Variation in the volatile constituents of wild and in vitro propagated Tanacetum sinaicum Del. ex DC through GC-MS chemical fingerprint

Tanacetum sinaicum (Asteraceae) is a rare perennial herb growing wild in the mountains of Southern Sinai (Egypt). It is a medicinal and endangered plant. So, this work aimed to develop an in vitro propagation method for the conservation of this highly threatened plant. Sterile seedlings were used as a source of explants which were cultivated on Murashige and Skoog (M&S) media supplemented with different combinations of growth regulators for callus formation and induction of shoots and roots. M&S media with 1 mg/L kinetin (Kn) showed direct shoot induction. For root induction, excised shoots were transferred to M&S medium supplemented with 1 mg/L naphthalene acetic acid (NAA). Moreover, n-hexane extracts of wild and in vitro propagated plants were analyzed for their volatile constituents by gas chromatography-mass spectrometry (GC-MS) which resulted in the identification of 38 and 27 constituents, accounting for 87.75 and 75.51 % of their total composition; respectively

Variation in the volatile constituents of wild and in vitro propagated Tanacetum sinaicum Del. ex DC through GC-MS chemical fingerprint

238-246Tanacetum sinaicum (Asteraceae) is a rare perennial herb growing wild in the mountains of Southern Sinai (Egypt). It is a medicinal and endangered plant. So, this work aimed to develop an in vitro propagation method for the conservation of this highly threatened plant. Sterile seedlings were used as a source of explants which were cultivated on Murashige and Skoog (M&S) media supplemented with different combinations of growth regulators for callus formation and induction of shoots and roots. M&S media with 1 mg/L kinetin (Kn) showed direct shoot induction. For root induction, excised shoots were transferred to M&S medium supplemented with 1 mg/L naphthalene acetic acid (NAA). Moreover, n-hexane extracts of wild and in vitro propagated plants were analyzed for their volatile constituents by gas chromatography-mass spectrometry (GC-MS) which resulted in the identification of 38 and 27 constituents, accounting for 87.75 and 75.51 % of their total composition; respectively

Formulation and Development of Oral Fast-Dissolving Films Loaded with Nanosuspension to Augment Paroxetine Bioavailability: In Vitro Characterization, Ex Vivo Permeation, and Pharmacokinetic Evaluation in Healthy Human Volunteers

Paroxetine (PX) is the most potent serotonin reuptake inhibitor utilized in depression and anxiety treatment. It has drawbacks, such as having a very bitter taste, low water solubility, and undergoing extensive first pass metabolism, leading to poor oral bioavailability (2 × 31 full factorial design was applied to choose the optimized OFDF, utilizing Design-Expert® software (Stat-Ease Inc., Minneapolis, MN, USA). The optimized OFDF (F1) had a 3.89 ± 0.19 Mpa tensile strength, 53.08 ± 1.28% elongation%, 8.12 ± 0.13 MPa Young’s modulus, 17.09 ± 1.30 s disintegration time, and 96.02 ± 3.46% PX dissolved after 10 min. This optimized OFDF was subjected to in vitro dissolution, ex vivo permeation, stability, and palatability studies. The permeation study, using chicken buccal pouch, revealed increased drug permeation from the optimized OFDF; with a more than three-fold increase in permeation over the pure drug. The relative bioavailability of the optimized OFDF in comparison with the market tablet was estimated clinically in healthy human volunteers and was found to be 178.43%. These findings confirmed the success of the OFDFs loaded with PX nanosuspension for increasing PX bioavailability

Tripling the Bioavailability of Rosuvastatin Calcium Through Development and Optimization of an In-Situ Forming Nanovesicular System

In situ forming nanovesicular systems (IFNs) were prepared and optimized to improve Rosuvastatin calcium (RC) oral bioavailability through increasing its solubility and dissolution rate. The IFN was composed of Tween® 80 (T80), cetyl alcohol (CA), in addition to mannitol or Aerosil 200. A single simple step was adopted for preparation, then the prepared formulations were investigated by analyzing their particle size (PS), polydispersity index (PDI), Zeta potential (ZP), entrapment efficiency (EE), and flowability properties. D-optimal design was applied to choose the optimized formulations. The maximum desirability values were 0.754 and 0.478 for the optimized formulations containing 0.05 g CA, 0.18 g T80, and 0.5 g mannitol (OFM) or Aerosil (OFA), respectively. In vitro drug release from the optimized formulations showed a significantly faster dissolution rate when compared to the market product. In vivo performance of the optimized formulations in rabbits was investigated after filling them into enteric-coated capsules. Ultimately, OFA formulation achieved a 3 times increase in RC oral bioavailability in comparison with the market product, supporting the hypothesis of considering IFNs as promising nanocarriers able to boost the bioavailability of BCS class II drugs

