scholarly journals Enhancement of Antimicrobial and Antiproliferative Activities of Standardized Frankincense Extract Using Optimized Self-Nanoemulsifying Delivery System

2021 ◽  
Vol 89 (3) ◽  
pp. 36
Author(s):  
Shereen S. El-Mancy ◽  
Alaadin E. El-Haddad ◽  
Walaa A. Alshareef ◽  
Amr M. Saadeldeen ◽  
Soad Z. El-Emam ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Delivery System ◽  
Low Cost ◽  
In Vivo Studies ◽  
Major Constituent ◽  
Lattice Design ◽  
Natural Resin ◽  
Antiproliferative Activities

Boswellic acids (BAs) are the main bioactive compounds of frankincense, a natural resin obtained from the genus Boswellia. This study aimed to develop a self-nanoemulsifying delivery system (SNEDS) to improve the antimicrobial and antiproliferative activities of standardized frankincense extract (Fr-extract). Fr-extract was standardized, and BA content was quantified using the developed HPLC-UV method. Screening studies of excipients followed by formula optimization using a mixture simplex lattice design was employed. The optimized Fr-SENDS formulation was characterized. Furthermore, microbiological and antiproliferative assessments of the standardized Fr-extract and Fr-SNEDS were evaluated. Quantification demonstrated that the major constituent is 11-keto-boswellic acid (KBA) (16.25%) among BA content (44.96%). The optimized Fr-SENDS (composed of 5% CapryolTM 90, 48.7% Gelucire® 44/14 and 46.3% ethanol) showed spherical nanosized dispersions with DS, PDI, and zeta potential of 17.9 nm, 0.2, and −14.5 mV, respectively. Fr-SNEDS exhibited lower MIC and MBC values compared with Fr-extract against pathogens conjugated with lung cancer and was comparable to reference antimicrobials. Fr-SNEDS showed superior antiproliferative activity over Fr-extract, with IC50 values of 20.49 and 109.5 μg mL−1, respectively. In conclusion, the optimized Fr-SNEDS could be easily developed and manufactured at a low cost and the in vitro results support its use as a potential adjuvant oral therapy for lung cancer. Further in vivo studies could be continued to assess the therapeutic efficiency of the prepared system.

Novel Self-Micro Emulsifying Drug Delivery System for safe intra muscular delivery with improved pharmacodynamics and pharmacokinetics

2021 ◽  
Vol 18 ◽  
Author(s):  
Subheet Kumar Jain ◽  
Neha Panchal ◽  
Amrinder Singh ◽  
Shubham Thakur ◽  
Navid Reza Shahtaghi ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Inflammatory Diseases ◽  
Diclofenac Sodium ◽  
Physical Stability ◽  
In Vivo Studies ◽  
High Concentration

Background: Diclofenac sodium (DS) injection is widely used in the management of acute or chronic pain and inflammatory diseases. It incorporates 20 % w/v Transcutol-P as a solubilizer to make the stable injectable formulation. However, the use of Transcutol-P in high concentration leads to adverse effects such as severe nephrotoxicity, etc. Some advancements resulted in the formulation of an aqueous based injectable but that too used benzyl alcohol reported to be toxic for human use. Objective: To develop an injectable self-micro emulsifying drug delivery system (SMEDDS) as a novel carrier of DS for prompt release with better safety and efficacy. Methods: A solubility study was performed with different surfactants and co-surfactants. The conventional stirring method was employed for the formulation of SMEDDS. Detailed in vitro characterization was done for different quality control parameters. In vivo studies were performed using Wistar rats for pharmacokinetic evaluation, toxicological analysis, and analgesic activity. Results: The optimized formulation exhibited good physical stability, ideal globule size (156±0.4 nm), quick release, better therapeutics, and safety, increase in LD50 (221.9 mg/kg) to that of the commercial counterpart (109.9 mg/kg). Further, pre-treatment with optimized formulation reduced the carrageenan-induced rat paw oedema by 88±1.2 % after 4 h, compared to 77±1.6 % inhibition with commercial DS formulation. Moreover, optimized formulation significantly (p<0.05) inhibited the pain sensation in the acetic-acid induced writhing test in mice compared to its commercial equivalent with a better pharmacokinetic profile. Conclusion: The above findings confirmed that liquid SMEDDS could be a successful carrier for the safe and effective delivery of DS

scholarly journals STRUCTURE-BASED MULTITARGETED MOLECULAR DOCKING ANALYSIS OF PYRAZOLE-CONDENSED HETEROCYCLICS AGAINST LUNG CANCER

2021 ◽  
pp. 157-169
Author(s):  
JAINEY P. JAMES ◽  
AISWARYA T. C. ◽  
SNEH PRIYA ◽  
DIVYA JYOTHI ◽  
SHESHAGIRI R. DIXIT
Keyword(s):  
Lung Cancer ◽  
Molecular Docking ◽  
Binding Mode ◽  
Pharmacophore Modeling ◽  
In Vivo Studies ◽  
Spectral Studies ◽  
Pyrazole Derivatives ◽  
Anticancer Activities

