Oil based nanocarrier for improved oral delivery of silymarin: In vitro and in vivo studies

Parveen, Rabea; Baboota, Sanjula; Ali, Javed; Ahuja, Alka; Vasudev, Suruchi S.; Ahmad, Sayeed

doi:10.1016/j.ijpharm.2011.04.041

Cited by 141 publications

(80 citation statements)

References 23 publications

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“…Refractive index of selected formulations was determined in triplicate using an Abbe type refractometer. The apparent pH of the formulation was measure by a pH meter (Systronic 362 mpH system, India) at 25 C (Bali et al, 2010;Parveen et. al., 2011).…”

Section: Characterization Of Sqvm Nementioning

confidence: 99%

Nanoemulsion-based intranasal drug delivery system of saquinavir mesylate for brain targeting

et al. 2013

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The central nervous system (CNS) is an immunological privileged sanctuary site-providing reservoir for HIV-1 virus. Current anti-HIV drugs, although effective in reducing plasma viral levels, cannot eradicate the virus completely from the body. The low permeability of anti-HIV drugs across the blood-brain barrier (BBB) leads to insufficient delivery. Therefore, developing a novel approaches enhancing the CNS delivery of anti-HIV drugs are required for the treatment of neuro-AIDS. The aim of this study was to develop intranasal nanoemulsion (NE) for enhanced bioavailability and CNS targeting of saquinavir mesylate (SQVM). SQVM is a protease inhibitor which is a poorly soluble drug widely used as antiretroviral drug, with oral bioavailability is about 4%. The spontaneous emulsification method was used to prepare drug-loaded o/w nanoemulsion, which was characterized by droplet size, zeta potential, pH, drug content. Moreover, ex-vivo permeation studies were performed using sheep nasal mucosa. The optimized NE showed a significant increase in drug permeation rate compared to the plain drug suspension (PDS). Cilia toxicity study on sheep nasal mucosa showed no significant adverse effect of SQVM-loaded NE. Results of in vivo biodistribution studies show higher drug concentration in brain after intranasal administration of NE than intravenous delivered PDS. The higher percentage of drug targeting efficiency (% DTE) and nose-to-brain drug direct transport percentage (% DTP) for optimized NE indicated effective CNS targeting of SQVM via intranasal route. Gamma scintigraphy imaging of the rat brain conclusively demonstrated transport of drug in the CNS at larger extent after intranasal administration as NE.

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Section: Characterization Of Sqvm Nementioning

confidence: 99%

Nanoemulsion-based intranasal drug delivery system of saquinavir mesylate for brain targeting

et al. 2013

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“…The mechanism of action of silymarin and its role in the treatment of viral hepatitis will be discussed below. Silymarin is reported to have antioxidant activity (Parveen, Baboota, et al 2011), by increasing superoxide dismutase activity in erythrocytes and lymphocytes (Varga, Czompa, et al 2001).It is also reported to stabilize hepatocyte membrane structure, thereby preventing toxins from entering the cell through enterohepatic recirculation. It promotes liver regeneration by stimulating nuclear polymerase A (Leng-Peschlow.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of Silibinin Enriched Silymarin in Chronic HCV Patients

Hamed¹,

Khaled²,

Fathelbab³

et al. 2017

IAM

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Background/ Aim: Silymarin is a polyphenolic compound with anti-hepatotoxic activity. It has low oral bioavailability due to its poor aqueous solubility. Thus enhancement of its dissolution may lead to a better bioavailability. The objective of the presented study was to prepare fast dissolving enriched silymarin preparation via the preparation of enriched silymarin as solid dispersion and compare it with Legalon capsules in chronic HCV patients in a clinical study. Method: Enriched silymarin solid dispersion was prepared in sufficient amount. A clinical study was conducted including 24 patients. The patients were divided into two groups; each group had 12 patients. One group received the solid dispersion. The second group received Legalon capsules. Patients received capsules 3 times daily for 12 weeks. All these patients had been subjected to full medical history, abdominal ultrasonography, laboratory investigations and quality of life assessment at baseline and after treatment. Results: Solid dispersion had significantly faster dissolution rate. It is effective in reducing AST, ALT, total bilirubin, improving prothrombin concentration, prothrombin time and quality of life. Conclusion: Silymarin solid dispersion is a promising preparation. Large scale and longer duration may be required to ascertain its effects.

