Development of Oral Chewable Tablets Containing Montelukast Nanoparticles for the Treatment of Childhood Asthma: Preclinical Study in Animal Model

2021 ◽  
Vol 11 (4) ◽  
pp. 786-791
Author(s):  
Ye Liu ◽  
Guihua Xia ◽  
Shaosheng Liu ◽  
Zhenyu Song
Keyword(s):  
Zeta Potential ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Crosslinking Agent ◽  
Preclinical Study ◽  
Control Group ◽  
Physical Parameters ◽  
Disintegration Time ◽  
Saturation Solubility ◽  
Chewable Tablets

The aim of the present study was to formulate oral chewable tablets of Montelukast (MTL) in the form of nanoparticles (NP’s). The MTL loaded NP’s were formulated by ionotropic external gelation method using tripolyphosphate (TPP) as crosslinking agent and Tween 60 as surfactant. NP’s were characterized for drug loading, encapsulation efficiency, surface morphology, saturation solubility, particle size, zeta potential and polydispersity index. The optimized NP formulation was used for development of chewable tablets using direct compression method. The prepared tablets were characterized for disintegration test, dissolution, thickness, hardness, friability and assay. The optimized formulation was evaluated in asthamatic animals to demonstrate the efficiency in asthama. The encapsulation efficiency of NP’s was found between 91.24 to 98.21% while drug loading was in the range of 10.09–14.25%. All formulations were found of nanosized in nature (110 to 200 nm) with excellent zeta potential (20.12 to 22.27 mV). PDI of all NP formulations were found within acceptable limit (less than 0.3). The nanoparticles were found spherical in shape with smooth surface. The saturation solubility of MTL was enhanced nearly 10 times (92 mg/ml) as compared to pure MTL saturation solubility. All physical parameters of the tablets were found within range. The optimized tablets showed disintegration time of 20 sec while other formulations showed DT in the rage of 35–57 sec. Tab1 (Optimized formulation) showed almost 100% MTL release from chewable tablets within the period of 30 min. Reduction in lung resistance (RI) was found in animals treated with Tab1. This reduction in RI was found nearly two fold and three fold as compare to MTL treated and control group animals. These observations clearly support the efficacy of chewable tablets containing nanoparticulate MTL in asthmatic animals.

scholarly journals PREPARATION AND CHARACTERIZATION OF ORAL NANOSUSPENSION LOADED WITH CURCUMIN

2018 ◽  
Vol 10 (6) ◽  
pp. 90 ◽  
Author(s):  
Sneha Dekate Shreeram Hirlekar ◽  
Srinivas Bhairy ◽  
Srinivas Bhairy ◽  
Rajashree Hirlekar ◽  
Rajashree Hirlekar
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
High Speed ◽  
Drug Loading ◽  
Research Work ◽  
Release Kinetic ◽  
Pharmacokinetic Studies ◽  
Sprague Dawley ◽  
Saturation Solubility

Objective: The principle objective of the present research work was to improve the bioavailability of curcumin (CUR) by decreasing its particle size. Nanosuspension (NS) of CUR was prepared using poloxamer-188 (P188) as a surfactant. The prepared NSs were characterized for particle size, polydispersity index (PDI), zeta potential, drug loading, saturation solubility, and drug release kinetic studies.Methods: Components required for NS preparation, such as solvent, anti-solvent and surfactant were screened. Precipitation high-speed homogenization (HSH) method was used for the preparation of NS using selected components. Evaluation of NS for particle size, PDI, drug loading, saturation solubility and in vitro drug release was done. Pharmacokinetic studies of the NS in sprague dawley (SD) rats were performed.Results: The particle size, PDI and zeta potential of the optimized formulation was 596.5±5 nm, 0.233±0.010 and-23±2 mV respectively. The pH of all the formulations was in the range of 5-6 which is acceptable when related to drug stability. The optimized formulation showed an increase in saturation solubility in water and phosphate buffer pH 6.8 when compared to plain CUR suspension (S). Results of pharmacokinetic studies indicated that Cmax and AUC0-6 were increased 8 and 10 times respectively from plain CUR S to CUR NS.Conclusion: CUR NS was prepared using P188 as the stabilizer. Amongst various stabilizers screened P188 rendered a stable NS with the particle size in nano range. Pharmacokinetic studies revealed the better performance of CUR NS as compared to plain CUR S.

