Nose-to-brain delivery of amisulpride-loaded lipid-based poloxamer-gellan gum nanoemulgel: In vitro and in vivo pharmacological studies

2021 ◽  
Vol 607 ◽  
pp. 121050
Author(s):  
Dnyandev Gadhave ◽  
Shrikant Tupe ◽  
Amol Tagalpallewar ◽  
Bapi Gorain ◽  
Hira Choudhury ◽  
...  
Keyword(s):  
Gellan Gum ◽  
Brain Delivery ◽  
Pharmacological Studies

Ferula hermonis: A Review of Current Use and Pharmacological Studies of its Sesquiterpene Ester Ferutinin

2020 ◽  
Vol 21 (5) ◽  
pp. 499-508 ◽  
Author(s):  
Rémi Safi ◽  
Marwan El-Sabban ◽  
Fadia Najjar
Keyword(s):  
Wide Spectrum ◽  
Endemic Plant ◽  
Anti Cancer ◽  
Pharmacological Studies ◽  
Sexual Impotence ◽  
Novel Applications ◽  
Anti Fungal ◽  
Sesquiterpene Ester

Ferula hermonis Boiss, is an endemic plant of Lebanon, locally known as “shilsh Elzallouh”. It has been extensively used in the traditional medicine as an aphrodisiac and for the treatment of sexual impotence. Crude extracts and isolated compounds of ferula hermonis contain phytoestrogenic substances having a wide spectrum of in vitro and in vivo pharmacological properties including anti-osteoporosis, anti-inflammatory, anti-microbial and anti-fungal, anti-cancer and as sexual activity enhancer. The aim of this mini-review is to highlight the traditional and novel applications of this plant’s extracts and its major sesquiterpene ester, ferutinin. The phytochemical constituents and the pharmacological uses of ferula hermonis crude extract and ferutinin specifically will be discussed.

scholarly journals The Genus Lagochilus (Lamiaceae): A Review of Its Diversity, Ethnobotany, Phytochemistry, and Pharmacology

Plants ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 132
Author(s):  
Nilufar Z. Mamadalieva ◽  
Davlat Kh. Akramov ◽  
Ludger A. Wessjohann ◽  
Hidayat Hussain ◽  
Chunlin Long ◽  
...  
Keyword(s):  
Secondary Metabolites ◽  
Chemical Constituents ◽  
Iridoid Glycosides ◽  
Herbal Medicines ◽  
Future Research ◽  
South Central ◽  
Pharmacological Studies ◽  
Central South

The genus Lagochilus (Lamiaceae) is native to Central, South-Central, and Eastern Asia. It comprises 44 species, which have been commonly used as herbal medicines for the treatments of various ailments for thousands of years, especially in Asian countries. This review aims to summarize the chemical constituents and pharmacological activities of species from the genus Lagochilus to unveil opportunities for future research. In addition, we provide some information about their traditional uses, botany, and diversity. More than 150 secondary metabolites have been reported from Lagochilus, including diterpenes, flavonoids, phenolic compounds, triterpenoids, iridoid glycosides, lignans, steroids, alkaloids, polysaccharides, volatile, non-volatile and aromatic compounds, lipids, carbohydrates, minerals, vitamins, and other secondary metabolites. In vitro and in vivo pharmacological studies on the crude extracts, fractions, and isolated compounds from Lagochilus species showed hemostatic, antibacterial, anti-inflammatory, anti-allergic, cytotoxic, enzyme inhibitory, antispasmodic, hypotensive, sedative, psychoactive, and other activities.

scholarly journals Brain Delivery of Thyrotropin-Releasing Hormone via a Novel Prodrug Approach

Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 349 ◽  
Author(s):  
Katalin Prokai-Tatrai ◽  
Daniel L. De La Cruz ◽  
Vien Nguyen ◽  
Benjamin P. Ross ◽  
Istvan Toth ◽  
...  
Keyword(s):  
Brain Homogenate ◽  
Thyrotropin Releasing Hormone ◽  
Metabolic Stability ◽  
Antidepressant Effect ◽  
Brain Delivery ◽  
Small Peptides ◽  
Releasing Hormone ◽  
Membrane Affinity

Using thyrotropin-releasing hormone (TRH) as a model, we explored whether synergistic combination of lipoamino acid(s) and a linker cleaved by prolyl oligopeptidase (POP) can be used as a promoiety for prodrug design for the preferential brain delivery of the peptide. A representative prodrug based on this design principle was synthesized, and its membrane affinity and in vitro metabolic stability, with or without the presence of a POP inhibitor, were studied. The in vivo formation of TRH from the prodrug construct was probed by utilizing the antidepressant effect of the peptide, as well as its ability to increase acetylcholine (ACh) synthesis and release. We found that the prototype prodrug showed excellent membrane affinity and greatly increased metabolic stability in mouse blood and brain homogenate compared to the parent peptide, yet a POP inhibitor completely prevented prodrug metabolism in brain homogenate. In vivo, administration of the prodrug triggered antidepressant-like effect, and microdialysis sampling showed greatly increased ACh release that was also antagonized upon a POP inhibitor treatment. Altogether, the obtained promising exploratory data warrant further investigations on the utility of the prodrug approach introduced here for brain-enhanced delivery of small peptides with neurotherapeutic potential.

scholarly journals Boosting the Brain Delivery of Atazanavir through Nanostructured Lipid Carrier-Based Approach for Mitigating NeuroAIDS