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“…Dissimilar volume ratios (1:0, 1:1, 1:2, 1:3, 2:1 and 3:1) of surfactant (Tween-80) and co-surfactant (Transcutol) mixtures (S mix ) were prepared and stocks of 100 ml from each faction were arranged (Chennamsetty et al, 2005;Parveen et al, 2011;Akhtar et al, 2014). For every phase diagram, 16 dissimilar combinations of oil (Sefsol 218) and S mix [1:9, 1:8, 1:7, 1:6, 1:5, 2:8 (1:4), 1:3.5, 1:3, 3:7 (1:2.3), 1:2, 4:6 (1:1.5), 5:5 (1:1), 6:4 (1:0.7), 7:3 (1:0.43), 8:2 (1:0.25), 9:1 (1:0.1)] were made in unusual volume ratios from 1:9 to 9:1; as a result, maximum ratios were covered for the study (Lawrence & Rees, 2000;Akhtar et al, 2014).…”

Section: Phase Diagram Constructionmentioning

confidence: 99%

“…Numerous potent lipophilic drugs exhibit low oral bioavailability due to their poor aqueous solubility and cannot be delivered by the oral route of administration in their original form due to instability, low membrane permeability, poor solubility and efflux transport mechanisms (Parveen et al, 2011;Akhtar et al, 2013). In recent years, lipid-based formulations (incorporation of the active lipophilic component into inert lipid vehicles) are used to improve the oral bioavailability of poorly water-soluble drug compounds, which include micro or nanoemulsions, oils, self-emulsifying formulations, surfactant dispersions, liposomes, solid lipid nanoparticles and lipid nanocarriers.…”

Section: Introductionmentioning

confidence: 99%

“…In recent years, lipid-based formulations (incorporation of the active lipophilic component into inert lipid vehicles) are used to improve the oral bioavailability of poorly water-soluble drug compounds, which include micro or nanoemulsions, oils, self-emulsifying formulations, surfactant dispersions, liposomes, solid lipid nanoparticles and lipid nanocarriers. Nanoemulsion offers several advantages over these drug delivery systems such as higher solubilization capacity, rapid onset of action (no extra time for dispersion), reduced intersubject variability in terms of gastrointestinal fluid volume and longer shelf life, toxicological safety, a high content of the lipid phase and the possibility of large scale production by high-pressure homogenization (Mustafa et al, 2009;Shakeel & Faisal, 2010;Parveen et al, 2011;Akhtar et al, 2014).…”

Section: Introductionmentioning

confidence: 99%

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Nanoemulsion: for improved oral delivery of repaglinide

Akhtar

Siddiqui

Fareed³

et al. 2015

Drug Delivery

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Repaglinide (RPG) is a fast-acting prandial glucose regulator. It acts by stimulating insulin release from pancreatic b-cells. Recurrent dosing of RPG before each meal is burdensome remedy. Hence the plan of the present study was to evaluate nanoemulsion as a hopeful carrier for RPG for persistent hypoglycemic effect. The drug was incorporated into oil phase of nanoemulsion to give improved biopharmaceutical properties as compared to the lipid-based systems. Pseudo ternary phase diagrams were prepared by aqueous titration method. Formulations were selected at a difference of 5% w/w of oil from the o/w nanoemulsion region of phase diagrams. The optimized nanoemulsion formulation constituted sefsol-218 (5% v/v) as an oil phase, 30% v/v of Tween-80 and transcutol as a surfactant and co-surfactant to restrain nanodroplet size and low viscosity and distilled water (65%). In vitro dissolution studies showed higher drug release (98.22%), finest droplet size (76.23 nm), slightest polydispersity value (0.183), least viscosity (21.45 cps) and immeasurable dilution capability from the nanoemulsion as compared with existing oral tablet formulation. The optimized RPG nanoemulsion formulation showed better hypoglycemic effect in comparison to tablet formulation in experimental diabetic rats. No significant variations were also observed in the optimized formulation when subjected to accelerated stability study at different temperature and relative humidity over a period of 3 months.

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Oil based nanocarrier for improved oral delivery of silymarin: In vitro and in vivo studies

Cited by 141 publications

References 23 publications

Nanoemulsion-based intranasal drug delivery system of saquinavir mesylate for brain targeting

Nanoemulsion-based intranasal drug delivery system of saquinavir mesylate for brain targeting

Evaluation of Silibinin Enriched Silymarin in Chronic HCV Patients

Nanoemulsion: for improved oral delivery of repaglinide

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