scholarly journals Inulin-Grafted Stearate (In-g-St) as the Effective Self-Assembling Polymeric Micelle: Synthesis and Evaluation for the Delivery of Betamethasone

2020 ◽  
Vol 2020 ◽  
pp. 1-8
Author(s):  
Gholamabbas Chehardoli ◽  
Parham Norouzian ◽  
Farzin Firozian
Keyword(s):  
Zeta Potential ◽  
Sustained Release ◽  
Targeted Delivery ◽  
Encapsulation Efficiency ◽  
Polymeric Micelles ◽  
Drug Loading ◽  
Polymeric Micelle ◽  
Water Soluble ◽  
Burst Release ◽  
Potential Measurement

Background. Betamethasone as a corticosteroid drug is commonly used for the treatment of rheumatoid arthritis. Unfortunately, betamethasone is a low water-soluble drug and its efficacy is low. So an attractive strategy is the targeted delivery of betamethasone to the damaged joint using polymeric micelle-based carriers. Methods. Inulin-grafted stearate (In-g-St) was synthesized via the reaction of stearoyl chloride and inulin, then characterized by FT-IR and H-NMR. In-g-St forms micelles in the presence of betamethasone. The prepared polymeric micelles were characterized for size, zeta potential, drug loading, particles’ morphology, critical micelle concentration (CMC), and encapsulation efficiency. So sustained release polymeric micelles of betamethasone were developed by employing In-g-St. Results. The measurement of particle size showed a mean diameter of 60 and 130 nm for 10% and 20% drug-loaded micelles, respectively, and SEM showed that the particle’s morphologies are spherical. Zeta potential measurement for the drug-containing micelles showed a value of -11.8 mV. Drug loading efficiency and the encapsulation efficiency were 6.36% and 63.6%, as well as 18.97% and 94.88% for 10% and 20%, respectively. 20% drug-loaded polymer showed a small burst release of betamethasone at the first 3 h which was followed by sustained release in the next 24 h. Furthermore, the formula with 10% exhibited good sustained release properties except for the minor initial burst release. Conclusion. Data from the zeta potential, CMC, drug loading capacity, and in vitro drug release studies indicated that In-g-St polymeric micelles can be suitable candidates for the efficient delivery of hydrophobic drugs like betamethasone.

scholarly journals Coencapsulation of Polyphenols and Anthocyanins from Blueberry Pomace by Double Emulsion Stabilized by Whey Proteins: Effect of Homogenization Parameters

Molecules ◽  
2018 ◽  
Vol 23 (10) ◽  
pp. 2525 ◽  
Author(s):  
Bio Bamba ◽  
John Shi ◽  
Carole Tranchant ◽  
Sophia Xue ◽  
Charles Forney ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Encapsulation Efficiency ◽  
Droplet Diameter ◽  
Whey Proteins ◽  
Double Emulsion ◽  
Protein Isolate ◽  
Hydrodynamic Diameter ◽  
Physical Parameters ◽  
Oil Droplets ◽  
Homogenization Time

