Eudragit RS 100 microparticles containing 2-hydroxypropyl-β-cyclodextrin and glutathione: Physicochemical characterization, drug release and transport studies

2007 ◽  
Vol 30 (1) ◽  
pp. 64-74 ◽  
Author(s):  
Adriana Trapani ◽  
Valentino Laquintana ◽  
Nunzio Denora ◽  
Angela Lopedota ◽  
Annalisa Cutrignelli ◽  
...  
Keyword(s):  
Drug Release ◽  
Physicochemical Characterization ◽  
Eudragit Rs ◽  
Transport Studies

Formulation and Evaluation of Luliconazole Microsponges Loaded Gel for Topical Delivery

2021 ◽  
pp. 5775-5780
Author(s):  
Farhana Sultan ◽  
Himansu Chopra ◽  
Gyanendra Kumar Sharma
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Entrapment Efficiency ◽  
Topical Delivery ◽  
Production Yield ◽  
In Vitro Drug Release ◽  
Eudragit Rs ◽  
Diffusion Studies

Microsponge containing Luliconazole (LCZ) with different proportion of drug:polymer (Ethyl cellulose and Eudragit RS 100) were obtained efficiently using Quasi-emulsion solvent diffusion method. Luliconazole is an anti-fungal drug used for the topical delivery. The purpose of the microsponge formulation is to control the release of LCZ drug to the skin through Microsponge Delivery System (MDS) known to be the novel technique which overcome the maximum concentration of active ingredient, frequency doses, and skin irritation. The prepared microsponges were examined using drug content, % production yield, % entrapment efficiency and in-vitro drug release. The formulation were subjected to in-vitro drug release studies for 6 hr in which it was concluded that Ethyl cellulose microsponges formulated by drug:polymer (1:1) and Eudragit RS 100 microsponges formulated by drug:polymer (1:3) showed maximum controlled release i.e., Increase in drug:polymer ratio (1:1 to 1:9) increased the production yield and entrapment efficiency of microsponges using Ethyl cellulose with no significant effect for Eudragit RS 100.Therefore, both formulation F1 and F2 was dispersed in carbopol gel preparation for controlled delivery of LCZ to the skin. Various physical parameters like pH, spreadability, viscosity and in-vitro drug diffusion studies were evaluated for the prepared gel formulations. Microsponge gel formulation i.e., FG1 showed better results for controlled release of 89.40% as compared to FG2 i.e., 92.18% over the period of 12 hrs which is performed in Franz Diffusion Cell. On basis of in-vitro diffusion studies for LCZ gel formulation, microsponges using Ethyl cellulose (FG1) was found to be best for its controlled release of LCZ for 12 hrs and followed zero order kinetics. Hence, formulated LCZ loaded gel have potential to treat fungal infections i.e., tinea pedis, tinea cruris and tinea corporis.

scholarly journals In vitro Release Kinetics Study of Ambroxol Hydrochloride Pellets Developed by Extrusion Spheronization Technique Followed by Acrylic Polymer Coating

1970 ◽  
Vol 7 (1) ◽  
pp. 75-81 ◽  
Author(s):  
Ishtiaq Ahmed ◽  
Monzurul Amin Roni ◽  
Golam Kibria ◽  
Muhammad Rashedul Islam ◽  
Reza-ul Jalil
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Dissolution ◽  
Acrylic Polymer ◽  
Eudragit Rs ◽  
Methacrylate Copolymer ◽  
Ambroxol Hydrochloride ◽  
Eudragit Rl ◽  
Extrusion Spheronization

