Formulation and Evaluation of Gliclazide Nanosponges

Solunke, Rahul Shivajirao; Borge, Uday R.; Murthy, K. V. S.; Deshmukh, Madhuri; Shete, Rajkumar V.

doi:10.22159/ijap.2019v11i6.35006

Cited by 30 publications

(20 citation statements)

References 9 publications

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“…6 Different nano-carrier models for gliclazide were addressed and evaluated in-vitro with complete disregard for in-vivo behavior. [7][8][9][10][11] Other studies were satisfied with either the pharmacokinetics evaluation, 12 or both pharmacokinetics and pharmacodynamics appraisal. 13 However, they did not tackle the safety of the prepared systems.…”

Section: Introductionmentioning

confidence: 99%

<p>Lipid-Based Gliclazide Nanoparticles for Treatment of Diabetes: Formulation, Pharmacokinetics, Pharmacodynamics and Subacute Toxicity Study</p>

Nazief

Hassaan

Khalifa

et al. 2020

IJN

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Introduction: Solid lipid nanoparticles (SLNs) are considered a promising system in enhancing the oral bioavailability of poorly water-soluble drugs; owing to their intrinsic ability to increase the solubility together with protecting the incorporated drugs from extensive metabolism. Objective: Exploiting such properties, SLNs loaded with gliclazide (GLZ) were developed in an attempt to improve the oral bioavailability and the anti-diabetic action of GLZ, together with prolonging its duration of action for better glycemic control. Methods: SLNs were prepared by ultra-sonication technique using glyceryl behenate (Compritol ® 888 ATO) as a lipid matrix and poloxamer 188 (PLX) as a stabilizer. A 2*3 asymmetrical factorial design was adopted to study the effect of different stabilizer concentrations at different sonication times on the shape, and size of the particles, PDI and drug loading. The selected optimum formulation was then freeze dried using trehalose di-hydrate as a cryo-protectant in different ratios with respect to glyceryl behenate concentration. After freeze drying, the formulation was tested for in-vitro drug release, pharmacokinetics, and pharmacodynamics. Safety of the selected formula was established after carrying out a subacute toxicity study. Results: The factorial design experiment resulted in an optimum formulation coded 10F2 (150 mg PLX/10 min sonication). Scanning electron micrographs showed spherical particles with smooth surface, whereas a ratio of 2:1 cryo-protectant:lipid was found to be optimum with particle size of 245.9 ± 26.2 nm, polydispersity index of 0.482 ± 0.026, and biphasic in-vitro release with an initial burst effect, followed by a prolonged release phase. On the other hand, the selected SLNs exhibited prolonged drug release when compared with the GLZ commercial immediate release (IR) tablets (Diamicron ® ). Pharmacokinetics study showed about 5-fold increase in GLZ oral bioavailability loaded in SLNs when compared with raw GLZ powder. Pharmacodynamics study on a diabetic rat model confirmed the better anti-diabetic action of GLZ loaded SLNs when compared to raw GLZ powder. Subacute toxicity study indicated the safety of SLNs upon repetitive oral administration.

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Section: Introductionmentioning

confidence: 99%

<p>Lipid-Based Gliclazide Nanoparticles for Treatment of Diabetes: Formulation, Pharmacokinetics, Pharmacodynamics and Subacute Toxicity Study</p>

Nazief

Hassaan

Khalifa

et al. 2020

IJN

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“…At this point, for 2 hours at 1000 rpm, the blend is thoroughly blended. The required NSs were collected by the filtration method and held for drying in an oven at 40 °C for 24 h. Dried NSs have been put away in desiccators and the evacuation of remaining solvents is assured [ 55 ] (Fig. 6 ).…”

Section: Methods Of Preparation Of Nanospongesmentioning

confidence: 99%

The ascension of nanosponges as a drug delivery carrier: preparation, characterization, and applications

Tiwari

Bhattacharya

2022

J Mater Sci: Mater Med

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Nanosponges are nanosized drug carriers with a three-dimensional structure created by crosslinking polymers. They have the advantage of being able to hold a wide range of drugs of various sizes. Nanosponges come in a variety of shapes and sizes. They are distinguished by the research method used, the type of polymer used, and the type of drug they may contain. Nanosponges are superior to other delivery systems because they can provide a controlled drug release pattern with targeted drug delivery. The period of action, as well as the drug’s residence time, may be regulated. Since it is made of biodegradable materials, it has a low toxicity and is safe to use. The efficiency of drug encapsulation is determined by the size of the drug molecule and the amount of void space available. Cancer, enzyme and biocatalyst carrier, oxygen delivery, solubility enhancement, enzyme immobilization, and poison absorbent are some of the applications for nanosponges. The method of preparation, characterization, factors affecting nanosponge development, drug loading and release mechanism, recent developments in this area, and patents filed in the area of nanosponges are all highlighted in this study.

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“…The lafutidine nanosponges obtained after drying was weighed. Percentage yield value was calculated as follows: 13 % Yield Weight of nanosponge Total solid weight = × 100…”

Section: Percentage Yieldmentioning

confidence: 99%

Gastroretentive Floating Tablets Enclosing Nanosponge Loaded with Lafutidine for Gastric Ulcer: Formulation and Evaluation

Poornima¹,

Priya²

2021

IJPER

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Aim and Objectives: The present study aimed to formulate and evaluate gastroretentive nanosponge loaded with lafutidine for a gastric ulcer to overcome the drawbacks of oral conventional dosage forms such as the inability to confine and locate within the desired region of the gastrointestinal tract due to variable gastric emptying and motility. The floating tablets of nanosponge were formulated to increase the bioavailability of lafutidine by prolonging retention time in the upper gastric region. Materials and Methods: The emulsion solvent diffusion method was used to prepare the nanosponge and 3 2 factorial design was employed to assess the influence of two independent variables ethyl cellulose: polyvinyl alcohol ratio and sonication time on particle size, entrapment efficiency and zeta potential of the prepared nanosponges. The optimized nanosponges were compressed into tablets by the direct compression method. Results: Statistical analysis revealed the significant effect of ethyl cellulose: polyvinyl alcohol ratio and sonication time on particle size, entrapment efficiency and zeta potential. The SEM images of the optimized formulation revealed the spherical shape and porous surface of the nanosponges. Pre and post-compression parameters of floating tablets found to be within the limit and the floating tablets of nanosponge remained buoyant for 24 h whereas nanosponges remained buoyant only for 7 h. The F1 formulation showed short lag time, maximum drug content (98.7%), sustained the drug release for 24 h and it was stable for the entire period study. Conclusion: The floating tablet of nanosponge is promising in retaining and controlling drug release for a pronged period of time in the stomach.

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Formulation and Evaluation of Gliclazide Nanosponges

Cited by 30 publications

References 9 publications

<p>Lipid-Based Gliclazide Nanoparticles for Treatment of Diabetes: Formulation, Pharmacokinetics, Pharmacodynamics and Subacute Toxicity Study</p>

<p>Lipid-Based Gliclazide Nanoparticles for Treatment of Diabetes: Formulation, Pharmacokinetics, Pharmacodynamics and Subacute Toxicity Study</p>

The ascension of nanosponges as a drug delivery carrier: preparation, characterization, and applications

Gastroretentive Floating Tablets Enclosing Nanosponge Loaded with Lafutidine for Gastric Ulcer: Formulation and Evaluation

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