituents were trans-anethole (23.5%) and myrcene (14.5%) (Mojaba et al. 2008).
Mechanisms of increased bioavailability through amorphous solid dispersions: a review
Published in Drug Delivery, 2020
Andreas Schittny, Jörg Huwyler, Maxim Puchkov
A fundamental question of uptake from dissolved ASDs is to identify if molecularly dispersed API is the only fraction that is taken up or if entire particles can be absorbed, e.g. by M-cells. A review (Buckley et al., 2013) looking at the uptake from enabling formulations for poorly soluble drugs concluded that based on experimental results from available studies, only supersaturated (i.e. molecularly dissolved) API can increase the transmembrane flux. In contrast, solubilized API (e.g. in micelles from endogenous bile salts or surfactants contained in the formulation) might limit the transport. This is corroborated by a study on biomimetic micelles, where authors conclude that even the uptake of particles mimicking endogenous structures is unlikely (Ma et al., 2017). Furthermore, active uptake mechanisms were not observed for ASDs: using single-pass intestinal backflow (in rats), Cheng et al. (2010) investigated the uptake of bifendate delivered in form of an ASD. There were no indications found that the transport mechanisms were active. Passive diffusion was also observed in a study on α-asarone, which showed an enhanced in vivo bioavailability through ASD formulation (Deng et al., 2017). Therefore, in this section, we assume that only molecularly dissolved API is absorbed significantly by the intestinal epithelium and that this uptake is generally passive (except for API-specific active transport). Alternative routes of uptake are discussed in the next section.
Pharmacokinetics and drug delivery systems for puerarin, a bioactive flavone from traditional Chinese medicine
Published in Drug Delivery, 2019
As mentioned above, single puerarin possessed the ability to across the blood-brain barrier, however to a relatively low degree. Some compounds could improve the absorption rate and distribution level of puerarin in the brain. Borneol and α-asarone could easily penetrate the blood–brain barrier and also promoted many other drugs into brain tissue (Gao et al., 2010; Yi et al., 2017; Wu et al., 2018). From the main brain distribution kinetic parameters, the values of t1/2 and AUC of the puerarin with borneol or α-asarone pretreatment group were obviously greater than that of the puerarin alone group, and the rates of distribution and elimination of the puerarin with borneol or α-asarone pretreatment group were obviously slower than those of the puerarin alone group, with statistically significant differences. Table 1 summarized the effects of single compound on pharmacokinetics of puerarin in rat plasma.
Development and evaluation of a drug-in-adhesive transdermal delivery system for delivery of olanzapine
Published in Expert Opinion on Drug Delivery, 2022
It is widely known that functional excipients such as penetration modifiers and solubilizers can alter skin barrier properties. The incorporation of these excipients can affect the skin barrier properties by either diffusing into the stratum corneum and altering the solubility properties of the skin or disrupting the lipid packing of the stratum corneum [20]. Our previous studies have demonstrated the feasibility of incorporating chemical enhancers into transdermal systems to enhance the permeation of a drug into and across the skin [21]. Our study on the formulation and evaluation of matrix-type transdermal systems also included the use of penetration enhancers such as oleic acid, oleyl alcohol, and isopropyl myristate for enhanced delivery of 4-benzyl piperidine [22]. The current study screened various chemical enhancers such as oleic acid, oleyl alcohol, and isopropyl myristate based on their saturation solubility. Oleic acid had the highest solubility for OZP as compared to the other two. Hence, we compared the delivery of OZP from solutions in PG via passive diffusion and incorporation of the chemical enhancer (10% w/w oleic acid in PG) to understand the effect of oleic acid as a chemical enhancer on the transdermal delivery of OZP. The group with a chemical enhancer (10% oleic acid) delivered a significantly higher amount of OZP than passive diffusion and exceeded the target for 3-day delivery. This study indicated that chemical enhancers significantly increased transdermal delivery of OZP and can be utilized for further development of a transdermal delivery system for OZP. Similar results were reported by Hu et al. about the synergistic effect of using combinations of oleic acid and isopropyl myristate as co-enhancers on the permeability of alpha-asarone in a drug in adhesive patch for the treatment of asthma [23].
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