Physicochemical Characterization and Antinociceptive Effect of β-cyclodextrin/Lippia pedunculosa Essential Oil in Mice

2018 ◽  
Vol 18 (9) ◽  
pp. 797-807 ◽  
Author(s):  
Paula dos Passos Menezes ◽  
Francielly de Oliveira Araujo ◽  
Tatianny Araujo Andrade ◽  
Igor Araujo Santos Trindade ◽  
Heitor Gomes de Araujo-Filho ◽  
...  
Keyword(s):  
Essential Oil ◽  
Physicochemical Properties ◽  
Water Solubility ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Antinociceptive Effect ◽  
Physicochemical Characterization ◽  
Good Tool ◽  
Main Challenge ◽  
Higher Temperature

Background: Some research studies have shown that Lippia pedunculosa essential oil (EOLP) has interesting biological activities. However, its low water solubility is the main challenge to achieve its therapeutic potential. In this context, Cyclodextrins (CDs) have been widely used in order to overcome this problem due to your capability to improve the physicochemical properties of drugs. Objective: In this perspective, the main goal of this study was to investigate how the improvement of the physicochemical properties of inclusion complexes (EOLP and β-CD) enhance the antinociceptive effect in mice. Methods: To achieve that, we prepared samples by Physical Mixture (PM), Paste Complexation (PC) and Slurry Complexation (SC) methods, followed by their physicochemical characterization. In addition, it was evaluated if the use of β-CD enhances the antinociceptive effect of EOLP in mice. Results: The analysis showed that rotundifolone (72.02%) was the major compound of EOLP and we found out based on DSC results that β-CD protected it from oxidation. In addition, TG techniques demonstrated that the best inclusion methods were PC and SC, due to their greater weight loss (10.8 and 11.6%, respectively) in the second stage (171-312°C), indicating that more complexed oil was released at the higher temperature than oil free. Other characteristics, such as changes in the typical crystalline form, and reduced particle size were observed by SEM and laser diffraction, respectively. The SC was the most effective complexation method, once the presence of rotundifolone was detected by FTIR. Based on that, SC method was used in all mice tests. In this regard, the number of paw licks was reduced for both compounds (all doses), but EOLP was more effective in reducing the nociceptive behavior. Conclusion: Therefore, CDs seem not to be a good tool to enhance the pharmacological properties of EOs rich in peroxide compounds such as rotundifolone.

scholarly journals Ellagic Acid ameliorates Streptozotocin-Induced Diabetic Hyperalgesia in Rat: Involvement of Oxidative Stress

2021 ◽  
Author(s):  
Siamak Shahidi ◽  
◽  
Alireza Komaki ◽  
Safoura Raoufi ◽  
Iraj Salehi ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Ellagic Acid ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Antinociceptive Effect ◽  
Diabetic Rats ◽  
Diabetic Rat ◽  
Tail Flick ◽  
Stress Markers ◽  
Total Antioxidant

Background/Aim: Hyperalgesia is one of the current complications of diabetes mellitus that Oxidative stress and inflammation have principal role in its development. Ellagic Acid (EA) as a herbal component, has some biological activities, including antioxidant and anti-inflammatory effects. This study was designed to evaluate the possible beneficial effect of EA on hyperalgesia in streptozotocin (STZ)-induced diabetic rat. Materials and Methods: Rats were divided into control(vehicle received), diabetic, EA (25, 50 mg/kg)-treated control and EA(25, 50 mg/kg)-treated diabetic groups. Diabetes was induced by a single intraperitoneal (IP) injection of streptozotocin (STZ) (60 mg/Kg). EA was administered daily by oral gavage for 4 weeks. Hyperalgesia was assessed using tail flick (TF) and hot plate (HP) tests. Also, oxidative stress markers including malondialdehyde (MDA), total oxidant status (TOS) and total antioxidant capacity (TAC) in the serum were evaluated. Results: Diabetic animals showed marked reductions in TF and HP latencies, elevation of serum MDA level and TOS and diminution of serum TAC compared to controls significantly. Treatment of Diabetic rats with EA ameliorated reduction of TF latency at the dose of 25 mg/kg and HP latency at the dose of 50 mg/kg. Furthermore EA significantly increased TAC and decreased MDA level at dose of 50 mg/kg and reduced TOS at both doses in the serum of diabetic animals. In EA treated normal rats we could see no significant alterations in the parameters studied. Conclusion: These results displayed potent antinociceptive effect of EA in diabetic rats via attenuating oxidative stress. This proposes therapeutic potential of EA for damping diabetic hyperalgesia.

