scholarly journals The main stages of pharmaceutical development of emulgel “Probioskin”

2021 ◽  
pp. 75-84
Author(s):  
Alina Soloviova ◽  
Olha Kaliuzhnaia ◽  
Oksana Strilets ◽  
Dmytro Lytkin ◽  
Olga Goryacha
Keyword(s):  
Microbial Contamination ◽  
Study Drug ◽  
Central Research ◽  
Reference Drug ◽  
Pharmaceutical Development ◽  
Dermatological Diseases ◽  
Biological Studies ◽  
Pharmacological Studies ◽  
Complex Preparation ◽  
Anti Inflammatory

The aim. To conduct research on the pharmaceutical development of a complex preparation with probiotic “Probioskin” in the form of an emulgel for the treatment of infectious and inflammatory dermatological diseases. Methods. Uniformity was determined by visual inspection of the test samples using an XSP-128 ULAB biological microscope. The study of the rheological properties of the samples was carried out using a Rheolab QC rheovisosimeter (Anton Paar, Austria) using a system of coaxial cylinders C-CC27 / SS. Microbiological studies and biotesting on a biological model of ciliates were carried out in aseptic conditions of a laminar box (biological safety cabinet AC2-4E1 “Esco”, Indonesia) of the Department of Biotechnology of the National University of Pharmacy (completely). Pharmacological studies (determination of the parameters of acute toxicity and anti-inflammatory properties on the model of acute exudative inflammation of the foot in rats caused by zymosan and carrageenan) were carried out on the basis of the Central Research Laboratory of the NUPh. Results. On the basis of the complex of the carried out studies, the composition of the complex preparation for skin use “Probioskin” was substantiated. The analysis of the microbiological purity of the developed agent during the proposed shelf life of 12 months showed that the drug meets the requirements of the State Pharmacopoeia Monograph for cutaneous application in terms of the level of microbial contamination by foreign microflora. The complex of pharmacological studies carried out indicates that the drug “Probioskin” can be attributed to group 6 of class and classified as a “relatively harmless” agent. The study of the anti-inflammatory effect of the drug indicates that the drug exhibits moderate anti-inflammatory properties. Under the condition of zymosan inflammation, which is associated with the activation of leukotrienes as inflammatory mediators, the average antiexudative activity of the drug is 33 %. The drug has a moderate antiexudative effect under the condition of carrageenan edema, which is evidence of its effect on exudation processes mediated by prostaglandins. The mean AEA of the study drug was 24 %. Conclusions. For the development of a soft preparation for skin use for the treatment of infectious and inflammatory dermatological diseases, the following components have been selected: active – lactobacilli, dexpanthenol, lactic acid; auxiliary - propylene glycol, peach oil, polysorbate-80, aristophlex, tocopherol, the concentration of which was substantiated on the basis of a complex of organoleptic, physicochemical, pharmacological, microbiological and biological studies. It has been experimentally established that the “Probioskin” emulgel meets the requirements of the SPhU in terms of the level of microbial contamination by extraneous microflora. Pharmacological studies allow the drug to be classified as “relatively harmless” with anti-inflammatory properties at a level not lower than the reference drug

Nanotechnological Innovations Enhancing the Topical Therapeutic Efficacy of Quercetin: A Succinct Review

2020 ◽  
Vol 17 (4) ◽  
pp. 270-278
Author(s):  
Maha Nasr ◽  
Rawan Al-Karaki
Keyword(s):  
Side Effects ◽  
Therapeutic Efficacy ◽  
Skin Permeation ◽  
Skin Penetration ◽  
Topical Delivery ◽  
Natural Compounds ◽  
Therapeutic Activity ◽  
Dermatological Diseases ◽  
Anti Inflammatory ◽  
Topical Applications

Nanotechnology is currently a hot topic in dermatology and nutraceutical/cosmeceutical delivery, owing to the advantages it provides in terms of enhancing the skin permeation of drugs, as well as increasing their therapeutic efficacy in the treatment of different dermatological diseases. There is also a great interest in the topical delivery of nutraceuticals; which are natural compounds with both therapeutic and cosmetic benefits, in order to overcome the side effects of topically applied chemical drugs. Quercetin is a key nutraceutical with topical antioxidant and anti-inflammatory properties which was reported to be effective in the treatment of different dermatological diseases, however, its topical therapeutic activity is hindered by its poor skin penetration. This review highlights the topical applications of quercetin, and summarizes the nanocarrier-based solutions to its percutaneous delivery challenges.

