Formulation of Novel Liquid Crystal (LC) Formulations with Skin-Permeation-Enhancing Abilities of Plantago lanceolata (PL) Extract and Their Assessment on HaCaT Cells

Exposure to reactive oxygen species can easily result in serious diseases, such as hyperproliferative skin disorders or skin cancer. Herbal extracts are widely used as antioxidant sources in different compositions. The importance of antioxidant therapy in inflammatory conditions has increased. Innovative formulations can be used to improve the effects of these phytopharmacons. The bioactive compounds of Plantago lanceolata (PL) possess different effects, such as anti-inflammatory, antioxidant, and bactericidal pharmacological effects. The objective of this study was to formulate novel liquid crystal (LC) compositions to protect Plantago lanceolata extract from hydrolysis and to improve its effect. Since safety is an important aspect of pharmaceutical formulations, the biological properties of applied excipients and blends were evaluated using assorted in vitro methods on HaCaT cells. According to the antecedent toxicity screening evaluation, three surfactants were selected (Gelucire 44/14, Labrasol, and Lauroglycol 90) for the formulation. The dissolution rate of PL from the PL-LC systems was evaluated using a Franz diffusion chamber apparatus. The antioxidant properties of the PL-LC systems were evaluated with 2,2-diphenyl-1-picrylhydrazyl (DPPH) and malondialdehyde (MDA) assessments. Our results suggest that these compositions use a nontraditional, rapid-permeation pathway for the delivery of drugs, as the applied penetration enhancers reversibly alter the barrier properties of the outer stratum corneum. These excipients can be safe and highly tolerable thus, they could improve the patient’s experience and promote adherence.

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Isobornylchalcones as Scaffold for the Synthesis of Diarylpyrazolines with Antioxidant Activity

Molecules ◽

10.3390/molecules26123579 ◽

2021 ◽

Vol 26 (12) ◽

pp. 3579

Author(s):

Svetlana A. Popova ◽

Evgenia V. Pavlova ◽

Oksana G. Shevchenko ◽

Irina Yu. Chukicheva ◽

Aleksandr V. Kutchin

Keyword(s):

Antioxidant Activity ◽

Antioxidant Properties ◽

Biological Properties ◽

High Reactivity ◽

Biologically Active ◽

Brain Lipids ◽

Wide Range ◽

Privileged Structure ◽

Vitro Model

The pyrazoline ring is defined as a “privileged structure” in medicinal chemistry. A variety of pharmacological properties of pyrazolines is associated with the nature and position of various substituents, which is especially evident in diarylpyrazolines. Compounds with a chalcone fragment show a wide range of biological properties as well as high reactivity which is primarily due to the presence of an α, β-unsaturated carbonyl system. At the same time, bicyclic monoterpenoids deserve special attention as a source of a key structural block or as one of the pharmacophore components of biologically active molecules. A series of new diarylpyrazoline derivatives based on isobornylchalcones with different substitutes (MeO, Hal, NO2, N(Me)2) was synthesized. Antioxidant properties of the obtained compounds were comparatively evaluated using in vitro model Fe2+/ascorbate-initiated lipid peroxidation in the substrate containing brain lipids of laboratory mice. It was demonstrated that the combination of the electron-donating group in the para-position of ring B and OH-group in the ring A in the structure of chalcone fragment provides significant antioxidant activity of synthesized diarylpyrazoline derivatives.

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Determination of in vitro antioxidant activity of the leaves extracts of Ehretia pubescens

International Journal of Research in Pharmaceutical Sciences ◽

10.26452/ijrps.v11i4.3308 ◽

2020 ◽

Vol 11 (4) ◽

pp. 6262-6267

Author(s):

Krishnamoorthy Meenakumari ◽

Giridharan Bupesh ◽

Mayur Mausoom Phukan

Keyword(s):

Antioxidant Activity ◽

Ethyl Acetate ◽

Radical Scavenging Activity ◽

Antioxidant Properties ◽

Radical Scavenging ◽

Reducing Power ◽

Biological Properties ◽

Scavenging Activity ◽

Reducing Power Assay

The foods from plants were known to ensure against degenerative diseases and maturing because of their antioxidant activitycredited to their high content. Information on antioxidant activity of Indian medicinal plant is abundant. To the best of our knowledge, biological properties have not been accounted in the literature for this species of . As a point, this is the first results to assess the anti-oxidant activity of the plant which belongs to the family . The antioxidant activity of Methanol, , Ethyl acetate and Aqueous extracts of E. was determined using the DPPH free radical scavenging activity, ABTS radical scavenging activity and reducing power assay. The DPPH scavenging activity showed higher activity observed in extract (63%) of E. than (54%), (44%) and aqueous (30%). the ABTS assay inhibition in extract (58%) than (43%), (38%) and aqueous (32%) extracts. The reducing power assay of different extracts was increased in extract (54%) than (40%), (34%) and aqueous (28%) extracts. Overall, the and ethyl acetate extract had higher antioxidant properties than other extract. However, in this study, extracts exhibit great potential for antioxidant activity and may be useful for their nutritional and medicinal functions.

