Preparation, Optimization and In vitro Evaluation of Glipizide Nanoparticles Integrated with Eudragit RS-100

Saharan, Priyanka; Bahmani, Kavita; Saharan, Sameer

doi:10.2174/2211738507666190319124513

Cited by 20 publications

(9 citation statements)

References 29 publications

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“…Average hydrodynamic diameter of microsphere formulation was evaluated using Zetasizer (Malvern Instruments, UK) and size found to be 0.5-0.6 µm that is within the range of microsphere size (0.5-1000 µm). This result is in good compliance with the findings by Saharan et al [23].…”

Section: Particle Size Analysissupporting

confidence: 94%

Gastroretentive floating microspheres for the management hypertension based on drug combination of amlodipine /losartan

Ali

Aamir

Khalid³

et al. 2022

JCP

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Background: Hypertension is one of the serious global health issues that affect millions of people and leads to cardiovascular damage if remain untreated. Various antihypertensive drugs have been developed but it is difficult to achieve better control of blood pressure by using mono-therapy so in this research work, combination therapy having sustained effect for the treatment of hypertension was developed. Method: Gastroretentive floating microspheres of amlodipine besylate and losartan potassium were formulated for the purpose of increasing the time of retention of drugs in the upper gastrointestinal tract and ultimately extend drug release. Eudragit RS100 was used as release controlling agent. The method adopted to prepare microspheres was solvent extraction. Formulated microspheres after that tested for assessing flow properties, buoyancy (%), percentage yield, drug release, surface morphology, by FTIR drug and polymer compatibility, size analysis and entrapment efficiency. Release kinetics on cumulative release data were applied. Results: It was observed from the findings that all the formulation remained buoyant in 1.2 pH buffer up to 12 hrs. It was also found that release of drug from formulation was prolonged which indicates sustained effect of dosage form. All the other results were satisfactory and it was also found that entrapment efficiency of formulation increased when concentration of polymer increased. On the basis of results, formulation 1 with 1:1 drug polymer ratio was selected as optimum formulation. Conclusion: It was concluded from the study that gastroretentive floating microspheres could be a one of best approach to extend the release of drug delivery system.

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Section: Particle Size Analysissupporting

confidence: 94%

Gastroretentive floating microspheres for the management hypertension based on drug combination of amlodipine /losartan

Ali

Aamir

Khalid³

et al. 2022

JCP

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“…When the results obtained according to DDSolver criteria are examined; release kinetics of all formulations were fitted to Korsmeyer-Peppas model. Korsmeyer-Peppas model indicated that drug release followed a combination of diffusion as well as erosion mechanisms [8]. The n values of 0.280 and 0.212 for NP-1 and NP-2 coded NP formulation, respectively.…”

Section: In Vitro Release and Release Kinetic Evaluationmentioning

confidence: 95%

“…Many polymers with natural or synthetic origin are used in the production of NPs. One of the synthetic ones is Eudragit RS 100 (ERS) [8]. ERS is a co-polymer of poly (ethyl acrylate, methyl-methacrylate, and chloro-trimethyl-ammonio-ethyl methacrylate).…”

Section: Introductionmentioning

confidence: 99%

Design of cefaclor monohydrate containing nanoparticles with extended antibacterial effect by Nano-Spray dryer: A Nanoenglobing study

Öztürk¹,

Aygül²

2020

jrp

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Spray drying is an important method used in pharmaceutical product manufacturing for many years. The nano-spray dryer developed in recent years provides ultrafine powders at nanoscale and high product yields. In this study, which was aimed at prolonged release in oral use, nanoparticles-(NPs) were obtained by nanoenglobation of cefaclor monohydrate-(CEF) with Eudragit RS 100-(ERS) with the help of nano-spray drying method. The particle size (PS) of the blank formulation was 186 nm whereas PSs of CEF containing NPs were between 328 and 389 nm. The average PDI of all NP formulations were below 0.4 and all prepared NPs had a positive ZP value. The encapsulation efficiency values were a range of 78-84 %. In vitro release studies of NPs showed extended-release up to 24 hours after the first 3 hours of burst effect. The results showed that the release kinetics were fitted to the Korsmeyer-Peppas model. As a result, it was found that all pharmaceutical technology analysis results were affected by the solid concentration ratio in the feed dispersion. Antibacterial activity of NP formulations was determined by microdilution method. After minimum inhibitory concentration (MIC) determination, time-dependent activity for NP-2 was investigated by the time-kill method. MIC value for NP-2 was 4-fold lower than MIC value of CEF for Staphylococcus aureus and Escherichia coli. No growth was observed for both bacteria with NP-2 during 18 hours incubation in the time-kill method. As a result, prolonged antibiotic release and long-term antibacterial activity were obtained by NP-2, the optimum formulation of our study.

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“…BH can not only be adsorbed on the surface of Mt but also be exchanged with intercalated Na + to generate Mt-drug complex (Mt-BH) carriers (Zhao et al, 2019 ). Eudragit polymers are a type of ammonium methacrylate copolymer with permeabilities and release parameters that can be conveniently adjusted by changing the proportions of the Eudragit RS/RL mixtures (Singh et al, 2011 ; Saharan et al, 2019 ).…”

Section: Introductionmentioning

confidence: 99%

Wettability and contact angle affect precorneal retention and pharmacodynamic behavior of microspheres

Liu

Han

et al. 2021

Drug Delivery

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In the present study, we describe the development of betaxolol hydrochloride and montmorillonite with ion exchange in a single formulation to create a novel micro-interactive dual-functioning sustained-release delivery system (MIDFDS) for the treatment of glaucoma. Betaxolol hydrochloride molecule was loaded onto the montmorillonite by ion exchange and MIDFDS formation was confirmed by XPS data. MIDFDS showed similar physicochemical properties to those of Betoptic, such as particle size, pH, osmotic pressure, and rheological properties. Nevertheless, the microdialysis and intraocular pressure test revealed better in vivo performance of MIDFDS, such as pharmacokinetics and pharmacodynamics. With regards to wettability, MIDFDS had a larger contact angle (54.66 ± 5.35°) than Betoptic (36.68 ± 1.77°), enabling the MIDFDS (2.93 s) to spread slower on the cornea than Betoptic (2.50 s). Moderate spreading behavior and oppositely charged electrostatic micro-interactions had a comprehensive influence on micro-interactions with the tear film residue, resulting in a longer precorneal retention time. Furthermore, MIDFDS had a significant sustained-release effect, with complete release near the cornea. The dual-functioning sustained-release carrier together with prolonged pre-corneal retention time (80 min) provided sufficiently high drug concentrations in the aqueous humor to achieve a more stable and long-term IOP reduction for 10 h. In addition, cytotoxicity and hemolysis tests showed that MIDFDS had better biocompatibility than Betoptic. The dual-functioning microspheres presented in this study provide the possibility for improved compliance due to low cytotoxicity and hemolysis, which suggests promising clinical implications.

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Preparation, Optimization and In vitro Evaluation of Glipizide Nanoparticles Integrated with Eudragit RS-100

Cited by 20 publications

References 29 publications

Gastroretentive floating microspheres for the management hypertension based on drug combination of amlodipine /losartan

Gastroretentive floating microspheres for the management hypertension based on drug combination of amlodipine /losartan

Design of cefaclor monohydrate containing nanoparticles with extended antibacterial effect by Nano-Spray dryer: A Nanoenglobing study

Wettability and contact angle affect precorneal retention and pharmacodynamic behavior of microspheres

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