scholarly journals The Anti-Inflammatory Effect of a γ-Lactone Isolated from Ostrich Oil of Struthio camelus (Ratite) and Its Formulated Nano-Emulsion in Formalin-Induced Paw Edema

Molecules ◽  
2021 ◽  
Vol 26 (12) ◽  
pp. 3701
Author(s):  
Salah E. M. Eltom ◽  
Ahmed A. H. Abdellatif ◽  
Hamzah Maswadeh ◽  
Mohsen S. Al-Omar ◽  
Atef A. Abdel-Hafez ◽  
...  
Keyword(s):  
Oral Administration ◽  
Standard Procedure ◽  
P Value ◽  
Skin Thickness ◽  
Paw Edema ◽  
Reference Drug ◽  
Struthio Camelus ◽  
Anti Inflammatory ◽  
Nano Emulsion ◽  
Inflammatory Effect

The ostrich oil of Struthio camelus (Ratite) found uses in folk medicine as an anti-inflammatory in eczema and contact dermatitis. The anti-inflammatory effect of a γ-lactone (5-hexyl-3H-furan-2-one) isolated from ostrich oil and its formulated nano-emulsion in formalin-induced paw edema was investigated in this study. Ostrich oil was saponified using a standard procedure; the aqueous residue was fractionated, purified, and characterized as γ-lactone (5-hexyl-3H-furan-2-one) through the interpretation of IR, NMR, and MS analyses. The γ-lactone was formulated as nano-emulsion using methylcellulose (MC) for oral solubilized form. The γ-lactone methylcellulose nanoparticles (γ-lactone-MC-NPs) were characterized for their size, shape, and encapsulation efficiency with a uniform size of 300 nm and 59.9% drug content. The γ-lactone was applied topically, while the formulated nanoparticles (NPs) were administered orally to rats. A non-steroidal anti-inflammatory drug (diclofenac gel) was used as a reference drug for topical use and ibuprofen suspension for oral administration. Edema was measured using the plethysmograph method. Both γ-lactone and γ-lactone-MC-NPs showed reduction of formalin-induced paw edema in rats and proved to be better than the reference drugs; diclofenac gel and ibuprofen emulsion. Histological examination of the skin tissue revealed increased skin thickness with subepidermal edema and mixed inflammatory cellular infiltration, which were significantly reduced by the γ-lactone compared to the positive control (p-value = 0.00013). Diuretic and toxicity studies of oral γ-lactone-MC-NPs were performed. No diuretic activity was observed. However, lethargy, drowsiness, and refusal to feeding observed may limit its oral administration.

Rare-earth complexes with anti-inflammatory drug sulindac: synthesis, characterization, spectroscopic and in vitro biological studies

2021 ◽  
pp. 120516
Author(s):  
Renan Barrach Guerra ◽  
Diogo Alves Gálico ◽  
Thais Fernanda de Campos Fraga-Silva ◽  
Julia Aguiar ◽  
James Venturini ◽  
...  
Keyword(s):  
Rare Earth ◽  
Rare Earth Complexes ◽  
Inflammatory Drug ◽  
Biological Studies ◽  
Anti Inflammatory

Ozone Therapy Alleviates Monosodium Urate Induced Acute Gouty Arthritis in Rats Through Inhibition of NLRP3 Inflammasome

2021 ◽  
Vol 16 ◽  
Author(s):  
Doaa M. Abdullah ◽  
Soad L. Kabil
Keyword(s):  
Gouty Arthritis ◽  
Antioxidant Defense System ◽  
Albino Rats ◽  
Monosodium Urate ◽  
Ozone Therapy ◽  
Reference Drug ◽  
Acute Gouty Arthritis ◽  
Beneficial Effects ◽  
Anti Inflammatory ◽  
Domain 3