The aim of the present study was to investigate the effect of Ammonio Methacrylate Copolymer Dispersion Type A (Eudragit RL 30 D) and Ammonio Methacrylate Copolymer Dispersion Type B (Eudragit RS 30 D) combination in different weight ratios on the release kinetics of Ambroxol Hydrochloride from coated pellets. Microcrystalline cellulose, lactose, maize starch, hydroxypropyl methylcellulose and the drug was incorporated in the nuclei prepared by Extrusion-Spheronization technique which was coated with Eudragit RL 30D and Eudragit RS 30D in 1:1,1:1.5,1:2,1:2.5 and 1:3 ratios. The in vitro dissolution studies were carried out in 0.1N HCl for 1 hour followed by phosphate buffer (pH 6.8) for 11 h with USP dissolution apparatus Type-II. Drug release decreased with increasing amount of Eudragit RS 30 D in all cases. The drug release followed first order and Higuchi release kinetics. The Korsmeyer plot revealed n=0.50-0.61 or non-Fickian transport mechanism for drug release. From one way ANOVA it was found that the ratio of binary polymer mixer had significant (p < 0.05) effect on drug release. Key words: Aqueous coating, Eudragit, release kinetics, pellet, extrusion-spheronization  DOI = 10.3329/dujps.v7i1.1222 Dhaka Univ. J. Pharm. Sci. 7(1): 75-81, 2008 (June)

scholarly journals Novel Gliclazide Electrosprayed Nano-Solid Dispersions: Physicochemical Characterization and Dissolution Evaluation

2019 ◽  
Vol 9 (2) ◽  
pp. 231-240
Author(s):  
Khosro Adibkia ◽  
Solmaz Ghajar ◽  
Karim Osouli-Bostanabad ◽  
Niloufar Balaei ◽  
Shahram Emami ◽  
...  
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Amorphous State ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Peg 6000

Purpose: In the current study, electrospraying was directed as a novel alternative approach to improve the physicochemical attributes of gliclazide (GLC), as a poorly water-soluble drug, by creating nanocrystalline/amorphous solid dispersions (ESSs). Methods: ESSs were formulated using Eudragit® RS100 and polyethylene glycol (PEG) 6000 as polymeric carriers at various drug: polymer ratios (i.e. 1:5 and 1:10) with different total solution concentrations of 10, 15, and 20% w/v. Morphological, physicochemical, and in-vitro release characteristics of the developed formulations were assessed. Furthermore, GLC dissolution behaviors from ESSs were fitted to various models in order to realize the drug release mechanism. Results: Field emission scanning electron microscopy analyses revealed that the size and morphology of the ESSs were affected by the drug: polymer ratios and solution concentrations. The polymer ratio augmentation led to increase in the particle size while the solution concentration enhancement yielded in a fiber establishment. Differential scanning calorimetry and powder X-ray diffraction investigations demonstrated that the ESSs were present in an amorphous state. Furthermore, the in vitro drug release studies depicted that the samples prepared employing PEG 6000 as carrier enhanced the dissolution rate and the model that appropriately fitted the release behavior of ESSs was Weibull model, where demonstrating a Fickian diffusion as the leading release mechanism. Fourier-transform infrared spectroscopy results showed a probability of complexation or hydrogen bonding, development between GLC and the polymers in the solid state. Conclusion: Hence the electrospraying system avails the both nanosizing and amorphization advantages, therefore, it can be efficiently applied to formulating of ESSs of BCS Class II drugs.

scholarly journals MULTIPARTICULATE FLOATING DRUG DELIVERY SYSTEM OF ANAGLIPTIN: DESIGN AND OPTIMIZATION FOR ITS EFFICACY IN MANAGEMENT OF METABOLIC SYNDROME

2019 ◽  
pp. 171-181
Author(s):  
RAKESH V. MISHRA ◽  
SHASHIKANT N. DHOLE
Keyword(s):  
Metabolic Syndrome ◽  
Drug Release ◽  
Wistar Rats ◽  
Lag Time ◽  
Cafeteria Diet ◽  
High Density Lipoproteins ◽  
Eudragit Rs ◽  
The Metabolic Syndrome ◽  
Male Wistar Rats ◽  
Eudragit Rl

