scholarly journals pH-Sensitive Alginate/Carboxymethyl Chitosan/Aminated Chitosan Microcapsules for Efficient Encapsulation and Delivery of Diclofenac Sodium

Pharmaceutics ◽  
2021 ◽  
Vol 13 (3) ◽  
pp. 338
Author(s):  
Ahmed M. Omer ◽  
Maha S. Ahmed ◽  
Gehan M. El-Subruiti ◽  
Randa E. Khalifa ◽  
Abdelazeem S. Eltaweil

To develop an effective pH-sensitive drug carrier, alginate (Alg), carboxymethyl chitosan (CMCs), and aminated chitosan (AmCs) derivatives were employed in this study. A simple ionic gelation technique was employed to formulate Alg-CMCs@AmCs dual polyelectrolyte complexes (PECs) microcapsules as a pH-sensitive carrier for efficient encapsulation and release of diclofenac sodium (DS) drug. The developed microcapsules were characterized by Fourier transform infrared spectroscopy (FT-IR), thermogravimetric analyzer (TGA), and scanning electron microscope (SEM). The results clarified that formation of dual PECs significantly protected Alg microcapsules from rapid disintegration at colon conditions (pH 7.4), and greatly reduced their porosity. In addition, the dual PECs microcapsules can effectively encapsulate 95.4% of DS-drug compared to 86.3 and 68.6% for Alg and Alg-CMCs microcapsules, respectively. Higher DS-release values were achieved in simulated colonic fluid [SCF; pH 7.4] compared to those obtained in simulated gastric fluid [SGF; pH 1.2]. Moreover, the drug burst release was prevented and a sustained DS-release was achieved as the AmCs concentration increased. The results confirmed also that the developed microcapsules were biodegradable in the presence of the lysozyme enzyme. These findings emphasize that the formulated pH-sensitive microcapsules could be applied for the delivery of diclofenac sodium.

2019 ◽  
Vol 16 (12) ◽  
pp. 4954-4959
Author(s):  
Norsyazwani Solehah Norudin ◽  
Hajaratul Najwa Mohamed ◽  
Nor Aisyah Mat Yahya

Recently, a lot of strategies have been developed to enhance oral protein delivery. The combination of biodegradable polymer which is alginate-inulin as the material for hydrogel matrices was studied as a carrier of BSA which was used as a model protein. The effects of different formulations on the BSA release profile in physiological saline was investigated. Meanwhile, the compatibility of protein and polymer was characterized by FT-IR spectroscopy. High BSA encapsulation efficiency was found with the increase of inulin amount in the hydrogel matrices. The BSA release pattern showed that the minor released of BSA in simulated gastric fluid, SGF pH (1.2) throughout 2 hours’ incubation and after changing the solution into simulated intestinal fluid, SIF pH (7.4) the protein release started to increase gradually up to 100% within 90 minutes. Incorporation of inulin in the alginate beads also resulted in improved BSA release in physiological saline solution. In addition, swelling behavior revealed that highest swelling rate of hydrogel was in alkali solution indicating that alginate-inulin hydrogels were influenced by the pH of test medium. The FT-IR results show that encapsulating matrices are compatible with protein and can be used as drug carrier. Therefore, the alginate-inulin hydrogel showing a good efficiency in oral administration of protein drug.


2012 ◽  
Vol 560-561 ◽  
pp. 434-437 ◽  
Author(s):  
Lan Wang ◽  
Wen Ji Guo ◽  
Yan Zhao Zhao

The objective of this paper was to prepare the composite of crefradine/montmorillionite in the method of solution intercalation. The drug load and intercalation rate varied with the drug concentration. X-ray diffraction (XRD), Fourier transformed infrared (FT-IR) Spectroscopy, and thermal analysis (TG-DSC) were applied to characterize composite mentioned above. Together with drug release tests, results indicate cefradine intercalated into montmorillionite.The release profiles of cefradine/MMT in simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 7.4) at 37°Cduring 10h are shown in Fig. 4. The amount of cefradine in the beginning 2h came up to 35% and 50%, and in the following time, cefradine released slowly. The release behaviors met the requirements of sustained release.