scholarly journals Formulation and Evaluation of Guggul Lipid Nanovesicles for Transdermal Delivery of Aceclofenac

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Praveen Kumar Gaur ◽  
Shikha Mishra ◽  
Vidhu Aeri
Keyword(s):  
Physicochemical Properties ◽  
Water Solubility ◽  
Skin Permeation ◽  
Stability Study ◽  
New Drugs ◽  
Systemic Absorption ◽  
Accelerated Stability ◽  
Planar Molecule ◽  
Higher Temperature ◽  
Dicetyl Phosphate

Context. Most new drugs have low water solubility and liposome is an important formulation to administer such drugs; however, it is quite unstable and has negligible systemic absorption.Objective. Aceclofenac nanovesicles were made using guggul lipid for formulating stable transdermal formulation.Materials and Methods. Guggul lipid was formulated into vesicles along with cholesterol and dicetyl phosphate using film hydration method. The formulations were analyzed for physicochemical properties and stability. Then its skin permeation and anti-inflammatory activity were determined.Results. Both categories of vesicles (PC and GL) showed optimum physicochemical properties; however, accelerated stability study showed considerable differences. GL-1 was appreciably stable for over 6 months at 4°C. Corresponding gels (PCG-1 and GLG-1) showedCmaxvalues at 4.98 and 7.32 μg/mL along with theTmaxvalues at 4 and 8 hours, respectively. GLG-1 inhibited edema production by 90.81% in 6 hours.Discussion. PC liposomes are unstable at higher temperature and upon longer storage. The formulation with higher lipid content (GL-1) showed good drug retention after 24 hours and appreciable stability both at higher temperature and for longer duration. Guggul lipid being a planar molecule might be stacked in vesicle wall with cholesterol.Conclusion. The composition of the nanovesicle played an important role in stability and drug permeation. Guggul lipid is suitable for producing stable vesicles.

scholarly journals Preparation and Physicochemical Characterization of Water-Soluble Pyrazole-Based Nanoparticles by Dendrimer Encapsulation of an Insoluble Bioactive Pyrazole Derivative

Nanomaterials ◽  
2021 ◽  
Vol 11 (10) ◽  
pp. 2662
Author(s):  
Silvana Alfei ◽  
Chiara Brullo ◽  
Debora Caviglia ◽  
Guendalina Zuccari
Keyword(s):  
Clinical Application ◽  
Antimicrobial Agents ◽  
Water Solubility ◽  
Biological Activities ◽  
Drug Loading ◽  
Physicochemical Characterization ◽  
Water Soluble ◽  
First Order Kinetics ◽  
Physical Entrapment ◽  
Nano Formulation

2-(4-Bromo-3,5-diphenyl-pyrazol-1-yl)-ethanol (BBB4) was synthetized and successfully evaluated concerning numerous biological activities, except for antimicrobial and cytotoxic effects. Due to the antimicrobial effects possessed by pyrazole nucleus, which have been widely reported, and the worldwide need for new antimicrobial agents, we thought it would be interesting to test BBB4 and to evaluate its possible antibacterial effects. Nevertheless, since it is water-insoluble, the future clinical application of BBB4 will remain utopic unless water-soluble BBB4 formulations are developed. To this end, before implementing biological evaluations, BBB4 was herein re-synthetized and characterized, and a new water-soluble BBB4-based nano-formulation was developed by its physical entrapment in a biodegradable non-cytotoxic cationic dendrimer (G4K), without recovering harmful solvents as DMSO or surfactants. The obtained BBB4 nanoparticles (BBB4-G4K NPs) showed good drug loading (DL%), satisfying encapsulation efficiency (EE%), and a biphasic quantitative release profile governed by first-order kinetics after 24 h. Additionally, BBB4-G4K was characterized by ATR-FTIR spectroscopy, NMR, SEM, dynamic light scattering analysis (DLS), and potentiometric titration experiments. While, before the nanotechnological manipulation, BBB4 was completely water-insoluble, in the form of BBB4-G4K NPs, its water-solubility resulted in being 105-fold higher than that of the pristine form, thus establishing the feasibility of its clinical application.