The Promising Role of the Potential Medical Benefits of Cannabidiol Derived from an Herbal Plant to Enhance the Hepatic Defense in Adult Male Rats

A critical natural chemical substance present in cannabis Sativa plants that may have therapeutic benefits is Cannabidiol or CBD. The inquiry was made to assess CBD's possible protection against liver injury. Fifty Sprague-Dawley male rats weighing (150±25g) were divided into five equal groups. Group I received distilled water orally, while Group II received an intraperitoneal injection of Doxorubicin (18 mg/kg bwt). Group III received CBD orally, while Group IV received 1 ml of CBD (26 mg/kg bwt) and Group V received Trimetazidine (10 mg/kg bwt), in addition to a single dose of Doxorubicin (18 mg/kg bwt) on the 11th day for both groups (IV, V). The results revealed that the administration of CBD (26 mg/kg bwt) demonstrated a significant improvement in lowering liver enzyme activity (ALT and AST), as well as an impact on decreasing tumor necrosis factor-alpha (TNF- α), interleukin 6 (IL-6), and MDA in liver tissue linked to liver histopathology results, resulting in an increase in serum levels of albumin, total protein, and oxidative stress parameters (SOD and GSH) in rats. In conclusion, Cannabidiol's potential protective properties may be due to its anti-inflammatory and antioxidant properties. Thus, CBD-derived compounds have long saved interest as a cure for a broad choice of hepatic disorders .

Development of Transdermal Oleogel Containing Olmesartan Medoxomil: Statistical Optimization and Pharmacological Evaluation

Olmesartan medoxomil (OLM) is a first-line antihypertensive drug with low oral bioavailability (28.6%). This study aimed to develop oleogel formulations to decrease OLM side effects and boost its therapeutic efficacy and bioavailability. OLM oleogel formulations were composed of Tween 20, Aerosil 200, and lavender oil. A central composite response surface design chose the optimized formulation, containing Oil/Surfactant (SAA) ratio of 1:1 and Aerosil % of 10.55%, after showing the lowest firmness and compressibility, and the highest viscosity, adhesiveness, and bioadhesive properties (Fmax and Wad). The optimized oleogel increased OLM release by 4.21 and 4.97 folds than the drug suspension and gel, respectively. The optimized oleogel formulation increased OLM permeation by 5.62 and 7.23 folds than the drug suspension and gel, respectively. The pharmacodynamic study revealed the superiority of the optimized formulation in maintaining normal blood pressure and heart rate for 24 h. The biochemical analysis revealed that the optimized oleogel achieved the best serum electrolyte balance profile, preventing OLM-induced tachycardia. The pharmacokinetic study showed that the optimized oleogel increased OLM’s bioavailability by more than 4.5- and 2.5-folds compared to the standard gel and the oral market tablet, respectively. These results confirmed the success of oleogel formulations in the transdermal delivery of OLM

Atheroprotective potentials of curcuminoids against ginger extract in hypercholesterolaemic rabbits

<div><p>The anti-atherogenic potentials of total ginger (<i>Zingiber officinale</i>) extract (TGE) or curcuminoids extracted from turmeric (<i>Curcuma longa</i>), members of family Zingiberaceae, were compared in hypercholesterolaemia. Rabbits were fed either normal or atherogenic diet. The rabbits on atherogenic diet received treatments with TGE or curcumenoids and placebo concurrently for 6 weeks (<i>n</i> = 6). The anti-atherogenic effects of curcuminoids and ginger are mediated via multiple mechanisms. This effect was correlated with their ability to lower cholesteryl ester transfer protein activity. Ginger extract exerted preferential effects on plasma lipids, reverse cholesterol transport, cholesterol synthesis and inflammatory status. Curcuminoids, however, showed superior antioxidant activity.</p></div