20 research outputs found
Self-Nanoemulsifying Drug Delivery Systems Containing Plantago lanceolata—An Assessment of Their Antioxidant and Antiinflammatory Effects
The most important components of Plantago lanceolata L. leaves are catalpol, aucubin, and acteoside (=verbascoside). These bioactive compounds possess different pharmacological effects: anti-inflammatory, antioxidant, antineoplastic, and hepatoprotective. The aim of this study was to protect Plantago lanceolata extract from hydrolysis and to improve its antioxidant effect using self-nano-emulsifying drug delivery systems (SNEDDS). Eight SNEDDS compositions were prepared, and their physical properties, in vitro cytotoxicity, and in vivo AST/ALT values were investigated. MTT cell viability assay was performed on Caco-2 cells. The well-diluted samples (200 to 1000-fold dilutions) proved to be non-cytotoxic. The acute administration of PL-SNEDDS compositions resulted in minor changes in hepatic markers (AST, ALT), except for compositions 4 and 8 due to their high Transcutol contents (80%). The non-toxic compositions showed a significant increase in free radical scavenger activity measured by the DPPH test compared to the blank SNEDDS. An indirect dissolution test was performed, based on the result of the DPPH antioxidant assay; the dissolution profiles of Plantago lancolata extract were statistically different from each SNEDDS. The anti-inflammatory effect of PL-SNEDDS compositions was confirmed by the ear inflammation test. For the complete examination period, all compositions decreased ear edema as compared to the positive (untreated) control. It can be concluded that PL-SNEDDS compositions could be used to deliver active natural compounds in a stable, efficient, and safe manner
Self-Nanoemulsifying Drug Delivery Systems Containing Plantago lanceolata—An Assessment of Their Antioxidant and Antiinflammatory Effects
The most important components of Plantago lanceolata L. leaves are catalpol, aucubin, and acteoside (=verbascoside). These bioactive compounds possess different pharmacological effects: anti-inflammatory, antioxidant, antineoplastic, and hepatoprotective. The aim of this study was to protect Plantago lanceolata extract from hydrolysis and to improve its antioxidant effect using self-nano-emulsifying drug delivery systems (SNEDDS). Eight SNEDDS compositions were prepared, and their physical properties, in vitro cytotoxicity, and in vivo AST/ALT values were investigated. MTT cell viability assay was performed on Caco-2 cells. The well-diluted samples (200 to 1000-fold dilutions) proved to be non-cytotoxic. The acute administration of PL-SNEDDS compositions resulted in minor changes in hepatic markers (AST, ALT), except for compositions 4 and 8 due to their high Transcutol contents (80%). The non-toxic compositions showed a significant increase in free radical scavenger activity measured by the DPPH test compared to the blank SNEDDS. An indirect dissolution test was performed, based on the result of the DPPH antioxidant assay; the dissolution profiles of Plantago lancolata extract were statistically different from each SNEDDS. The anti-inflammatory effect of PL-SNEDDS compositions was confirmed by the ear inflammation test. For the complete examination period, all compositions decreased ear edema as compared to the positive (untreated) control. It can be concluded that PL-SNEDDS compositions could be used to deliver active natural compounds in a stable, efficient, and safe manner
Formulation and investigation of Self-Emulsifying Drug Delivery System (SEDDS) containing natural herb extract or different antitumor agents
Approximately 70-75% of medications marketed worldwide are administrated per os and are proven to be less effective than desired. The majority of newly developed drugs represent poor aqueous solubility and stability. Drug instability results in lack of dose appropriateness after oral administration. Many different methods have been found to enhance drug dissolution rate and improve the physicochemical stability of drugs by applying surface-active agents, Cyclodextrins, nanoparticles or liposomes. Lipid-based drug delivery systems represent one of the most popular technologies for improving oral bioavailability and solubility. Micro- and nanoemulsions are lipid-based formulations that have a significant potential for drug delivery applications and self-micro/nanoemulsifying drug delivery systems (SM/NEDDS) considered as the best of these systems. Many studies suggested that SM/NEDDS are suitable carrier systems drugs which are very sensitive to hydrolysis. SM/NEDDS are characterized as isotropic mixtures of synthetic or natural oil and solid or liquid surface active agents or, alternatively, a single or several hydrophilic solvents and co-solvents and a drug which spontaneously forms oil-in-water (o/w) nanoemulsion/microemulsion droplets with water following a gentle stirring. In gastrointestinal fluid, this system spreads readily in the GI lumen and the agitation necessary for self-emulsification is provided by the gastric and intestinal digestive motility. After dilution with aqueous media, the oil droplets keep the drug inside of them or they form a micellar solution due to the very high surface-active agent concentration of such formulations. The drug will be delivered to the GI mucosa in dissolved state by these fine droplets; therefore, it will be readily available for absorption and its efficacy and bioavailability will also be increased. Micro/nanoemulsions improve oral bioavailability, protect drugs from enymatic hydrolysis and have high drug solubilization capacity and outstanding thermodynamic stability.