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Synthesis, Molecular Docking and Biological Properties of Novel Thiazolo[4,5-b]pyridine Derivatives

Acta Chimica Slovenica ◽

10.17344/acsi.2019.5439 ◽

2020 ◽

Vol 67 (4) ◽

pp. 1035-1043

Author(s):

Taras I. Chaban ◽

Yulia E. Matiichuk ◽

Olga Ya. Shyyka ◽

Ihor G. Chaban ◽

Volodymyr V. Ogurtsov ◽

...

Keyword(s):

Molecular Docking ◽

Antioxidant Properties ◽

Biological Properties ◽

Pharmacological Profile ◽

Scavenging Effect ◽

Rat Paw Edema ◽

Anti Inflammatory ◽

Rat Paw ◽

Inflammatory Action

The synthesis, anti-inflammatory and antioxidant properties of novel 5-hydroxy-7-methyl-3H-thiazolo[4,5-b]pyridin-2-one derivatives were discussed. Fused thiazolo[4,5-b]pyridin-2-ones were synthesized and modified at the N3, C5 and C6 positions of the main core in order to obtain the compounds with a satisfactory pharmacological profile. The synthesized compounds were preselected via molecular docking for further testing of their anti-inflammatory activity in vitro. Evaluation of novel compounds over the carageenin induced rat paw edema revealed strong anti-inflammatory action of some compounds including (thiazolo[4,5-b]pyridin-3(2H)-yl) propanenitrile (5) and thiazolo[4,5-b]pyridin-3(2H)-yl) propanoic acid (6) even exceeding the standard – Ibuprofen. The antioxidant activity of the synthesized compounds was measured in vitro by the method of scavenging effect on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals.

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Resazurin Method for Evaluation of Bioactive Compounds from Cranberry Extracts Using the Metabolic Activity of a ΔSOD1 Mutant of Saccharomyces cerevisiae Yeast Under Severe Osmotic Stress

Journal of AOAC International ◽

10.5740/jaoacint.19-0264 ◽

2020 ◽

Vol 103 (2) ◽

pp. 422-427

Author(s):

Agata Święciło ◽

Kamila Rybczyńska-Tkaczyk

Keyword(s):

Saccharomyces Cerevisiae ◽

Growth Parameters ◽

Raw Materials ◽

Antioxidant Properties ◽

Biological Properties ◽

Biologically Active ◽

Antioxidant Compounds ◽

Alcohol Water

Abstract Background: In addition to nutrients, plant raw materials for food production should also contain substances with beneficial biological properties, which unquestionably include antioxidant compounds. Among the numerous methods of determining the antioxidant properties of samples of plant material, biological methods that provide information about not only the in vivo antioxidant potential of samples but also their metabolism and bioavailability are increasingly valued. Objective: The aim of the study was to assess the antioxidant properties of extracts from large cranberry (Vaccinium macrocarpon) obtained from different producers. Methods: Biologically active compounds were extracted from cranberry fruits using water alone and ethyl alcohol–water in proportions of 1+1 and 4+1 (v/v) as solvents. The following were determined in the extracts: content of phenolic compounds and anthocyanins, total antioxidant capacity based on reduction of the ABTS+• [2,20-azino-bis (3-ethylbenzothiazoline-6-sulphonic acid)] radical cation, and antioxidant properties as reflected by the growth of a Saccharomyces cerevisiae Δsod1 mutant in a liquid hypertonic environment. The growth parameters of this Δsod1 mutant, monitored by a method exploiting a color reaction with resazurin, reflected the antioxidant properties of the extracts. Results: The ethanol–water cranberry extracts showed higher content of polyphenols, anthocyanins, and total antioxidants expressed as Trolox equivalent, determined on the basis of ABTS+• reduction. Conclusions: The antioxidant properties determined by the bioassay did not respond strongly to the data obtained in the in vitro chemical and biochemical assays, because they were more closely associated with the batch of fruit than with the type of solvent used to extract phytochemicals.