Physicochemical Characterization of the Inclusion Complex of Diosmetin with Hydroxypropyl-β-Cyclodextrin

2013 ◽  
Vol 295-298 ◽  
pp. 298-302
Author(s):  
Yan Zhang ◽  
Korbanjhon Brad
Keyword(s):  
Differential Scanning Calorimetry ◽  
Inclusion Complex ◽  
Physicochemical Properties ◽  
Water Solubility ◽  
Physicochemical Characterization ◽  
Infrared Spectrometry ◽  
Scanning Calorimetry ◽  
Covalent Bonds ◽  
X Ray

In this study, the inclusion complex of diosmetin with hydroxypropyl-β- -cyclodextrin (HP-β-CD) was prepared to improve the water solubility of diosmetin by the solvent method. The content of diosmetin in the complex was determined by UV. And the physicochemical properties of the complex were analyzed by ultraviolet-visible spectrometry (UV), infrared spectrometry (IR), X-ray diffractometry (XRD), differential scanning calorimetry (DSC). The results showed that the physical phase of diosmetin had been changed. It was completely dispersed in HP-β-CD. HP-β-CD and diosmetin were combined by non-covalent bonds.

scholarly journals Identification of Mutations Conferring Tryptanthrin Resistance to Mycobacterium smegmatis

Antibiotics ◽  
2020 ◽  
Vol 10 (1) ◽  
pp. 6
Author(s):  
Svetlana G. Frolova ◽  
Ksenia M. Klimina ◽  
Ravinder Kumar ◽  
Aleksey A. Vatlin ◽  
Deepak B. Salunke ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Transcriptional Regulator ◽  
Test System ◽  
Comparative Genomic ◽  
Promising Alternative ◽  
Main Challenge

Tuberculosis (TB), caused by Mycobacterium tuberculosis, is a global burden, responsible for over 1 million deaths annually. The emergence and spread of drug-resistant M. tuberculosis strains (MDR-, XDR- and TDR-TB) is the main challenge in global TB-control, requiring the development of novel drugs acting on new biotargets, thus able to overcome the drug-resistance. Tryptanthrin is a natural alkaloid, with great therapeutic potential due to its simple way of synthesis and wide spectrum of biological activities including high bactericidal activity on both drug-susceptible and MDR M. tuberculosis strains. InhA was suggested as the target of tryptanthrins by in silico modeling, making it a promising alternative to isoniazid, able to overcome drug resistance provided by katG mutations. However, neither the mechanism of action of tryptanthrin nor the mechanism of resistance to tryptanthrins was ever confirmed in vitro. We show that the MmpS5-MmpL5 efflux system is able to provide resistance to tryptanthrins using an in-house test-system. Comparative genomic analysis of spontaneous tryptanthrin-resistant M. smegmatis mutants showed that mutations in MSMEG_1963 (EmbR transcriptional regulator) lead to a high-level resistance, while those in MSMEG_5597 (TetR transcriptional regulator) to a low-level one. Mutations in an MFS transporter gene (MSMEG_4427) were also observed, which might be involved in providing a basal level of tryptanthrins-resistance.

scholarly journals Phytochemistry and therapeutic potential of black pepper [Piper nigrum (L.)] essential oil and piperine: a review

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Kaliyaperumal Ashokkumar ◽  
Muthusamy Murugan ◽  
M. K. Dhanya ◽  
Arjun Pandian ◽  
Thomas D. Warkentin
Keyword(s):  
Animal Models ◽  
Essential Oil ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Biological Effects ◽  
Chemical Constituents ◽  
Black Pepper ◽  
Piper Nigrum ◽  
Bioactive Constituents ◽  
Intermittent Fever

Abstract Background Black pepper [Piper nigrum (L.), Family: Piperaceae] is used traditionally for the treatment of various diseases including; cough, cold, dyspnea throat diseases, intermittent fever, dysentery, stomachache, worms and piles. The pharmacological potential of black pepper is due to the presence of metabolites like phenolic compounds, alkaloids, flavonoids, carotenoids, terpenoids, etc. The multipurpose use of black pepper dried seeds has several other beneficial health effects that also received in the light of traditional as well as current medicine perspectives. The review aims to discuss the botany, phytochemical constituents, and pharmacological properties of piperine and black pepper essential oil (BPEO). Results Phytochemical analyses have described the main chemical constituents of black pepper, including carbohydrates, proteins, calcium, magnesium, potassium, iron, vitamin C, tannins, flavonoids and carotenoids. The volatile oil content ranges from 0.4 to 7 % in dried berries. The major constituents of BPEO are sabinene, 3-carene, D-limonene, α-pinene, caryophyllene, β-phellandrene, α-phellandrene, α-thujene, and β-bisabolene. Additionally, piperine is the naturally occurring and principal bioactive alkaloid constituent of black pepper owing to its potential therapeutic properties, including cerebral brain functioning and increased nutrient absorption. The BPEO has several biological roles, including antioxidant, anti-inflammatory, anticancer, anti-obesity, antidepressant, antidiabetic, antimicrobial, gastroprotective, and insecticidal activities. Conclusions This review examines and presents the appropriate evidence on black pepper and its traditional uses as well as biological activities of BPEO and piperine. Although several previous reports showed diverse biological effects for piperine and bioactive constitutes of BPEO. Thus, minimal investigations were conducted using animal models, and many of these studies also lacked appropriate experimental setting like doses, control details. Hence, future studies are necessary to understand the mechanism of piperine, BPEO, bioactive constituents and their effects upon their use by animal models and humans with the proper experimental procedure which we can facilitate the protection of human health from several diseases.