The phenomenon of self-emulsification occurs only when specific combinations of pharmaceutical excipients are present.
Several chemotherapeutic agents are used in the treatment of cervical cancer. Cisplatin is considered to be among the most effective drugs that treat advanced uterine and cervical cancer. Bleomycin sulfate is a mixture of glycopeptide antitumor antibiotics that has a unique mechanism of antitumor activity in cervical cancer. Ifosfamide is an anti-cancer drug and is widely used in the treatment of cervical, ovarian and testicular malignancies. In recent chemotherapy, cisplatin, bleomycin and ifosfamide (BIP) in combination has also been applied against inoperable cervical cancer. To decrease the serious side effects resulted from use of cytostatic medications it is necessary to formulate modern drug delivery systems which can reduce toxicity by decreasing the dose of potent therapeutic agent. SMEDDS are frequently used to increase the bioavailability of poorly soluble drugs by presenting and maintaining API in a dissolved state, in small droplets of oil with a ability to penetrate through various biological barriers.
Plantago lanceolata has been widely used for medical purposes, such as the treatment of bleeding and tissue damage, antioxidant, anti-inflammatory, antibacterial antiviral and hepatoprotective. Some prominent pharmacological studies are outlined in the following section. Iridoid glucoside aucubin and its derivatives have been identified as important biologically active compounds in plantain by several studies. The main bioactive component of Plantago lanceolata is verbascoside (acteoside), which is a phenylpropanoid glycoside. However the high capability of its bioactive components for hydrolysis resulted in poor stability of this natural extract. SNEDDS is frequently used for the stabilization of natural products and these carrier systems may also increase the bioavailability of natural bioactive materials.N
Chemical composition and antifungal effect of hydroalcoholic extract of Allium tripedale (Tvautv.) against Candida species
Background and Purpose: Treatment of life-threatening fungal infections caused by Candida species has become a major problem. Candida spp. are the most important causative agents of candidiasis. Allium tripedale is a medicinal plant that has been traditionally used to treat infections. In the present study, we aimed to determine the chemical compounds and antimicrobial activity of hydroalcoholic extract of A.tripedale against different species of Candida.
Materials and Methods: Phytochemical analysis was performed to identify the possible bioactive components of this extract by using gas chromatography and mass spectroscopy (GC-MS). The hydroalcoholic extract of A. tripedale were collected.Different concentrations of A. tripedale (50, 25, 12.5, and 6.25 mg/ml) were used to evaluate its antifungal activity against Candida species (C. albicans, C. parapsilosis,and C. krusei) using disk diffusion assay.
Results: The GC-MS analysis revealed the presence of 40 different phytoconstituents with peak area; the major compounds were tetracosane, hexadecanoic acid, 1-eicosanol, 1,2-dihydro-pyrido[3,2,1-kl]phenothiazin-3-one, 2-hexadecen-1-ol, and 3,7,11,15-tetramethyl. Hydroalcoholic extract showed strong antimicrobial activity (inhibition zone ⩾ 20 mm), moderate antimicrobial activity (inhibition zone < 12-20 mm), and no inhibition (zone < 12 mm). In addition, the hydroalcoholic extract exhibited the highest antimicrobial properties against C. albicans strains.
Conclusion: A. tripedale extract had a considerable inhibitory effect against various Candida species, but its highest inhibitory effect was against Candid albicans. Further investigations are required to detect the performance of this plant in the treatment of Candida infection.
 
Histopathological and Biomedical Parameters Determination in the Protective Effect of Hydroalcoholic Extract of Allium Jesdianum on Hepatotoxicity Induced by Bromobenzene: Effect of Allium Jesdianum Extract on Bromobenzene Induced Hepatotoxicity
Allium Jesdianum (AJ) is the native plant mostly grown in Middle East region that has the excellent pharmacological properties. In this study, we evaluated the hepatoprotective effect of hydroalcoholic extract of AJ on liver injury induced by Bromobenzene (BB) in male mice. Animals were randomly divided into five groups, control group received normal saline plus olive oil, groups 2-4 received (500, 1000 and 2000 mg/kg) AJ extract plus BB for 5 days and 5th group received BB (460 mg/kg). On the fifth day all groups received hexobarbital sodium (25 mg/kg, i.p). It should be noted that sleeping time of the all mice were recorded. After 24 hours the mice were sacrificed. By serum and tissue biomarkers such as alanine aminotransferase (ALT), aspartate aminotransferase (AST), reduced glutathione (GSH), malondialdehyde (MDA), and histopathological studies were measured. The results showed that BB significantly increased sleeping time, ALT, AST, and MDA levels besides and decreased GSH level compared with the control group. AJ extract at doses1000and 2000 mg/kg showed a significant alter in all studied endpoints and dose 2000 mg/kg showed a marked improvement in histopathological examination. The present finding indicated that administration of the hydroalcoholic extract of AJ could prevent hepatotoxicity induced by BB via improvement serum and tissue parameters and histopathological alterations in liver tissue