Materials ◽  
2020 ◽  
Vol 13 (7) ◽  
pp. 1624
Author(s):  
Lili Qin ◽  
Xinyu Zhao ◽  
Yiwei He ◽  
Hongqiang Wang ◽  
Hanjing Wei ◽  
...  

Resveratrol is a natural active ingredient found in plants, which is a polyphenolic compound and has a variety of pharmaceutical uses. Resveratrol-loaded TEMPO-oxidized cellulose aerogel (RLTA) was prepared using a freeze-drying method, employing high speed homogenization followed by rapid freezing with liquid nitrogen. RLTAs were designed at varying drug–cellulose aerogel ratios (1:2, 2:3, 3:2, and 2:1). It could be seen via scanning electron microscopy (SEM) that Res integrated into TEMPO-oxidized cellulose (TC) at different ratios, which changed its aggregation state and turned it into a short rod-like structure. Fourier transform infrared (FTIR) spectra confirmed that the RLTAs had the characteristic peaks of TC and Res. In addition, X-ray diffraction (XRD) demonstrated that the grain size of RLTA was obviously smaller than that of pure Res. RLTAs also had excellent stability in both simulated gastric fluid and phosphate buffer solution. The drug release rate was initially completed within 5 h under a loading rate of 30.7 wt%. The results of an MTT assay showed the low toxicity and good biocompatibility of the RLTAs. TC aerogel could be a promising drug carrier that may be widely used in designing and preparing novel biomedicine.


2019 ◽  
Author(s):  
Fatimah. A. Agili ◽  
Sahera. F. Mohamed

AbstractThe pH-sensitive nanocomposite composed of sodium alginate/ Pectin/ Tannic acid – silver SA/Pec/TA-Ag was prepared using microwave irradiation and employed as a carrier for Propranolol drug. Physico-chemical characteristics of the prepared systems using Fourier Transform Infrared Spectroscopy (FTIR), X-ray Diffraction (XRD), Field Emission Scanning Electron Microscope (FESEM), High-Resolution Transmission Electron Microscope (HRTEM), Dynamic light Scattering instrument (DLS), and Energy Dispersive X-Ray Analysis (EDX). The percentage drug release was 96% at pH 7.4 within 420 min. The drug release data was fitted into different kinetic models included zero order, First order, Higuchi and Ritger-Peppas model. The release mechanism is non-Fickian character where it controlled by diffusion and relaxation of polymer chains. It can be concluded that SA/Pec/TA-Ag nanocomposite is candidate for the oral drug carrier specific for intestinal system and has stability against gastric fluid.


1970 ◽  
Vol 2 ◽  
pp. 42-48
Author(s):  
Md Mosharaf Miazi ◽  
M Mohiuddinn A Choudhury ◽  
M Habibur Rahman ◽  
Abedur Rahman

The objective of this study was to evaluate the effects of magnesium hydroxide (MH) on disintegration time (DT) and dissolution profile of diclofenac sodium (DS) plain tablet. The tablets of DS were formulated with conventionally used excipients and investigational agent Mg [OH]2. Different parameters of tablets like hardness, thickness, friability, and disintegration time and dissolution rate were determined to assess the effects of MH on these parameters. The physical resistance against abrasion or shock of DS-MH tablets had been noticed by the results of hardness and friability test which were within the limits of standard specification. The disintegration times of tablets of the experimental batches except one, found 2.0 to 25 minutes were also within the limits of standard specification. The release rates of DS in simulated gastric fluid (SGF) at 30 minutes were inspiring about batches FO3: 84.78% and FO4: 90.38%. A positive correlation of coefficient determined between quantity of Mg(OH)2 in different batches of tablets and their effects on dissolution rate was found statistically significant (r = 0.66). The tmax of DS was not affected by the presence or increment of MH as evident in rtmax= 0.50. The overall study indicated that Magnesium hydroxide didn't affect the different physical parameters of plain tablet rather it in certain quantity while present in some batches assisted rapid disintegration and release profile of active content Diclofenac sodium. The DS-MH plain tablet to provide rapid disintegration, dissolution and absorption hence fastest anti-inflammatory action with acid neutralizing benefits by MH, might be considered sincerely Key words: Diclofenac Sodium; Magnesium Hydroxide; Disintegration; Dissolution DOI:10.3329/jbsp.v2i0.984 J Bangladesh Soc Physiol. 2007 Dec;(2): 42-48.    