Therapeutic Potential of Melaleuca alternifolia Essential Oil in New Drug Delivery Systems

2020 ◽  
Vol 26 (33) ◽  
pp. 4048-4055 ◽  
Author(s):  
Karoll M. A. de Assis ◽  
Renaly I. de A. Rêgo ◽  
Demis F. de Melo ◽  
Laryssa M. da Silva ◽  
João A. Oshiro- Júnior ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Essential Oil ◽  
Drug Delivery Systems ◽  
Therapeutic Potential ◽  
Biological Activities ◽  
Delivery Systems ◽  
Tea Tree ◽  
New Drug ◽  
Anti Inflammatory ◽  
Therapeutic Alternatives

Medicinal plants produce secondary metabolites with special biological activities, which may be used as new therapeutic alternatives. For instance, tea tree essential oil (TTO) was shown to exert antimicrobial, antifungal, anthelmintic, antiviral, anti-tumor and anti-inflammatory activities. Due to their thermal instability, active principles can be easily degraded by physicochemical processes; therefore, they must be protected to increase their time of action and improve their controlled release. The aim of this review is to discuss formulations incorporating encapsulated TTO as the active ingredient. Micro and nanoencapsulated systems proved to be more thermostable than TTO and to exert better antimicrobial, antifungal, antiparasitic and larvicidal effects. Nanoencapsulation also reduced oil toxicity. Emulsified and hybrid systems developed by various methods showed improved repellent, antibacterial, antifungal and anti-inflammatory activities, thereby proving promising for the pharmaceutical industry. Liposomal formulations produced by hydration of lipid films exhibited constant rate of terpinen-4-ol release. In addition, their incorporation into biomaterials, such as sponges, nanofibers and films, showed great potential for treating infections. Mainly due to the advantages of their incorporation into new drug delivery systems over conventional formulations, there is an interest in the development of systems containing TTO as a pharmaceutical ingredient of plant origin.

scholarly journals Evaluation of physicochemical properties and dissolution studies on quality control of low water solubility drugs (raw materials and pharmaceutical formulations)

2020 ◽  
Vol 49 (2) ◽  
Author(s):  
Matheus Da Silva Ferreira ◽  
Gilmar Antônio De Carvalho Teles Júnior ◽  
Carlos Magno Ramos Carvalho Júnior ◽  
Fernanda De Souza Dias ◽  
Wilson Saback Dias dos Santos Júnior ◽  
...  
Keyword(s):  
Quality Control ◽  
Physicochemical Properties ◽  
Water Solubility ◽  
Raw Materials ◽  
Physicochemical Characterization ◽  
Pharmaceutical Formulations ◽  
Quality Parameters ◽  
Drug Dissolution ◽  
Reference Drug ◽  
Dissolution Studies

The purpose of this study was to evaluate physicochemical properties and dissolution studies of furosemide (FUR), hydrochlorothiazide (HCTZ) and nifedipine (NIF), low water solubility drugs, in raw materials and pharmaceutical formulations. Surface and physicochemical characterization techniques -scanning electronic microscopy (SEM), thermogravimetry (TG), X-ray diffraction (XRD) and infrared (IR) spectrometry- as well as physical and physicochemical tests on tablets and capsules were applied as supporting information on drug quality control. Simple, rapid, and efficient UV-Vis methods were developed and validated for the determination of FUR, HCTZ and NIF samples. SEM exhibited considerable differences in the crystal morphological structures. Among the drugs studied, except for furosemide, more than one polymorph was present in the samples. Drug release profiles were satisfactory for all products. FUR and HCTZ tablets exhibited similar dissolution profiles, with very rapid release to the pharmaceutical specialties (reference, similar and generic). For HCTZ tablets, the similar drug (f2= 48.74) is not equivalent to the reference drug. NIF capsules (reference and compounded) showed a release ≥80% of stated on product labels, in 10 minutes. The results obtained in this study suggest that the quality parameters and drug dissolution profiles may have been influenced by the morphology and size of the crystals, excipients, and technological processes.

