Effect of processing variables and in-vitro study of microparticulate system of nimesulide

Dashora, Kamlesh; Saraf, Shailendra

doi:10.1590/s1516-93322007000400008

Cited by 13 publications

(16 citation statements)

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“…A 10‐g sample of the freeze‐dried NPs was dissolved in 10 mL methanol and, after dilution to 10 μg/mL, drug content was analyzed using a UV spectrophotometer (Pharmaspec‐1700; Shimadzu, Kyoto, Japan) at 274.5 nm. The RPG entrapment efficiency (%) and RPG content (% w/w) in NPs were calculated using , respectively: 13 …”

Section: Methodsmentioning

confidence: 99%

Repaglinide‐loaded long‐circulating biodegradable nanoparticles: Rational approach for the management of type 2 diabetes mellitus

Jain

Saraf

2009

Journal of Diabetes

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IntroductionDiabetes mellitus is a chronic metabolic disorder characterized by high blood glucose concentrations (hyperglycemia) caused by insulin deficiency that are often combined with insulin resistance.1 Non-insulin-dependent diabetes mellitus (NIDDM) is a heterogeneous disorder, comprising milder forms of diabetes that occur predominately in adults. Most diabetic patients have NIDDM.2 AbstractBackground: Repaglinide (RPG) is an oral hypoglycemic agent with excellent bioavailability (90-98%) and a short plasma half-life (2-6 h). A full dose of RPG is required before each meal; hence, therapy may become inconvenient. Thus, the aim of the present study was to design a novel delivery system to maintain peak plasma levels of RPG for the long-term management of diabetes mellitus. Methods: Two nanoparticle formulations were prepared by combining RPG with poly (lactic-co-glycolic) acid alone or as a copolymer with methoxypolyethylene glycol (RPGNP1 and RPGNP2, respectively); both formulations were subjected to in vitro and in vivo characterization. In vivo characterization was performed in a streptozotocin (STZ)-induced diabetic male albino rats. Results: The mean particle size of the RPGNP1 and RPGNP2 formulations was 387.8 ± 11.9 and 310.2 ± 12.4 nm, respectively, with a zeta potential of )27.4 ± 0.7 and )15.7 ± 0.5 mV, respectively. The entrapment efficiency and drug content of RPGNP1 (58.7 ± 1.3% and 27.4 ± 2.3%, respectively) was better than that of RPGNP2 (45.8 ± 1.2% and 24.3 ± 1.1%, respectively). Blood glucose levels of RPGNP1-and RPGNP2-treated STZ-diabetic rats were reduced significantly (to normal levels) compared with untreated STZ-diabetic rats (P < 0.05), but there was no difference between the two treatment groups (P > 0.05). However, whereas RPGNP1 was effective for a period of only 24 h, RPGNP2 was effective for up to 1 week. Conclusions:The results of the present study show that RPGNP2 effectively manages type 2 diabetes mellitus for up to 1 week. Surface-modified NPs could be used to improve patient compliance with drug treatment as a result of decreased dosing frequency.

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Section: Methodsmentioning

confidence: 99%

Repaglinide‐loaded long‐circulating biodegradable nanoparticles: Rational approach for the management of type 2 diabetes mellitus

Jain

Saraf

2009

Journal of Diabetes

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“…The formulation was subjected to accelerated stability studies as per ICH (The International Conference of Harmonization) guidelines. The optimized formulation was sealed in an aluminum foil and stored at 25 ± 2°C, 60 ± 5% RH and at 40 ± 2°C, 75 ± 5% RH for 3 months (Dashora et al, 2007). Microparticles were periodically removed and evaluated for physical characteristics and in-vitro drug release.…”

Section: Stability Studymentioning

confidence: 99%

Formulation development and evaluation of Glibenclamide loaded Eudragit RLPO microparticles