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FORMULATION AND EVALUATION OF TRANSDERMAL PATCHES OF METOPROLOL TARTRATE USING PERMEATION ENHANCERS OF NATURAL AND SYNTHETIC ORIGIN

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i5.32759 ◽

2019 ◽

pp. 317-323

Author(s):

SHIKHA BAGHEL CHAUHAN ◽

SUSHILA SAINI

Keyword(s):

Moisture Absorption ◽

Skin Permeation ◽

Penetration Enhancers ◽

Moisture Loss ◽

Metoprolol Tartrate ◽

Peg 400 ◽

Transdermal Patches ◽

Weight Variation ◽

Basil Oil

Objective: Oral metoprolol tartrate has a short elimination half-life (2-3h) and low bioavailability undergoes extensive first-pass metabolism and frequent dosing. The aim of the present investigation was to formulate, develop and evaluate metoprolol tartrate transdermal patches using various synthetic and natural penetration enhancers. Methods: Enhancers used were eugenol, limonene, basil oil, urea and SLS (sodium lauryl sulphate). Polymer used was chitosan and PEG 400 used as a plasticizer. Transdermal Films were prepared by using solvent casting method. FTIR and DSC were studied to assess any interaction between the drug and polymers. Films were evaluated for Physico-chemical Characteristics like thickness, weight variation, folding endurance, moisture loss, moisture absorption and drug content. In vitro skin permeation studies were performed using Keshary chien cell For 24 h across rat skin. Results: Chitosan was found to be a suitable polymer for matrix formation. 3.5% w/w was used to optimize to formulate transdermal patches. 1.5% of total solution v/v lactic acid was used for dissolution of chitosan. 2.5%v/v of total solution PEG 400 was used to provide plasticity and smoothness to the patches. From the evaluation of patches formulation, F10 containing Basil oil as penetration enhancer in the concentration of 1.5% v/v was found to be best among all batches because of its consistent release rate For 24 h and extent of drug release was 85.20%. It can be concluded that naturally occurring volatile oils i.e., terpenes appear acceptable permeation enhancer and shows the best permeation across skin as indicated by high percutaneous enhancement ability. Conclusion: The developed transdermal patches are stable, non-irritating, and had increased efficacy of metoprolol and therefore had a good potential for hypertension treatment.

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Phytochemical Characterization and Biological Evaluation of the Aqueous and Supercritical Fluid Extracts from Salvia sclareoides Brot

Open Chemistry ◽

10.1515/chem-2017-0011 ◽

2017 ◽

Vol 15 (1) ◽

pp. 82-91

Author(s):

Daniela Batista ◽

Pedro L. Falé ◽

Maria L. Serralheiro ◽

Maria-Eduarda Araújo ◽

Catarina Dias ◽

...

Keyword(s):

Linoleic Acid ◽

Supercritical Fluid ◽

Antioxidant Properties ◽

Biological Properties ◽

Biological Evaluation ◽

Cyclooxygenase 1 ◽

Wide Range ◽

Anti Inflammatory ◽

Β Carotene

AbstractPlants belonging to the genus Salvia (Lamiaceae) are known to have a wide range of biological properties. In this work, extracts obtained from the aerial parts of Salvia sclareoides Brot. were evaluated to investigate their chemical composition, toxicity, bioactivity, and stability under in vitro gastrointestinal conditions. The composition of the supercritical fluid extract was determined by GC and GC-MS, while the identification of the infusion constituents was performed by HPLC-DAD and LC-MS. The in vitro cytotoxicity of both extracts (0-2 mg/mL) was evaluated in Caco-2 cell lines by the MTT assay. The anti-inflammatory and anticholinesterase activities were determined through the inhibition of cyclooxygenase-1 and acetylcholinesterase enzymes, while β-carotene/linoleic acid bleaching test and the DPPH assays were used to evaluate the antioxidant activity. The infusion inhibited cyclooxygenase-1 (IC50 = 271.0 μg/mL), and acetylcholinesterase (IC50 = 487.7 μg/ mL) enzymes, also demonstrated significant antioxidant properties, as evaluated by the DPPH (IC50 = 10.4 μg/mL) and β-carotene/linoleic acid (IC50 = 30.0 μg/mL) assays. No remarkable alterations in the composition or in the bioactivities of the infusion were observed after in vitro digestion, which supports the potential of S. sclareoides as a source of bioactive ingredients with neuroprotective, anti-inflammatory and antioxidant properties.

