Preparation and characterization of water-soluble microcapsule for sustained drug release using Eudragit RS 100

2010 ◽  
Vol 18 (12) ◽  
pp. 1191-1194 ◽  
Author(s):  
Jeong-Min Park ◽  
Soo-Jin Park
2014 ◽  
Vol 2014 ◽  
pp. 1-13 ◽  
Author(s):  
Teresa Nabais ◽  
Grégoire Leclair

Substituted amylose (SA) polymers were produced from high-amylose corn starch by etherification of its hydroxyl groups with chloroacetate. Amorphous high-amylose sodium carboxymethyl starch (HASCA), the resulting SA polymer, was spray-dried to obtain an excipient (SD HASCA) with optimal binding and sustained-release (SR) properties. Tablets containing different percentages of SD HASCA and tramadol hydrochloride were produced by direct compression and evaluated for dissolution. Once-daily and twice-daily SD HASCA tablets containing two common dosages of tramadol hydrochloride (100 mg and 200 mg), a freely water-soluble drug, were successfully developed. These SR formulations presented high crushing forces, which facilitate further tablet processing and handling. When exposed to both a pH gradient simulating the pH variations through the gastrointestinal tract and a 40% ethanol medium, a very rigid gel formed progressively at the surface of the tablets providing controlled drug-release properties. These properties indicated that SD HASCA was a promising and robust excipient for oral, sustained drug-release, which may possibly minimize the likelihood of dose dumping and consequent adverse effects, even in the case of coadministration with alcohol.


2007 ◽  
Vol 57 (4) ◽  
pp. 413-427 ◽  
Author(s):  
Parauvathanahalli Rajinikanth ◽  
Brahmeshwar mishra

Preparation andin vitrocharacterization of gellan based floating beads of acetohydroxamic acid for eradication ofH. pyloriGellan based floating beads of acetohydroxamic acid (AHA) were prepared by the ionotropic gellation method to achieve controlled and sustained drug release for treatment ofHelicobacter pyloriinfection. The prepared beads were evaluated for diameter, surface morphology and encapsulation efficiency. Formulation parameters like concentrations of gellan, chitosan, calcium carbonate and the drug influenced thein vitrodrug release characteristics of beads. Drug and polymer interaction studies were carried out using differential scanning calorimetry. Chitosan coating increased encapsulation efficiency of the beads and reduced the initial burst release of the drug from the beads. Kinetic treatment of the drug release data revealed a matrix diffusion mechanism. Prepared floating beads showed good antimicrobial activity (in vitro H. pyloriculture) as potent urease inhibitors. In conclusion, an oral dosage form of floating gellan beads containing AHA may form a useful stomach site specific drug delivery system for the treatment ofH. pyloriinfection.


2014 ◽  
Vol 146 (2) ◽  
pp. 411-416 ◽  
Author(s):  
Amir Heydarinasab ◽  
Homayon Ahmad Panahi ◽  
Hamid Nematzadeh ◽  
Elham Moniri ◽  
Sara Nasrollahi

2011 ◽  
Vol 61 (2) ◽  
pp. 157-170 ◽  
Author(s):  
Ayrivan Puratchikody ◽  
Viswanadhan Prasanth ◽  
Sam Mathew ◽  
Balaraman Kumar

Development and characterization of mucoadhesive patches of salbutamol sulfate for unidirectional buccal drug delivery Buccal patches of salbutamol sulfate were prepared using five different water soluble polymers in various proportions and combinations using PEG-400/PG as plasticizers. A 32 full factorial design was used to design the experiments for each polymer combination. Patches were laminated on one side with a water impermeable backing layer for unidirectional drug release. The thickness of medicated patches ranged between 0.2 and 0.4 mm and showed an increase in mass whenever PEG-400 was used as plasticizer. The surface pH of all patches approached neutral. Eight formulations which had shown high folding endurance (> 300) were selected for evaluation. Patches prepared with PEG-400 showed a high swelling index. The residence time of the tested patches ranged between 105 and 130 min. Formulations A10, A32, B10 and B32 fitted the Higuchi model best, whereas formulations A19 and B19 showed super case II transport drug release. Stability studies indicated that there was no change in the chemical and physical characteristics during the test period of 6 months.