Objective: The significant drawbacks of chemotherapy are that it destroys healthy cells, resulting in adverse effects. Hence, there is a need to adopt new techniques to develop cancer-specific chemicals that target the molecular pathways in a non-toxic fashion. This study aims to screen pyrazole-condensed heterocyclics for their anticancer activities and analyse their enzyme inhibitory potentials EGFR, ALK, VEGFR and TNKS receptors. Methods: The structures of the compounds were confirmed by IR, NMR and Mass spectral studies. The in silico techniques applied in this study were molecular docking and pharmacophore modeling to analyse the protein-ligand interactions, as they have a significant role in drug discovery. Drug-likeness properties were assessed by the Lipinski rule of five and ADMET properties. Anticancer activity was performed by in vitro MTT assay on lung cancer cell lines. Results: The results confirm that all the synthesised pyrazole derivatives interacted well with the selected targets showing docking scores above-5 kcal/mol. Pyrazole 2e interacted well with all the four lung cancer targets with its stable binding mode and was found to be potent as per the in vitro reports, followed by compounds 3d and 2d. Pharmacophore modeling exposed the responsible features responsible for the anticancer action. ADMET properties reported that all the compounds were found to have properties within the standard limit. The activity spectra of the pyrazoles predicted that pyrazolopyridines (2a-2e) are more effective against specific receptors such as EGFR, ALK and Tankyrase. Conclusion: Thus, this study suggests that the synthesised pyrazole derivatives can be further investigated to validate their enzyme inhibitory potentials by in vivo studies.

scholarly journals Power spectral density-based nearinfrared sub-band detection for noninvasive blood glucose prediction in both in-vitro and in-vivo studies

2018 ◽  
Vol 11 (06) ◽  
pp. 1850035
Author(s):  
Ibrahim Akkaya ◽  
Erman Selim ◽  
Mert Altintas ◽  
Mehmet Engin
Keyword(s):  
Blood Glucose ◽  
Spectral Density ◽  
Power Spectral Density ◽  
Optical System ◽  
Low Cost ◽  
Linear Regression Analysis ◽  
In Vivo Studies ◽  
Power Spectral

Diabetes is a widespread and serious disease and noninvasive measurement has been in high demand. To address this problem, a power spectral density-based method was offered for determining glucose sensitive sub-bands in the nearinfrared (NIR) spectrum. The experiments were conducted using phantoms of different optical properties in-vitro conditions. The optical bands 1200–1300[Formula: see text]nm and 2100–2200[Formula: see text]nm were found feasible for measuring blood glucose. After that, a photoplethysmography (PPG)-based low cost and portable optical system was designed. It has six different NIR wavelength LEDs for illumination and an InGaAs photodiode for detection. Optical density values were calculated through the system and used as independent variables for multiple linear regression analysis. The results of blood glucose levels for 24 known healthy subjects showed that the optical system prediction was nearly 80% in the A zone and 20% in the B zone according to the Clarke Error Grid analysis. It was shown that a promising easy-use, continuous, and compact optical system had been designed.

scholarly journals Effects of Resveratrol against Lung Cancer: In Vitro and In Vivo Studies

Nutrients ◽  
2017 ◽  
Vol 9 (11) ◽  
pp. 1231 ◽  
Author(s):  
Michael Yousef ◽  
Ioannis Vlachogiannis ◽  
Evangelia Tsiani
Keyword(s):  
Lung Cancer ◽  
In Vivo Studies

scholarly journals The Biological and Clinical Relevance of Inhibitor of Growth (ING) Genes in Non-Small Cell Lung Cancer

Cancers ◽  
2019 ◽  
Vol 11 (8) ◽  
pp. 1118 ◽  
Author(s):  
Elisabeth Smolle ◽  
Nicole Fink-Neuboeck ◽  
Joerg Lindenmann ◽  
Freyja Smolle-Juettner ◽  
Martin Pichler
Keyword(s):  
Lung Cancer ◽  
Family Members ◽  
In Vivo Studies ◽  
Action Mode ◽  
Inhibition Of Growth ◽  
Molecular Mechanism Of Action ◽  
Anchor Points ◽  
Lung Cancer Detection

Carcinogenic mutations allow cells to escape governing mechanisms that commonly inhibit uncontrolled cell proliferation and maintain tightly regulated homeostasis between cell death and survival. Members of the inhibition of growth (ING) family act as tumor suppressors, governing cell cycle, apoptosis and cellular senescence. The molecular mechanism of action of ING genes, as well as their anchor points in pathways commonly linked to malignant transformation of cells, have been studied with respect to a variety of cancer specimens. This review of the current literature focuses specifically on the action mode of ING family members in lung cancer. We have summarized data from in vitro and in vivo studies, highlighting the effects of varying levels of ING expression in cancer cells. Based on the increasing insight into the function of these proteins, the use of ING family members as clinically useful biomarkers for lung cancer detection and prognosis will probably become routine in everyday clinical practice.

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