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1059
Author(s):  
Saif Ahmad Khan ◽  
Saleha Rehman ◽  
Bushra Nabi ◽  
Ashif Iqubal ◽  
Nida Nehal ◽  
...  
Keyword(s):  
Targeted Delivery ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Fold Increase ◽  
Pharmacokinetic Studies ◽  
Nanostructured Lipid Carrier ◽  
Brain Delivery ◽  
The Brain

Atazanavir (ATZ) presents poor brain availability when administered orally, which poses a major hurdle in its use as an effective therapy for the management of NeuroAIDS. The utilization of nanostructured lipid carriers (NLCs) in conjunction with the premeditated use of excipients can be a potential approach for overcoming the limited ATZ brain delivery. Methods: ATZ-loaded NLC was formulated using the quality by design-enabled approach and further optimized by employing the Box–Behnken design. The optimized nanoformulation was then characterized for several in vitro and in vivo assessments. Results: The optimized NLC showed small particle size of 227.6 ± 5.4 nm, high entrapment efficiency (71.09% ± 5.84%) and high drug loading capacity (8.12% ± 2.7%). The release pattern was observed to be biphasic exhibiting fast release (60%) during the initial 2 h, then trailed by the sustained release. ATZ-NLC demonstrated a 2.36-fold increase in the cumulative drug permeated across the rat intestine as compared to suspension. Pharmacokinetic studies revealed 2.75-folds greater Cmax in the brain and 4-fold improvement in brain bioavailability signifying the superiority of NLC formulation over drug suspension. Conclusion: Thus, NLC could be a promising avenue for encapsulating hydrophobic drugs and delivering it to their target site. The results suggested that increase in bioavailability and brain-targeted delivery by NLC, in all plausibility, help in improving the therapeutic prospects of atazanavir.

scholarly journals Pharmacological studies on the laxative effects of Fagonia indica on rodents

2019 ◽  
Vol 14 (4) ◽  
pp. 166-173
Author(s):  
Muhammad Zeeshan Ali ◽  
Malik Hassan Mehmood ◽  
Muhammad Saleem ◽  
Anwar-ul-Hassan Gilani
Keyword(s):  
Ursolic Acid ◽  
Video Clip ◽  
In Vitro Assays ◽  
Aqueous Fraction ◽  
Laxative Effects ◽  
Pharmacological Studies ◽  
Full Screen ◽  
Species Specific

This study explores the pharmacological basis for the folk use of Fagonia indica in constipation using in vivo and in vitro assays. The crude extract of F. indica contained tannins, saponins, anthraquinones, alkaloids, flavonoids, glycosides and phenols. The administration of F. indica extract (100 and 300 mg/kg) to mice caused a partially atropine-sensitive 35 and 42.6% laxation, respectively, similar to ursolic acid which showed 22 and 36% laxation at 10 and 30 mg/kg, respectively. In loperamide-induced constipation mice, F. indica (27.3 and 34.6%) and ursolic acid (15 and 28%) also displayed laxative effects at the aforementioned doses. In mice and rats ileum, F. indica, its fractions (ethyl acetate, aqueous) and ursolic acid produced atropine-sensitive stimulatory effects, while in rats ileum, F. indica and aqueous fraction showed partially atropine-sensitive effects. F. indica and ursolic acid possess laxative and species-specific gut stimulant effects predominantly involving the activation of muscarinic receptor, thus eliciting its folk use in constipation. Video Clip of Methodology: 7 min 7 sec:  Full Screen   Alternate

scholarly journals Development of Meloxicam-Human Serum Albumin Nanoparticles for Nose-to-Brain Delivery via Application of a Quality by Design Approach

Pharmaceutics ◽  
2020 ◽  
Vol 12 (2) ◽  
pp. 97 ◽  
Author(s):  
Gábor Katona ◽  
György Tibor Balogh ◽  
Gergő Dargó ◽  
Róbert Gáspár ◽  
Árpád Márki ◽  
...  
Keyword(s):  
Human Serum Albumin ◽  
Zeta Potential ◽  
Serum Albumin ◽  
Human Serum ◽  
Quality By Design ◽  
Tween 80 ◽  
Critical Parameters ◽  
Brain Delivery

The aim of this study was to optimize the formulation of meloxicam (MEL)-containing human serum albumin (HSA) nanoparticles for nose-to-brain via a quality by design (QbD) approach. Liquid and dried formulations of nanoparticles containing Tween 80 and without the surfactant were investigated. Various properties, such as the Z-average, zeta potential, encapsulation efficacy (EE), conjugation of MEL and HSA, physical stability, in vitro dissolution, in vitro permeability, and in vivo plasma and brain distribution of MEL were characterized. From a stability point of view, a solid product (Mel-HSA-Tween) is recommended for further development since it met the desired critical parameters (176 ± 0.3 nm Z-average, 0.205 ± 0.01 PdI, −14.1 ± 0.7 mV zeta potential) after 6 months of storage. In vitro examination showed a significantly increased drug dissolution and permeability of MEL-containing nanoparticles, especially in the case of applying Tween 80. The in vivo studies confirmed both the trans-epithelial and axonal transport of nanoparticles, and a significantly higher cerebral concentration of MEL was detected with nose-to-brain delivery, in comparison with intravenous or per os administration. These results indicate intranasal the administration of optimized MEL-containing HSA formulations as a potentially applicable “value-added” product for the treatment of neuroinflammation.

Sign in / Sign up

Export Citation Format

Share Document