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Evaluation of Skin Permeation and Analgesic Activity Effects of Carbopol Lornoxicam Topical Gels Containing Penetration Enhancer

The Scientific World JOURNAL ◽

10.1155/2014/127495 ◽

2014 ◽

Vol 2014 ◽

pp. 1-9 ◽

Cited By ~ 17

Author(s):

Saleh A. Al-Suwayeh ◽

Ehab I. Taha ◽

Fahad M. Al-Qahtani ◽

Mahrous O. Ahmed ◽

Mohamed M. Badran

Keyword(s):

Analgesic Activity ◽

Skin Permeation ◽

Tween 80 ◽

Skin Penetration ◽

Penetration Enhancers ◽

Topical Gel ◽

Carbopol Gel ◽

Franz Diffusion Cells ◽

Gel Formulations

The current study was designed to develop a topical gel formulation for improved skin penetration of lornoxicam (LOR) for enhancement of its analgesic activity. Moreover, the effect of different penetration enhancers on LOR was studied. The LOR gel formulations were prepared by using hydroxylpropyl methylcellulose (HPMC) and carbopol. The carbopol gels in presence of propylene glycol (PG) and ethanol were developed. The formulated gels were characterized for pH, viscosity, and LOR release using Franz diffusion cells. Also,in vitroskin permeation of LOR was conducted. The effect of hydroxypropylβ-cyclodextrin (HPβ-CD), beta-cyclodextrin (β-CD), Tween 80, and oleic acid on LOR permeation was evaluated. The optimized LOR gel formulation (LORF8) showed the highest flux (14.31 μg/cm2/h) with ER of 18.34 when compared to LORF3. Incorporation of PG and HPβ-CD in gel formulation (LORF8) enhanced the permeation of LOR significantly. It was observed that LORF3 and LORF8 show similar analgesic activity compared to marketed LOR injection (Xefo). This work shows that LOR can be formulated into carbopol gel in presence of PG and HPβ-CD and may be promising in enhancing permeation.

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Influence of different penetration enhancers on in vitro skin permeation and in vivo photoprotective effect of flavonoids

International Journal of Pharmaceutics ◽

10.1016/s0378-5173(98)00259-2 ◽

1998 ◽

Vol 175 (1) ◽

pp. 85-94 ◽

Cited By ~ 75

Author(s):

Antonella Saija ◽

Antonio Tomaino ◽

Domenico Trombetta ◽

Marcella Giacchi ◽

Anna De Pasquale ◽

...

Keyword(s):

Skin Permeation ◽

Penetration Enhancers ◽

In Vitro Skin Permeation

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Innovative Eco-Friendly Hydrogel Film for Berberine Delivery in Skin Applications

Molecules ◽

10.3390/molecules26164901 ◽

2021 ◽

Vol 26 (16) ◽

pp. 4901

Author(s):

Stefania Cometa ◽

Maria Addolorata Bonifacio ◽

Caterina Licini ◽

Annalisa Bellissimo ◽

Loris Pinto ◽

...

Keyword(s):

Skin Permeation ◽

Healing Process ◽

Antioxidant Properties ◽

Biological Assessment ◽

New Class ◽

New Frontier ◽

Biodegradable Hydrogel ◽

Speed Up ◽

Hydrogel Films

Hydrogel formulations (masks or patches, without tissue support) represent the new frontier for customizable skin beauty and health. The employment of these materials is becoming popular in wound dressing, to speed up the healing process while protecting the affected area, as well as to provide a moisturizing reservoir, control the inflammatory process and the onset of bacterial development. Most of these hydrogels are acrylic-based at present, not biodegradable and potentially toxic, due to acrylic monomers residues. In this work, we selected a new class of cellulose-derived and biodegradable hydrogel films to incorporate and convey an active compound for dermatological issues. Films were obtained from a combination of different polysaccharides and clays, and berberine hydrochloride, a polyphenolic molecule showing anti-inflammatory, immunomodulatory, antibacterial and antioxidant properties, was chosen and then embedded in the hydrogel films. These innovative hydrogel-based systems were characterized in terms of water uptake profile, in vitro cytocompatibility and skin permeation kinetics by Franz diffusion cell. Berberine permeation fitted well to Korsmeyer–Peppas kinetic model and achieved a release higher than 100 µg/cm2 within 24 h. The latter study, exploiting a reliable skin model membrane, together with the biological assessment, gained insights into the most promising formulation for future investigations.

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