Blueberry pomace is a rich source of high-value bioactive polyphenols with presumed health benefits. Their incorporation into functional foods and health-related products benefits from coencapsulation and protection of polyphenol-rich extracts in suitable carriers. This study aimed to create a water-in-oil-in-water (W1/O/W2) double emulsion system suitable for the coencapsulation of total phenolics (TP) and anthocyanins (TA) from a polyphenol-rich extract of blueberry pomace (W1). The effect of critical physical parameters for preparing stable double emulsions, namely homogenization pressure, stirring speed and time, was investigated by measuring the hydrodynamic diameter, size dispersity and zeta potential of the oil droplets, and the encapsulation efficiency of TP and TA. The oil droplets were negatively charged (negative zeta potential values), which was related to the pH and composition of W2 (whey protein isolate solution) and suggests stabilization by the charged whey proteins. Increasing W1/O/W2 microfluidization pressure from 50 to 200 MPa or homogenization speed from 6000 to 12,000 rpm significantly increased droplet diameter and zeta potential and decreased TA and TP encapsulation efficiency. Increasing W1/O/W2 homogenization time from 15 to 20 min also increased droplet diameter and zeta potential and lowered TA encapsulation efficiency, while TP encapsulation did not vary significantly. In contrast, increasing W1/O homogenization time from 5 to 10 min at 10,000 rpm markedly increased TA encapsulation efficiency and reduced droplet diameter and zeta potential. High coencapsulation rates of blueberry polyphenols and anthocyanins around 80% or greater were achieved when the oil droplets were relatively small (mean diameter < 400 nm), with low dispersity (<0.25) and a high negative surface charge (−40 mV or less). These characteristics were obtained by homogenizing for 10 min at 10,000 rpm (W1/O), then 6000 rpm for 15 min, followed by microfluidization at 50 MPa.

Liposomal Mediated Carriers of α Lipoic Acid for the Treatment of Acute Lung Injury: Preclinical Study in Rat Model

2020 ◽  
Vol 10 (1) ◽  
pp. 53-57
Author(s):  
Yu Cao ◽  
Yanling Chai ◽  
Xiaoqun Niu ◽  
Bing Hai ◽  
Xiaojie He ◽  
...  
Keyword(s):  
Thin Film ◽  
Particle Size ◽  
Pulmonary Fibrosis ◽  
Lung Injury ◽  
Lipoic Acid ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Preclinical Study ◽  
Liposomal Formulation ◽  
Experimental Animals

The present investigation deals with formulation of lipoic acid as liposomal formulation and to evaluate its efficacy in Lung injury (Pulmonary Fibrosis). The liposomal formulation of Lipoic acid (LA-liposomes) was successfully prepared by thin film hydration method. Such prepared liposomes were characterized for particle size, encapsulation efficiency, drug loading etc. characteristic. An Pulmonary fibrosis was induced using Bleomycin experimental animals rats. The effect of LA liposomal formulation on pulmonary fibrosis was observed. The histopathological finding confirms the efficiency of formulation in attenuation of pulmonary fibrosis.

scholarly journals Casein Micelles as Nanocarriers for Benzydamine Delivery

Polymers ◽  
2021 ◽  
Vol 13 (24) ◽  
pp. 4357
Author(s):  
Nikolay Zahariev ◽  
Maria Marudova ◽  
Sophia Milenkova ◽  
Yordanka Uzunova ◽  
Bissera Pilicheva
Keyword(s):  
Particle Size ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Crosslinking Agent ◽  
Morphological Characteristics ◽  
Average Particle ◽  
Scanning Calorimetry ◽  
Casein Micelles ◽  
Fourier Transformed Infrared Spectroscopy

The aim of the present work was to optimize the process parameters of the nano spray drying technique for the formulation of benzydamine-loaded casein nanoparticles and to investigate the effect of some process variables on the structural and morphological characteristics and release behavior. The obtained particles were characterized in terms of particle size and size distribution, surface morphology, production yield and encapsulation efficiency, drug-polymer compatibility, etc., using dynamic light scattering, scanning electron microscopy, differential scanning calorimetry, and Fourier transformed infrared spectroscopy. Production yields of the blank nanoparticles were significantly influenced by the concentration of both casein and the crosslinking agent. The formulated drug-loaded nanoparticles had an average particle size of 135.9 nm to 994.2 nm. Drug loading varied from 16.02% to 57.41% and the encapsulation efficiency was in the range 34.61% to 78.82%. Our study has demonstrated that all the investigated parameters depended greatly on the polymer/drug ratio and the drug release study confirmed the feasibility of the developed nanocarriers for prolonged delivery of benzydamine.