Objective: The present research aims to design and optimize gastroretentive floating pellets of anagliptin (a dipeptidyl peptidase-4 inhibitor), so as to reduce P-Glycoprotein (PGP)–mediated efflux in the intestine hence to improve oral bioavailability. Methods: The drug-containing core pellets were prepared by extrusion and spheronization process followed by subsequent coating with three successive layers i.e. Eudragit RS 100, sodium bicarbonate (NaHCO3): hydroxypropyl methylcellulose E5LV (HPMC E5LV) and Eudragit RL 100 using fluidized bed processor. A 3 level 3 factor box-behnken design was adopted to investigate the effect of Eudragit RS 100, NaHCO3: HPMC E5LVand Eudragit RL 100 on floating lag time and drug release at 10 h. Desirability function under numerical optimization technique was used to identify the optimum formulation. Results: The study reveals the significant effect of the amount of NaHCO3 and coating level of polymers on floating lag time and drug release. The optimum system could float within 4 min and exhibited more than 85% drug release in 10 h. The pharmacokinetic study conducted in male Wistar rats indicated 2.51 fold increase in relative bioavailability of optimized formulation compare to anagliptin drug. Formulated anagliptin pellets were evaluated in cafeteria diet-induced metabolic syndrome model in male Wistar rats. Anagliptin floating pellets treatment compared to cafeteria diet group significantly inhibited increase in body weight (238.79±2.52 g vs. 277.98±3.69 g, P<0.001), calorie intake (2283.99 kcal vs. 3086.05 kcal, P<0.05) and serum levels of total cholesterol (95.19±0.61 mg/dl vs. 110.04±1.31 mg/dl, P<0.01), triglycerides (96.12±1.25 mg/dl vs. 105.99±1.29 mg/dl, P<0.01) while high-density lipoproteins levels were improved (42.15±0.92 mg/dl vs. 30.92±0.77 mg/dl, P<0.01) indicated its hypophagic and anti-hyperlipidemic effects. Conclusion: The gastroretentive floating pellets of anagliptin was obtained and could be a promising technique to deliver anagliptin with improved bioavailability in the management of the metabolic syndrome.

The Synthesis and Characterization of PVA-Ketoprofen Cryogel, Biomaterial with Extended Drug Release Properties for Cartilage Replacement

2014 ◽  
Vol 216 ◽  
pp. 205-209
Author(s):  
Monica Cretan Stamate ◽  
Ciprian Stamate
Keyword(s):  
Articular Cartilage ◽  
Drug Release ◽  
Polyvinyl Alcohol ◽  
Water Solubility ◽  
Physicochemical Characterization ◽  
Gravimetric Method ◽  
Controlled Drug Release ◽  
High Wear Resistance ◽  
Mechanical Resistance ◽  
Swelling Properties

The present paper aims to study the possibility to modify the properties of polyvinyl alcohol (pva) cryogels prepared in the presence of ketoprofen in order to replace the damaged articular cartilage. Articular cartilage is the most important part of articulation characterized by very low friction, high wear resistance, and poor regenerative qualities. Polyvinyl alcohol is a non-expensive polymer, versatile and adaptable to various needs, with exceptional properties such as water solubility, biocompatibility, non-toxicity and with capability to form hydrogels by chemical or physical methods. The aims of this paper are the synthesis, the physicochemical characterization and analysis of the tribological properties of pva cryogels for cartilage replacement and the introduction of new concept in medication by creating the cryogel like a controlled drug release system. The morphology of the cryogels, the interaction between the pva macromolecular chains and medicament has been studied by Scanning Electronic Microscopy. The gels swelling in physiologic ser have been monitored by gravimetric method in order to evidence the hydrophilic properties. The mechanical properties of the cryogels have been investigated by dynamic mechanical measurements. In conclusion, the biomaterial obtained provides good swelling properties, mechanical resistance and it is ideal for extended drug release implantable systems.

Sign in / Sign up

Export Citation Format

Share Document