Polyelectrolyte complexes of carboxymethyl chitosan/alginate based drug carrier for targeted and controlled release of dual drug

2019 ◽  
Vol 51 ◽  
pp. 569-582 ◽  
Author(s):  
T.S. Anirudhan ◽  
Chithra Sekhar V. ◽  
Syam S. Nair
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.


2020 ◽  
Vol 20 (16) ◽  
pp. 1966-1980
Author(s):  
Jaleh Varshosaz ◽  
Saeedeh Fardshouraki ◽  
Mina Mirian ◽  
Leila Safaeian ◽  
Setareh Jandaghian ◽  
...  

Background: Using imatinib, a tyrosine kinase inhibitor drug used in lymphoblastic leukemia, has always had limitations due to its cardiotoxicity and hepatotoxicity side effects. The objective of this study is to develop a target-oriented drug carrier to minimize these adverse effects by the controlled release of the drug. Methods: KIT-5 nanoparticles were functionalized with 3-aminopropyltriethoxysilane and conjugated to rituximab as the targeting agent for the CD20 positive receptors of the B-cells. Then they were loaded with imatinib and their physical properties were characterized. The cell cytotoxicity of the nanoparticles was studied by MTT assay in Ramos (CD20 positive) and Jurkat cell lines (CD20 negative) and their cellular uptake was shown by fluorescence microscope. Wistar rats received an intraperitoneal injection of 50 mg/kg of the free drug or targeted nanoparticles for 21 days. Then the level of aspartate Aminotransferase (AST), alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP) and Lactate Dehydrogenase (LDH) were measured in serum of animals. The cardiotoxicity and hepatotoxicity of the drug were also studied by hematoxylin and eosin staining of the tissues. Results: The targeted nanoparticles of imatinib showed to be more cytotoxic to Ramos cells rather than Jurkat cells. The results of the biochemical analysis displayed a significant reduction in AST, ALT, ALP, and LDH levels in animals treated with targeted nanoparticles, compared to the free drug group. By comparison with the free imatinib, histopathological results represented less cardiotoxicity and hepatotoxicity in the animals, which received the drug through the current designed delivery system. Conclusion: The obtained results confirmed that the rituximab targeted KIT-5 nanoparticles are promising in the controlled release of imatinib and could decrease its cardiotoxicity and hepatotoxicity side effects.


2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chukwuebuka H. Ozoude ◽  
Chukwuemeka P. Azubuike ◽  
Modupe O. Ologunagba ◽  
Sejoro S. Tonuewa ◽  
Cecilia I. Igwilo

Abstract Background Khaya gum is a bark exudate from Khaya senegalensis (Maliaecae) that has drug carrier potential. This study aimed to formulate and comparatively evaluate metformin-loaded microspheres using blends of khaya gum and sodium alginate. Khaya gum was extracted and subjected to preformulation studies using established protocols while three formulations (FA; FB and FC) of metformin (1% w/v)-loaded microspheres were prepared by the ionic gelation method using 5% zinc chloride solution as the cross-linker. The formulations contained 2% w/v blends of khaya gum and sodium alginate in the ratios of 2:3, 9:11, and 1:1, respectively. The microspheres were evaluated by scanning electron microscopy, Fourier transform-infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, swelling index, and in vitro release studies. Results Yield of 28.48%, pH of 4.00 ± 0.05, moisture content (14.59% ± 0.50), and fair flow properties (Carr’s index 23.68 ± 1.91 and Hausner’s ratio 1.31 ± 0.03) of the khaya gum were obtained. FTIR analyses showed no significant interaction between pure metformin hydrochloride with excipients. Discrete spherical microspheres with sizes ranging from 1200 to 1420 μm were obtained. Drug entrapment efficiency of the microspheres ranged from 65.6 to 81.5%. The release of the drug from microspheres was sustained for the 9 h of the study as the cumulative release was 62% (FA), 73% (FB), and 80% (FC). The release kinetics followed Korsmeyer-Peppas model with super case-II transport mechanism. Conclusion Blends of Khaya senegalensis gum and sodium alginate are promising polymer combination for the preparation of controlled-release formulations. The blend of the khaya gum and sodium alginate produced microspheres with controlled release properties. However, the formulation containing 2:3 ratio of khaya gum and sodium alginate respectively produced microspheres with comparable controlled release profiles to the commercial brand metformin tablet.