scholarly journals In-silico ADMET Pharmacoinformatics of Geraniol (3,7-dimethylocta-trans-2,6-dien-1-ol) - acyclic monoterpene alcohol drug from Leaf Essential Oil of Cymbopogon martinii from Sirumalai Hills (Eastern Ghats), INDIA

2021 ◽  
Vol 11 (4-S) ◽  
pp. 109-118
Author(s):  
C. Kandeepan ◽  
R.V. Kalaimathi ◽  
A. Jeevalatha ◽  
A. N. Basha ◽  
S. Ramya ◽  
...  
Keyword(s):  
Essential Oil ◽  
In Silico ◽  
Water Solubility ◽  
Biological Activities ◽  
Control Agent ◽  
Eastern Ghats ◽  
Vascular Effects ◽  
Medicinal Uses ◽  
In Silico Admet ◽  
Cymbopogon Martinii

Cymbopogon martinii is a grass from genus Cymbopogon (lemongrasses) native to India, but widely cultivated in other places for its aromatic essential oil. C. martinii known as Palmarosa smells sweet with rose-like odor. Geraniol, a terpene alcohol present in Cymbopogon martinii essential oil (CMEO) is much valued for its typical aroma and medicinal uses. In addition to the pleasant odor, Geraniol is known for fungicidal, nematicidal, acaricidal, insecticidal, repellent properties hence, used as Natural Pest Control Agent (NPCA) exhibiting low toxicity. Furthermore, geraniol has been suggested to exemplify a new class of chemoprevention agents in the treatment of cancer. Biological activities such as antimicrobial, anti-oxidant, anti-inflammatory and vascular effects have been investigated. In the present study, GCMS based in-silico ADMET pharmacoinformatics aspects (Physicochemical, Lipophilicity, Medicinal Chemistry, Druglikeness, Absorption, Water Solubility, Distribution, Metabolism, Pharmacokinetics, Excretion, Environmental Toxicity, Tox21 Pathway and Toxicophore Rules) with PASS prediction of geraniol from CMEO has been bioprospected from human health perspective point of view. Keywords: GCMS; ADMET; Pharmacoinformatics; Geraniol; Essential Oil; Cymbopogon martinii; Palmarosa; CMEO; PBNPs; Sirumalai Hills; Eastern Ghats

Primordial science and pioneering approaches of guggul for chronic ailments – A modernized review

2020 ◽  
Vol 7 (2) ◽  
pp. 14-20
Author(s):  
Jamal Basha D ◽  
Kumar P R ◽  
Ranganayakulu D
Keyword(s):  
Water Solubility ◽  
Therapeutic Potential ◽  
Chemical Constituents ◽  
Signs And Symptoms ◽  
Dosage Forms ◽  
The Novel ◽  
Lipids Metabolism ◽  
Clinical Conditions ◽  
Novel Drug ◽  
Conventional Dosage

An oleo gum resin guggulu is a product which obtained as a result of gummosis from the bark of Commiphora wightii (Arnott) Bhandari [syn. Commiphoramukul (Hook. Ex Stocks) Family, Burseraceae]. It has been known for its immense applicability in the Ayurveda since time immemorial for the treatment of variety of disorders such as inflammation, gout, rheumatism, impotence, leprosy, obesity, and disorders of lipids metabolism. It is a mixture of phytoconstituents like terpenoids, steroids, flavonoids, guggultetrols, lignans, sugars, and amino acids. This review is an effort to compile all the information available on all of its chemical constituents which are responsible for its therapeutic potential, limitation of guggul extracts and the necessity of novel principles for gum guggul. Nowadays, Guggul is available as the marketed formulation for curing numerous clinical conditions and is accessible in combination with various other ingredients. Though conventional dosage form shows the dominance as patient compliance and easy availability, yet it has found to pose the problems like dose fluctuation, peak-valley effect, non-adjustment of the administered drug, invasiveness etc. Guggul lacks its desired effect due to its low bioavailability and water solubility. This makes it a partial or a deficient therapy for remedy of many signs and symptoms. Novel drug delivery system (NDDS), a new approach and has excluded many of drawbacks exhibited by conventional dosage forms. Some of the novel dosage forms of guggul has been formed like nanoparticles, nanovesicles, gugglusomes and proniosomal gel. But still, the novel formulations for guggul has its less outspread in the market. Guggul can be executed as a profitable drug using NDDS. There is a need to highlight the unidentified and unexplained facts about guggul so as to make it more efficacious and effective in terms of bioavailability and aqueous insolubility.

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