Sustained-release diclofenac potassium-loaded solid lipid microparticle based on solidified reverse micellar solution:<i>in vitro</i>and<i>in vivo</i>evaluation

Chime, Salome Amarachi; Attama, Anthony A.; Builders, Philip F.; Onunkwo, Godswill C.

doi:10.3109/02652048.2012.726284

Cited by 50 publications

(30 citation statements)

References 21 publications

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“…Eighteen albino rats (average weight: 300 g) were divided in three groups and kept under standard laboratory conditions (temperature: 25 ± 2°C; relative humidity: 55 ± 5%), in polypropylene cages with free access to standard laboratory diet (Lipton feed, Mumbai, India) and water ad libitum . Animals were administered their respective treatments (Table 6) and blood samples (0.2 mL) were collected at predetermined time intervals till 24 hours [11, 23]. Plasma was separated by centrifuging the collected sample at 5000 rpm for 20 min and stored at −21°C until drug estimation using HPLC.

Group I = ES (~10 mg).

Group II = commercial formulation (~10 mg).

Group III = ESLN-3 (~10 mg).

…”

Section: Characterizationmentioning

confidence: 99%

“…The SLN's ability to incorporate hydrophilic/hydrophobic drugs imparts unique diversity. Hence controlled drug delivery, enhancement of bioavailability of entrapped drugs via modification of dissolution rate and/or improvement of tissue distribution, and targeting of drugs by using SLNs have been reported in various application routes like parenteral (intravenously, intramuscularly, or subcutaneously), oral, rectal, ophthalmic, and topical (cosmetics and dermatological) preparations [8–11]. …”

Section: Introductionmentioning

confidence: 99%

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Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles:In VitroDrug Release and Pharmacokinetics Studies

Gaur¹,

Mishra

Bajpai³

et al. 2014

BioMed Research International

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Solid lipid nanoparticle is an efficient lipid based drug delivery system which can enhance the bioavailability of poorly water soluble drugs. Efavirenz is a highly lipophilic drug from nonnucleoside inhibitor category for treatment of HIV. Present work illustrates development of an SLN formulation for Efavirenz with increased bioavailability. At first, suitable lipid component and surfactant were chosen. SLNs were prepared and analyzed for physical parameters, stability, and pharmacokinetic profile. Efavirenz loaded SLNs were formulated using Glyceryl monostearate as main lipid and Tween 80 as surfactant. ESLN-3 has shown mean particle size of 124.5 ± 3.2 nm with a PDI value of 0.234, negative zeta potential, and 86% drug entrapment. In vitro drug release study has shown 60.6–98.22% drug release in 24 h by various SLN formulations. Optimized SLNs have shown good stability at 40°C ± 2°C and 75 ± 5% relative humidity (RH) for 180 days. ESLN-3 exhibited 5.32-fold increase in peak plasma concentration (C max⁡) and 10.98-fold increase in AUC in comparison to Efavirenz suspension (ES).

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Group I = ES (~10 mg).

Group II = commercial formulation (~10 mg).

Group III = ESLN-3 (~10 mg).

…”

Section: Characterizationmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles:In VitroDrug Release and Pharmacokinetics Studies

Gaur¹,

Mishra

Bajpai³

et al. 2014

BioMed Research International

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“…Liu et al formulated diclofenac sodium-loaded SLN by emulsion/solvent evaporation method [20]. Chime et al prepared diclofenac potassium-loaded solid lipid microparticle using solidified reverse micellar solution and found them suitable for oral and parenteral administration [21]. …”

Section: Introductionmentioning

confidence: 99%

Solid Lipid Nanoparticles of Guggul Lipid as Drug Carrier for Transdermal Drug Delivery

Gaur¹,

Mishra

Purohit

2013

BioMed Research International

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Diclofenac sodium loaded solid lipid nanoparticles (SLNs) were formulated using guggul lipid as major lipid component and analyzed for physical parameters, permeation profile, and anti-inflammatory activity. The SLNs were prepared using melt-emulsion sonication/low temperature-solidification method and characterized for physical parameters, in vitro drug release, and accelerated stability studies, and formulated into gel. Respective gels were compared with a commercial emulgel (CEG) and plain carbopol gel containing drug (CG) for ex vivo and in vivo drug permeation and anti-inflammatory activity. The SLNs were stable with optimum physical parameters. GMS nanoparticle 1 (GMN-1) and stearic acid nanoparticle 1 (SAN-1) gave the highest in vitro drug release. Guggul lipid nanoparticle gel 3 (GLNG-3) showed 104.68 times higher drug content than CEG in receptor fluid. The enhancement ratio of GLNG-3 was 39.43 with respect to CG. GLNG-3 showed almost 8.12 times higher C max than CEG at 4 hours. The AUC value of GLNG-3 was 15.28 times higher than the AUC of CEG. GLNG-3 showed edema inhibition up to 69.47% in the first hour. Physicochemical properties of major lipid component govern the properties of SLN. SLN made up of guggul lipid showed good physical properties with acceptable stability. Furthermore, it showed a controlled drug release profile along with a promising permeation profile.

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“…[14] For each stomach, the severity of the mucosal damage was assessed according to the following scoring system: 0 -no lesions or one punctiform lesion; 1 -two to five punctiform lesions; 2 -one to five small ulcers; 3 -more than five small ulcers or one large ulcer; 4 -more than one large ulcers. Among them, control group received normal saline, the second group received with pure DS (10 mg/kg), and the third group administered CP pellets by oral route.…”

Section: Ulcerogenicitymentioning

confidence: 99%

Chitosan phthalate: A novel polymer for the multiparticulate drug delivery system for diclofenac sodium

et al. 2017

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This study investigates the preparation of colon specific drug delivery of diclofenac sodium (DS) using maltiparticulate system with chitosan phthalate (CP). Technique adopted to prepare sphere shaped multiparticulate system was extrusion and spheronization. The prepared pellets resulted with good spherical geometry with 1.1 ± 0.20 mm diameter. DS loaded system shows a maximum delivery pH of 7.4 and the same depressed at pH 1.2. The developed system significantly (p < .05) increase in the peak plasma concentration (C max ) of DS pellets when compared to that of pure DS. As expected the novel formulation showed a significant increase in oral bioavailability of DS for about three times. Additionally, the CP pellets of DS showed a momentous improvement in anti-inflammatory activity and reduced/ inhibited ulcer index. K E Y W O R D Schitosan phthalate, in vivo, pH dependent, sustained release

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Sustained-release diclofenac potassium-loaded solid lipid microparticle based on solidified reverse micellar solution:in vitroandin vivoevaluation

Abstract: Diclofenac potassium-loaded SLMs based on SRMS could be used orally or parenterally under controlled conditions, for once daily administration.

Cited by 50 publications

References 21 publications

Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles:In VitroDrug Release and Pharmacokinetics Studies

Enhanced Oral Bioavailability of Efavirenz by Solid Lipid Nanoparticles:In VitroDrug Release and Pharmacokinetics Studies

Solid Lipid Nanoparticles of Guggul Lipid as Drug Carrier for Transdermal Drug Delivery

Chitosan phthalate: A novel polymer for the multiparticulate drug delivery system for diclofenac sodium

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