Background: Gout is a metabolic disease strictly related to hyperuricemia. The associated intense inflammation and pain are triggered by the deposited monosodium urate crystals (MSU) in joints. The principal therapeutic strategies of gout involve the control of hyperuricemia and anti-inflammatory medications. Objectives: This study aimed to investigate the possible beneficial effects of ozone therapy, a well-known antioxidant, and an immunomodulation, on gouty arthritis and the underlying mechanisms. Methods : Acute gouty arthritis was induced in male albino rats via MSU crystals intra-articular injection in the ankle joint. The gouty arthritic rats received pre-treatment with ozone, colchicine (as a reference drug), or combination. Results : The obtained results of ozone therapy showed obvious reduction in the degree of ankle edematous swelling, pro-inflammatory cytokines, lipid peroxidation, the nucleotide binding oligomerization domain like receptor containing pyrin domain 3 (NLRP3), procaspase-1, caspase-1, interleukin-1β synovial tissue levels with enhancement of antioxidant defense system. Additionally, ozone therapy significantly attenuated the histological derangements in gouty arthritic rats. Conclusion : This study suggests that ozone is able to treat gouty arthritis and reducing synovial injury through an anti-inflammatory effect as well as antioxidant activity.

scholarly journals Antipyretic, Analgesic and Anti-inflammatory Activity of Qurs Afsanteen Saghir (A Polyherbal Unani Tablet) in Experimental Animals

2022 ◽  
Author(s):  
MD Maseehullah ◽  
Gulam Mohammed Husain ◽  
Mohammed Zakir ◽  
Mohd Kashif Husain ◽  
Ghazala Javed ◽  
...  
Keyword(s):  
Diclofenac Sodium ◽  
Study Drug ◽  
Prunus Dulcis ◽  
Inflammatory Activity ◽  
Apium Graveolens ◽  
Dependent Manner ◽  
Test Drug ◽  
Artemisia Absinthium ◽  
Hot Plate Test ◽  
Anti Inflammatory

Qurs Afsanteen Saghir is a polyherbal Unani formulation in the form of tablet. This formulation consists of multiple medicinal plants like Afsanteen (Artemisia absinthium L.), Badam Talkh (Prunus dulcis (Mill.) D.A.Webb), Asaroon (Asarum europaeum L.), Anisoon (Pimpinella anisum L.) and Tukhm-e-Karafs (Apium graveolens L.). The clinical adult dose of study drug is 3.5 –7 g per day as mentioned in Unani literature. The present study evaluated the antipyretic, analgesic and anti-inflammatory potential of Qurs Afsanteen Saghir using different animal models. Antipyretic activity was measured using yeast-induced pyrexia model in rats at 360 and 720 mg/kg bw dose of test drug and paracetamol (70 mg/kg bw p.o.) as standard control. Analgesic effect was evaluated using acetic acid-induced writhing test in mice using test drug at dose 720 and 1440 mg/kg bw and diclofenac sodium (15 mg/kg bw p.o.) as standard control. Eddy’s hot plate test was conducted in rats using test drug at the dose of 360 and 720 mg/kg bw and buprenorphine (0.10 mg/kg s.q.) as standard control. Anti-inflammatory activity was assessed by carrageenan-induced paw edema model in rats with the dose of 360 and 720 mg/kg of test drug and Indomethacin (10 mg/kg p.o.) as standard control. The study drug significantly reduced the temperature and pain at both dose levels in a time-dependent manner as compared to normal control. However, the reduction of inflammation was observed at low dose (360 mg/kg bw) only after 3 hours of carrageenan administration. These findings indicated that tested drug showed potential activity as antipyretic and analgesic; whereas the drug may not be considered quite effective as an anti-inflammatory agents.

scholarly journals Synthesis, Characterization and Acute Anti-inflammatory Evaluation of New Mefenamic Acid Derivatives Having 4-Thiazolidinone Nucleus

2019 ◽  
Vol 28 (1) ◽  
pp. 138-146
Author(s):  
Mustafa H. Ali Alsafi ◽  
Muthanna S. Farhan
Keyword(s):  
Side Effects ◽  
Mefenamic Acid ◽  
Paw Edema ◽  
Compound I ◽  
Reference Drug ◽  
Cox 2 ◽  
Anti Inflammatory ◽  
Derivatives Of ◽  
Cox 1 ◽  
Inflammatory Effect

Mefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug's potential side effects, new series of 4-thiazolidinone derivatives of mefenamic acid were synthesized IVa-g. The synthetic procedures for target compounds and their intermediates are designed to be as follows: acylation of secondary amine of mefenamic acid by chloroacetylchloride to produce compound (I), then reaction between compound (I) and hydrazine hydrate to form hydrazine derivative of mefenamic acid (compound II). After that, Schiff base formation by addition of seven benzaldehyde derivatives and finally, cyclization in presence of thioglycolic acid to form 4-thiazolidinone heterocyclic ring. The characterization of the titled compounds has been established on the basis of their spectral FTIR, 1HNMR data, and by measurements of their physical properties. In vivo acute anti-inflammatory effect of the synthesized compounds was evaluated in rats using egg-white induced edema model of inflammation. The tested compounds and the reference drug produced significant reduction of paw edema with respect to the effect of dimethyl sulfoxide 10%v/v (control group). Compound IVe showed more potent effect than mefenamic acid at 240-300 min, while at time 300 min, compounds IVa and IVd exhibit more potent anti-inflammatory effect than mefenamic acid (50mg/kg, i.p.) as they reduced paw edema significantly more than mefenamic acid at mentioned intervals (p<0.05) . On the other hand compound IVc exhibited lower anti-inflammatory effect.

scholarly journals Scientific Evaluation of anti-inflammatory potential of Macrotyloma uniflorum seeds extracts

2020 ◽  
Vol 11 (SPL4) ◽  
pp. 1883-1888
Author(s):  
Anandarajagopal K ◽  
Abdullah Khan ◽  
Sugalia S ◽  
Bama Menon ◽  
Tan Ching Siang ◽  
...  
Keyword(s):  
Antioxidant Properties ◽  
Water Extract ◽  
Ethanol Extract ◽  
Inflammatory Activity ◽  
Leguminous Plant ◽  
Paw Edema ◽  
Reference Drug ◽  
Macrotyloma Uniflorum ◽  
Phenolic Constituents ◽  
Anti Inflammatory

Phytochemicals possessing the antioxidant properties naturally present in food attract a greater interest to healthcare researchers due to their desirable health effects on human health as they can be explored for protection against oxidative deterioration. Macrtotyloma uniflorum is a leguminous plant belonging to the family Fabaceae and commonly known as Horse gram. Aqueous and ethanol extracts of seeds of Macrotyloma uniflorum were evaluated for their anti-inflammatory effects using the scientific protocol on experimental rats. Extraction was carried out using the cold maceration method, and the anti-inflammatory activity was evaluated using a digital plethysmometer in the experimental rats injected with carrageenan to produce paw edema. Preliminary phytochemical studies confirmed the presence of various bioactive compounds such as alkaloids, glycosides, carbohydrates, proteins and amino acids, terpenoids, tannins, and phenolic compounds in both extracts while flavonoids were found only in ethanol extract. Both extracts of M. uniflorum seeds (200 mg/ml) significantly (p<0.01) reduced the paw edema volume induced by carrageenan. The ethanol extract of M. uniflorum seeds exhibited more potent anti-inflammatory activity than water extract, that might be due to the presence of flavonoids in ethanol extract. The activity of the extracts was compared with diclofenac sodium (10mg/kg b.wt.) as a reference drug. From the results, it may be suggested that the antioxidative potential of phenolic constituents and flavonoids is the primary factors for the anti-inflammatory activity of M. uniflorum seeds extracts.

scholarly journals Acute Toxicity, Phytochemical Screening, Analgesic, and Anti-Inflammatory Activities of Aqueous and Methanol Root Extracts of Maerua triphylla A. Rich. (Capparaceae)

2021 ◽  
Vol 2021 ◽  
pp. 1-9
Author(s):  
Brian Muyukani Wangusi ◽  
Laetitia Wakonyu Kanja ◽  
Isaac Mpapuluu Ole-Mapenay ◽  
Jared Misonge Onyancha
Keyword(s):  
Acetic Acid ◽  
Diclofenac Sodium ◽  
Root Extract ◽  
Phytochemical Screening ◽  
Paw Edema ◽  
Reference Drug ◽  
Root Extracts ◽  
Significant Difference ◽  
Anti Inflammatory ◽  
Aqueous Root Extract