2017 ◽  
Vol 109 (2) ◽  
pp. 178-185 ◽  
Author(s):  
Azadeh Fakharmanesh ◽  
Hossein Tavanai ◽  
Taghi Khayamian ◽  
Mohammad Morshed

2016 ◽  
Vol 31 (4) ◽  
pp. 434 ◽  
Author(s):  
ZHU Kai-Ping ◽  
SUN Jing ◽  
YE Song ◽  
ZHOU Jie ◽  
WANG Hui ◽  
...  

Foods ◽  
2020 ◽  
Vol 9 (11) ◽  
pp. 1604
Author(s):  
Yu Xiao ◽  
Chi-Tang Ho ◽  
Yulian Chen ◽  
Yuanliang Wang ◽  
Zihao Wei ◽  
...  

Genistein is one of major isoflavones derived from soybean products and it is believed to have beneficial effects on human health. However, its low water-solubility and poor oral bioavailability severely hamper its use as a functional food ingredient or for pharmaceutical industry. In this study, zein and zein/carboxymethyl chitosan (CMCS) nanoparticles were prepared to encapsulate genistein using a combined liquid–liquid phase separation method. The physicochemical properties of fabricated nanoparticles were characterized by dynamic light scattering (DLS), atomic force microscopy (AFM), and Fourier transform infrared spectroscopy (FTIR). The results demonstrated that genistein encapsulated with zein nanoparticles significantly improved its water dispersibility, antioxidant activity in the aqueous phase, and photostability against UV light. Moreover, genistein encapsulated in zein nanoparticles showed a sustained release property. Furthermore, it was found that encapsulation efficiency of genistein was significantly enhanced after CMCS coating, and this effect was more pronounced after the complex nanoparticles cross-linked with calcium ions when compared with the use of zein as a single encapsulant. In addition, compared to zein nanoparticles without biopolymer coating, CMCS coating significantly enhanced the thermal and storage stability of the formed nanoparticles, and delayed the release of genistein. A schematic diagram of zein and zein/carboxymethyl chitosan (CMCS) nanoparticles formation mechanism for encapsulation of genistein was proposed. According to the results of the current study, it could be concluded that encapsulation of genistein in zein/CMCS nanoparticles is a promising approach to improve its water dispersibility, antioxidant activity, photostability against UV light and provide controlled release for food/pharmaceutical applications.


2020 ◽  
Vol 8 (22) ◽  
pp. 6212-6224
Author(s):  
Feng Tian ◽  
Bin Chi ◽  
Chen Xu ◽  
Caixue Lin ◽  
Zushun Xu ◽  
...  

Drug resistance and side effects are the two main problems of chemotherapy.


Fibers ◽  
2019 ◽  
Vol 7 (6) ◽  
pp. 56 ◽  
Author(s):  
Nafeesa Mohd Kanafi ◽  
Norizah Abdul Rahman ◽  
Nurul Husna Rosdi ◽  
Hasliza Bahruji ◽  
Hasmerya Maarof

The potential use of carboxymethyl sago pulp (CMSP) extracted from sago waste for producing hydrogel nanofibers was investigated as a methylene blue drug carrier. Sago pulp was chemically modified via carboxymethylation reaction to form carboxymethyl sago pulp (CMSP) and subsequently used to produce nanofibers using the electrospinning method with the addition of poly(ethylene oxide) (PEO). The CMSP nanofibers were further treated with citric acid to form cross-linked hydrogel. Studies on the percentage of swelling following the variation of citric acid concentrations and curing temperature showed that 89.20 ± 0.42% of methylene blue (MB) was loaded onto CMSP hydrogel nanofibers with the percentage of swelling 4366 ± 975%. Meanwhile, methylene blue controlled release studies revealed that the diffusion of methylene blue was influenced by the pH of buffer solution with 19.44% of MB released at pH 7.34 within 48 h indicating the potential of CMSP hydrogel nanofibers to be used as a drug carrier for MB.


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