2014 ◽  
Vol 936 ◽  
pp. 751-756 ◽  
Author(s):  
Yuan Yuan Liang ◽  
Tong Chen ◽  
Yu Qin Cui ◽  
Rui Qiong Tian ◽  
Tong Sheng Qi ◽  
...  

To accelerate the response rate of smart hydrogels to the environmental conditions, a novel pH-sensitive hydrogel microsphere with the controlled shapes and sizes were developed. Such monodispersed microspheres were synthesizedviafree radical polymerization under the protection of a multilayer stability system. The pH-responsibility of hydrogel microspheres was tested with the hydrogel bulk as a control.In vitrorelease studies were conducted in the simulated gastric fluid and intestinal juice with bovine serum albumin (BSA) as a model drug. The large specific surface areas endowed hydrogel microspheres a faster pH-responsibility than that of bulk ones. Therefore, such microspheres showed potential applications as the oral protein drugs carrier.


Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 842
Author(s):  
Cassiele T. Cesco ◽  
Artur J. M. Valente ◽  
Alexandre T. Paulino

Chitosan/DNA blend hydrogel (CDB) and chitosan/pectin blend hydrogel (CPB) were synthesized using an emulsion (oil-in-water) technique for the release of methylene blue (model molecule). Both hydrogels were characterized by swelling assays, Fourier transform infrared (FT-IR) spectroscopy, thermogravimetric analysis (TGA) and scanning electron microscopy (SEM), before and after the methylene blue (MB) loading. Higher swelling degrees were determined for both hydrogels in simulated gastric fluid. FT-IR spectra inferred absorption peak changes and shifts after MB loading. The TGA results confirmed changes in the polymer network degradation. The SEM images indicated low porosities on the hydrogel surfaces, with deformed structure of the CPB. Smoother and more uniform surfaces were noticed on the CDB chain after MB loading. Higher MB adsorption capacities were determined at lower initial hydrogel masses and higher initial dye concentrations. The MB adsorption mechanisms on the hydrogel networks were described by the monolayer and multilayer formation. The MB release from hydrogels was studied in simulated gastric and intestinal fluids, at 25 °C and 37 °C, with each process taking place at roughly 6 h. Higher release rates were determined in simulated gastric fluid at 25 °C. The release kinetics of MB in chitosan/DNA and chitosan/pectin matrices follows a pseudo-second-order kinetic mechanism.


2017 ◽  
Vol 58 (4) ◽  
Author(s):  
José Manuel Cornejo-Bravo ◽  
Víctor Gómez Reséndiz ◽  
Aracely Serrano-Medina ◽  
Eugenia Gabriela Carrillo-Cedillo ◽  
Manuel Cornejo

<p>Poly(methacryloiloxy-<em>o</em>-benzoic acid), an amphiphilic weak polyelectrolyte was bound by secondary forces to cationic drugs (propranolol. HCl and labetalol.HCl) to form water-insoluble complexes that release the bound drug only in ionic media. Compressed tablets were prepared from the polymer-drug complexes formed. The complex with propranolol suffers a fast release in simulated gastric fluid (pH 1.2), but presents a diffusion controlled release at pH 6.8 and 7.4. Moreover, the complex with labetalol (a less water soluble drug) presents controlled release at the three pH values studied. In this case, release is controlled by the erosion of the tablets. The results indicate that PMAOB is a good carrier for oral release of poorly soluble cationic drugs.</p>


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