Maerua triphylla root extracts are used by Maasai and Kikuyu communities in Kenya to manage headaches, stomachaches, migraines, and rheumatism. However, scientific data on their safety and efficacy are limited. The current study aims to investigate the safety, phytochemical constituents, analgesic, and anti-inflammatory activities of M. triphylla root extracts. Aqueous and methanol M. triphylla root extracts were prepared by cold maceration, and the extracts’ safety was evaluated using Wistar rats according to the Organization for Economic Cooperation and Development (2008) guidelines. Standard qualitative phytochemical screening methods were used for the detection of various phytochemical groups in the extracts. Analgesic activity assay in Swiss albino mice was done using the acetic acid-induced writhing test, while anti-inflammatory activity was determined in Wistar rats using the acetic acid-induced paw edema method. The methanol and aqueous extracts revealed LD50 > 2000 mg/kg bw, classifying them as nontoxic. The presence of cardiac glycosides, flavonoids, alkaloids, and phenols was observed in both extracts. However, saponins were only present in the methanol extract. In the analgesic study, mice that received 100 mg/kg bw and 500 mg/kg bw of aqueous root extract of M. triphylla had significantly lower acetic acid-induced writhing than mice that received acetylsalicylic acid 75 mg (reference drug) ( p < 0.05 ). Additionally, mice that received 500 mg/kg bw of methanol root extract of M. triphylla had significantly lower acetic acid-induced writhing than mice that received the acetylsalicylic acid 75 mg ( p < 0.05 ). In the anti-inflammatory study, there was no significant difference ( p < 0.05 ) between the inhibitory activity of different doses of the aqueous root extract of M. triphylla and a 50 mg/kg dose of diclofenac sodium (reference drug) on acetic acid-induced paw edema in rats. Moreover, there was no significant difference in the inhibitory activity of 100 mg/kg bw and 500 mg/kg bw doses of the methanol root extract of M. triphylla and a 50 mg/kg dose of diclofenac sodium on acetic acid-induced paw edema ( p > 0.05 ). These findings suggest that the roots of M. triphylla may be useful in the safe mitigation of pain and inflammation and therefore support their ethnomedicinal use in the management of pain and inflammation.

scholarly journals Study to Investigate the anti-inflammatory effect of Codelac® Broncho with Thymus Serpyllum (elixir) in comparison with reference drug Fenspiride (syrup) using accute Carrageenan-induced Paw Inflammation Model

2019 ◽  
Vol 5 (1) ◽  
pp. 45-52
Author(s):  
Pavel D. Kolesnichenko ◽  
Anna A. Peresypkina ◽  
Artem A. Poromov ◽  
Elena N. Kareva ◽  
Alexey N. Demidenko
Keyword(s):  
Inflammatory Activity ◽  
C Reactive Protein ◽  
Reference Drug ◽  
Reactive Protein ◽  
Model Control ◽  
Anti Inflammatory ◽  
Thymus Serpyllum ◽  
Carrageenan Inflammation ◽  
Subplantar Injection ◽  
Inflammatory Effect

Introduction: Evaluation of anti-inflammatory action of Codelac® Broncho with Thymus Serpyllum (elixir) in comparison with Fenspiride was carried out on the model of acute carrageenan inflammation of the paws in rats. Materials and methods: Edema was caused by subplantar injection of 0.1 ml of 1% λ- carrageenan gel into the hind paw. The severity of edema was assessed by using 37140 plethysmometer (UGO BASILE, Italy). The measurements were performed before edema induction and 1, 2, 4, 12, 24, 48, 72, 96 and 120 hours afterwards. Anti-inflammatory activity of the drugs was also evaluated based on the analysis of rats’ blood, C-reactive protein concentration and histological examination results. Results and discussion: A decrease in the paw volume increment was revealed in the group with the studied drug in comparison with the group with the carrageenan edema model (control) 4, 12, 24 hours after injection of carrageenan (p&lt;0.05). As a result of plethysmometry, a more pronounced anti-inflammatory effect of the studied drug than that of Fenspiride was revealed. There was a significant decrease in the levels of leukocytes (p&lt;0.05), lymphocytes (p&lt;0.05), monocytes (p&lt;0.05) and neutrophils (p&lt;0.05) in the group with the studied drug compared to those the the control 48 hours after the initiation of edema, while in the group with Fenspiride, there was only a decrease in the levels of leukocytes (p&lt;0.05) and lymphocytes (p&lt;0.05). There were no differences in the concentration of C-reactive protein between the groups. Conclusion: The obtained data indicate a more pronounced anti-inflammatory activity of Codelac® Broncho with Thymus Serpyllum in comparison with Fenspiride, on the model of acute carrageenan inflammation of the paw in rats.

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