2007 ◽  
Vol 57 (1) ◽  
pp. 61-72 ◽  
Author(s):  
Vishnu Patel ◽  
Bhupendra Prajapati ◽  
Madhabhai Patel

Design and characterization of chitosan-containing mucoadhesive buccal patches of propranolol hydrochloride Mucoadhesive buccal patches containing propranolol hydrochloride were prepared using the solvent casting method. Chitosan was used as bioadhesive polymer and different ratios of chitosan to PVP K-30 were used. The patches were evaluated for their physical characteristics like mass variation, drug content uniformity, folding endurance, ex vivo mucoadhesion strength, ex vivo mucoadhesion time, surface pH, in vitro drug release, and in vitro buccal permeation study. Patches exhibited controlled release for a period of 7 h. The mechanism of drug release was found to be non-Fickian diffusion and followed the first-order kinetics. Incorporation of PVP K-30 generally enhanced the release rate. Swelling index was proportional to the concentration of PVP K-30. Optimized patches (F4) showed satisfactory bioadhesive strength of 9.6 ± 2.0 g, and ex vivo mucoadhesion time of 272 minutes. The surface pH of all patches was between 5.7 and 6.3 and hence patches should not cause irritation in the buccal cavity. Patches containing 10 mg of drug had higher bioadhesive strength with sustained drug release as compared to patches containing 20 mg of drug. Good correlation was observed between the in vitro drug release and in vitro drug permeation with a correlation coefficient of 0.9364. Stability study of optimized patches was done in human saliva and it was found that both drug and buccal patches were stable.


2016 ◽  
Vol 4 (4) ◽  
pp. 760-767 ◽  
Author(s):  
Liping wu ◽  
Liyan Qiu

CA4P-loaded microspheres (CA4P-MS) composed of PELA reverse micelles (CA4P-RM) and PLGA with a sea-island structure were prepared. This unique type of construction can greatly improve the encapsulation efficiency of water-soluble CA4P and provide sustained drug release and action for cancer therapy.


2019 ◽  
pp. 23-28
Author(s):  
Hoang Nhan Ho ◽  
Ngoc Tuan Hoang ◽  
Thi Minh Nguyet Le

Background: Clotrimazole (CLO) is an imidazole derivative with antifungal activities. The conventional dosage forms for oral or topical administration have some disadvantages such as drug adverse reaction for long-term use, repeated doses daily due to short half-life. The aim of this study was to prepare gel containing CLO-loaded nanoparticles to increase drug solubility, enhance bioavailability, especially for a sustained drug release. Materials and methods: Eudragit RS 100 nanoparticles were prepared by the nanoprecipitation method, then was mixed with gel forming excipient. Gel containing CLO-loaded nanoparticles was characterized in terms of appearance, pH, particle size, PDI, encapsulation efficiency (EE), in vitro drug release. Results: The best formulation of gel containing 1% of CLO-loaded nanoparticles with 0.3% of Carbopol 934P, 5% of glycerin was smooth, homogenous, and particle size, PDI, EE, drug release of 154.6 ± 3.6 nm, 0.153 ± 0.011, 67.62 ± 0.89%, 51.46 ± 1.10% (after 24 hours). Conclusion: Gel containing CLO-loaded nanoparticles is a promising drug delivery system for the topical treatment of fungal infections. Key words: clotrimazole, Eudragit RS 100, fungal infection, nanoparticle, topical treatment


Pharmaceutics ◽  
2020 ◽  
Vol 12 (1) ◽  
pp. 51 ◽  
Author(s):  
Xu Liu ◽  
Xingyu Lu ◽  
Yongchao Su ◽  
Eucharist Kun ◽  
Feng Zhang

Clay–polymer nanocomposites have exhibited a great potential as carriers for controlled release drug delivery. This study aims to prepare exfoliated montmorillonite–Eudragit RS nanocomposites using reactive melt extrusion and investigate the influence of claying loading, clay types (sodium montmorillonite (Cloisite Na) vs. organomodified montmorillonite (Cloisite 20)) on clay–polymer interactions and drug release properties. The clays were used as the filler material at various levels in Eudragit RS and theophylline was used as the active pharmaceutical ingredient. The resulting structure of the nanocomposites was characterized using TEM (transmission electron microscopy) and XRPD (X-ray powder diffraction). The hygroscopicity of the nanocomposites was investigated using DVS (dynamic vapor sorption). The effect of the interfacial interaction between the polymer and clay sheet, the clay loading as well as the clay type on the drug release behavior were further studied by dissolution testing. TEM and XRPD data show that when the clay content is increased from 5% to 15% by weight, the nanocomposite’s structure switches from a fully exfoliated state to intercalated structures or partial exfoliation with stacked clay layers. FT-IR (fourier transform infrared spectroscopy) and ssNMR (solid-state NMR) results suggest that Cloisite Na and Cloisite 20 layers exhibit different interaction strengths with polymer networks by creating compacted complex structures. The addition of nanoclay in the formulation could robustly adjust drug release profiles, and the clay concentration and type are important factors that affect the crossing-linking density of the nanocomposites by adjusting the drug release properties. This study indicates that the clay–Eudragit RS nanocomposites provide an improved oral controlled drug delivery system that minimizes the drug dosing frequency, potentially leading to improved patient compliance.


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