Study on the Preparation of Repaglinide Chitosan Microspheres with Genipin

2013 ◽  
Vol 791-793 ◽  
pp. 252-255 ◽  
Author(s):  
Yue Zhang ◽  
Xian Xian Shi ◽  
Yi Feng Yu ◽  
Yong Xing Song
Keyword(s):  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Crosslinking Agent ◽  
Active Agent ◽  
Chemical Crosslinking ◽  
Coating Materials ◽  
Chitosan Microspheres ◽  
Chitosan Microsphere ◽  
Span 80

In this paper, the repaglinide chitosan microsphere crosslinked with genipin was prepared by emulsification-chemical crosslinking method, and chitosan is used as coating materials, genipin as a crosslinking agent, repaglinide as active agent, span-80 as emulsifier. The prepared microspheres were also characterized by SEM, IR and DSC. The encapsulation efficiency of repaglinide microsphere was 4.4% and the drug loading was 21.9%.

scholarly journals Development of a novel intraarticular injection of diclofenac for the treatment of arthritis: a preclinical study in the rabbit model

2021 ◽  
Author(s):  
Xinyuan Wen ◽  
Xiaoqing Huang ◽  
Huosheng Wu
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Rabbit Model ◽  
Intraarticular Injection ◽  
Average Particle ◽  
Prepared Nanoparticles

Purpose: To develop a novel intraarticular injection of diclofenac for the treatment of arthritis. Method: Diclofenac loaded nanoparticles were prepared by a nanoprecipitation technique using Eudragit L 100 as the polymer and polyvinyl alcohol as the surfactant. The nanoparticles were evaluated for particle size, zeta potential, scanning electron microscopy, drug release, encapsulation efficiency, and loading efficiency studies. The optimized nanoparticulate formulation was developed for intra articular injection. Intraarticulate injection was evaluated for pH, appearance, viscosity, osmolarity and syringability studies. The optimized injection formulation was tested in an arthritic model consisting of 25 rabbits. Result: Nanoprecipitation method was found to be suitable for diclofenac nanoparticles. The shape of the prepared nanoparticles was found to be spherical and devoid of any cracks and crevices. The average particle size of a diclofenac nanoparticle was found to range from 87±0.47 to 103±0.26 nm. The zeta potential of the prepared nanoparticles was found to be in the range of 0.598±0.34 to 0.826±0.25 mV. The encapsulation efficiency was found to be between 73.45% to 99.03%, while the drug loading was observed between 10.34 to 35.32%. The percentage drug release at 12 hours was found to range from 73.45% to 99.03%. Conclusion: The developed intraarticular injection was found to be within the physically and chemically accepted limits. Animals treated with the intra articular injection of diclofenac showed a significant reduction in swelling as compares to the other groups.

scholarly journals Polyethylene Glycol-Stabilized Zein Nanoparticles Containing Gallic Acid

2022 ◽  
Vol 60 (2) ◽  
Author(s):  
Heliton Augusto Wiggers ◽  
Margani Taise Fin ◽  
Najeh Maissar Khalil ◽  
Rubiana Mara Mainardes
Keyword(s):  
Antioxidant Activity ◽  
Polyethylene Glycol ◽  
Zeta Potential ◽  
Gallic Acid ◽  
Encapsulation Efficiency ◽  
Drug Carrier ◽  
Drug Loading ◽  
Polydispersity Index ◽  
Food Simulants ◽  
Mean Size