Kumar

Chandiran

Jayaveera³

2013

Int Curr Pharm J

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The objective of the present investigation was to formulate and evaluate microencapsulated Glibenclamide produced by the emulsion solvent evaporation method. Microparticles were prepared using Eudragit RLPO by emulsion solvent evaporation method and characterized for their micromeritic properties, encapsulation efficiency, particle size, drug loading, FTIR, DSC, SEM analysis. In vitro release studies were performed in phosphate buffer (pH 7.4). Stability studies were conducted as per ICH guidelines. The resulting microparticles obtained by solvent evaporation method were free flowing in nature. The mean particle size of microparticles ranges from 134.49 179.72 µm and encapsulation efficiency ranges from 92.30-98.32%. The infrared spectra and differential scanning calorimetry thermographs confirmed the stable character of Glibenclamide in the drug-loaded microparticles. Scanning electron microscopy revealed that the microparticles were spherical in nature. In vitro release studies revealed that the drug release was sustained up to 12 hrs. The release kinetics of Glibenclamide from optimized formulation followed zero-order and peppas mechanism. The mechanism of drug release from the microparticles was found to be non-Fickian type. Eudragit RLPO microparticles containing Glibenclamide could be prepared successfully by using an emulsion solvent evaporation technique, which will not only sustain the release of drug but also manage complicacy of the diabetes in a better manner.DOI: http://dx.doi.org/10.3329/icpj.v2i12.17016 International Current Pharmaceutical Journal, November 2013, 2(12): 196-201

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“…Particle size analysis of drug-loaded Eudragit S100 microspheres was performed by optical microscopy using a compound microscope (Erma, Tokyo, Japan). 20 A small amount of dry microspheres was suspended in purified water (10 mL). The suspension was ultrasonicated for 5 seconds.…”

Section: Particle Sizementioning

confidence: 99%

Influence of selected formulation variables on the preparation of enzyme-entrapped eudragit S100 microspheres

Rawat

Saraf

2007

AAPS PharmSciTech

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The aim of this work is to study the influence of formulation parameters in the preparation of sustained release enzyme-loaded Eudragit S100 microspheres by emulsion solvent diffusion technique. A 3(2) full factorial experiment was designed to study the effects of the amount of solvent (dichloromethane) and stabilizers (Tween 20, 40, or 80) on the drug content and microsphere size. The results of analysis of variance test for both effects indicated that the test is significant. The effect of amount of stabilizer was found to be higher on both responses (SS(Y1) = 45.60; SS(Y2) = 737.93), whereas solvent concentration comparatively produced significant effect on the size of microspheres (SS(Y1) = 0.81; SS(Y2) = 358.83). Scanning electron microscopy of microspheres with maximum drug content (2.5 mL dichloromethane and 0.1 mL Tween 80) demonstrated smooth surface spherical particles with mean diameter of 56.83 +/- 2.88 microm. The effect of formulation variables on the integrity of enzyme was confirmed by in vitro proteolytic activity. The enteric nature of microspheres was evaluated and results demonstrated ~6% to 7% release of enzyme in acidic medium. The release of enzyme from microspheres followed Higuchi kinetics. In phosphate buffer, microspheres showed an initial burst release of 20.34% +/- 2.35% in 1 hour with additional 58.79% +/- 4.32% release in the next 5 hours. Three dimensional response graphs were presented to visualize the effect of independent variables on the chosen response. Thus, Eudragit S100 microspheres can be successfully prepared for oral delivery of enzymes with desirable characters in terms of maximum loading and diffusion release pattern.

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Effect of processing variables and in-vitro study of microparticulate system of nimesulide

Cited by 13 publications

References 13 publications

Repaglinide‐loaded long‐circulating biodegradable nanoparticles: Rational approach for the management of type 2 diabetes mellitus

Repaglinide‐loaded long‐circulating biodegradable nanoparticles: Rational approach for the management of type 2 diabetes mellitus

Formulation development and evaluation of Glibenclamide loaded Eudragit RLPO microparticles

Influence of selected formulation variables on the preparation of enzyme-entrapped eudragit S100 microspheres

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