Research background. Gallic acid is a polyphenol presenting antioxidant and antitumor activities, however its use as a nutraceutical or drug is hindered by its low bioavailability. Zein is a natural protein found in corn and has been applied as nanoparticle for drug carrier. In this study, zein nanoparticles were obtained and stabilized with polyethylene glycol (PEG) as gallic acid carriers. Experimental approach. Nanoparticles were obtained by the liquid-liquid method and characterized in terms of mean size, polydispersity index, zeta potential, morphology, solid-state interactions, and encapsulation efficiency/drug loading. The stability of nanoparticles was evaluated in simulated gastrointestinal fluids and food simulants, and the antioxidant activity was determined by the scavenging of the 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical. Results and conclusions. Zein nanoparticles containing gallic acid were obtained and stabilized only in the presence of PEG. The optimal conditions originated nanoparticles with mean size <200 nm, low polydispersity index (<0.25) and negative zeta potential (20 mV). The gallic acid encapsulation efficiency was about 40 %, drug loading about 5 %, and the compound was encapsulated in an amorphous state. FTIR did not identify chemical interactions after gallic acid nanoencapsulation. Zein nanoparticles were more susceptible to release the gallic acid in gastric than intestinal simulated medium, however more than 50 % of drug content was protected from premature release. In food simulants, the gallic acid release from nanoparticles was prolonged and sustained. Moreover, the nanoencapsulation did not reduce the antioxidant activity of gallic acid. Novelty and scientific contribution. The results show the importance of PEG on the formation and properties of zein nanoparticles obtained by the liquid-liquid dispersion method. This study indicates PEG-stabilized zein nanoparticles are potential carriers for gallic acid delivery by the oral route to take advantage of its antioxidant properties and be applied both in the pharmaceutical and food industry.

Novel Formulation Development and Evaluation of Nanoparticles Based in Situ Gelling System for The Ophthalmic Delivery of Ciprofloxacin Hydrochloride

2015 ◽  
Vol 5 (4) ◽  
Author(s):  
Kranti Singh ◽  
Surajpal Verma ◽  
Shyam Prasad ◽  
Indu Bala
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Drug Loading ◽  
In Vitro Release ◽  
Formulation Development ◽  
Ciprofloxacin Hydrochloride ◽  
Potential Value ◽  
The Mean ◽  
In Situ Gelling

Ciprofloxacin hydrochloride loaded Eudragit RS100 nanoparticles were prepared by using w/o/w emulsification (multiple emulsification) solvent evaporation followed by drying of nanoparticles at 50°C. The nanoparticles were further incorporated into the pH-triggered in situ gel forming system which was prepared using Carbopol 940 in combination with HPMC as viscosifying agent. The developed nanoparticles was evaluated for particle size, zeta potential value and loading efficiency; nanoparticle incorporated in situ gelling system was evaluated for pH, clarity, gelling strength, rheological studies, in-vitro release studies and ex-vivo precorneal permeation studies. The nanopaticle showed the mean particle size varying between 263.5nm - 325.9 nm with the mean zeta potential value of -5.91 mV to -8.13 mV and drug loading capacity varied individually between 72.50% to 98.70% w/w. The formulation was clear with no suspended particles, showed good gelling properties. The gelling was quick and remained for longer time period. The developed formulation was therapeutically efficacious, stable and non-irritant. It provided the sustained release of drug over a period of 8-10 hours.

Formulation and In-vitro Evaluation of Chewable Tablets of Montelukast Sodium

2015 ◽  
Vol 5 (3) ◽  
Author(s):  
Laxman Devkota ◽  
Bhupendra Poudel ◽  
Junu Silwal
Keyword(s):  
In Vitro Release ◽  
Magnesium Stearate ◽  
Physical Parameters ◽  
Artificial Sweetener ◽  
Leukotriene Receptor Antagonist ◽  
Montelukast Sodium ◽  
Chewable Tablets ◽  
Leukotriene Receptor ◽  
Vitro Release

The objective of the present study is to develop chewable tablets containing different pharmaceutical compositions with simple manufacturing procedures using different excipients. Mannitols, L-HPC 11, Aspartame, Crospovidone, Crospovidone, Aerosil, and Magnesium Stearate are used as excipients for effective formulation of anti-asthmatic drug Montelukast. Montelukast is a selective, orally acting leukotriene receptor antagonist that is used for the treatment of asthma and seasonal allergic rhinitis. Montelukast chewable tablets were prepared by Direct Compression methods using suitable excipients. The chewable tablets were better presented using artificial sweetener Aspartame as flavouring agent. A total of forteen formulations were prepared and the granules were evaluated for pre-compression parameters. The formulated tablets were evaluated for post-compression parameters .The results showed that all the physical parameters were within the acceptable limits. The in vitro release study of all the formulations showed good release. The study concludes that aforementioned excipients can be used to design chewable montelukast sodium tablets.

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