scholarly journals Ionotropic Gelation Synthesis of Chitosan-Alginate Nanodisks for Delivery System and In Vitro Assessment of Prostate Cancer Cytotoxicity

2020 ◽  
Vol 2020 ◽  
pp. 1-10 ◽  
Author(s):  
David Patiño-Ruiz ◽  
Leandro Marrugo ◽  
Niradiz Reyes ◽  
María Acevedo-Morantes ◽  
Adriana Herrera

We report on the synthesis of chitosan-alginate nanodisks (Cs-Al NDs) using a simple approach consisting of the ionotropic gelation method. Sodium tripolyphosphate (STPP) was used as crosslinking agent to promote the electrostatic interaction between amine groups the chitosan and hydroxyl and carboxyl groups of alginate. Scanning electron microscopy (SEM) images provided direct evidence of the morphology of the nanodisks where agglomeration was observed due to the electrostatic interaction between the functional groups. Furthermore, dynamic light scattering (DLS) showed that the hydrodynamic size of the Cs-Al NDs was 227 nm and 152 nm in pH 1.2 and pH 7.4, respectively, which is in agreement with the information observed in the SEM images. The chemical structure is presented mainly the amine and carboxyl groups due to the presence of chitosan and alginate in the nanodisks, respectively, which allow the electrostatic interaction through N-H linkages. According to the X-ray diffraction, we found that the Cs-Al NDs exhibited the typical structure of chitosan and alginate, which lead the formation of polyelectrolyte complexes. We also evaluated the encapsulation of amoxicillin in the nanodisk, obtaining a loading efficiency of 74.98%, as well as a maximum in vitro release amount of 63.2 and 52.3% at pH 1.2 and 7.4, respectively. Finally, the cytotoxicity effect of the Cs-Al nanodisks was performed in human prostatic epithelial PWR-1E and Caucasian prostate adenocarcinoma PC-3 cell lines, in which the cell viability was above 80% indicating low inhibition and determining the Cs-Al NDs as a promising technology for controlled delivery systems.

2018 ◽  
Vol 8 (5-s) ◽  
pp. 378-387
Author(s):  
Mrs Kalpna ◽  
Druv Dev ◽  
Mohammad Shahnaz ◽  
Jyoti Parkash ◽  
DN Prasad

In this work an attempt was made for the preparation and evaluation of controlled release chitosan microspheres using anti-diabetes drug Metformin hydrochloride. The microspheres were prepared by Ionotropic gelation method using chitosan as polymer and Sodium Tripolyphosphate (TPP) as crosslinking agent. The compatibility of drug and polymer is analyzed by using FTIR and DSC method. There was no interaction detected by FTIR and DSC study. Further the prepared microspheres were evaluated for particle size, drug entrapment efficiency, surface morphology, drug content, drug loading and in vitro drug release. Amongst all the formulation batch 7 shows the best release when compared to other batch. SEM (Scanning electron microscopy) revealed that microspheres were spherical and porous. Finally it was concluded that Metformin hydrochloride loaded chitosan – TPP microspheres have been found suitable for controlled release formulation due to its bioavailability and biodegradability and thus lead to improved patient compliance. Keywords: Microspheres, Metformin hydrochloride, Ionotropic gelation method, chitosan.


Author(s):  
Hyemi Heo ◽  
Yun-Kyung Lee ◽  
Yoon Hyuk Chang

The present study aimed to investigate the physicochemical and in vitro digestibility properties of potato starch cross-linked using sodium trimetaphosphate (STMP)/ sodium tripolyphosphate (STPP). These properties were investigated by X-ray diffraction, analysis of the swelling factor and light transmittance, and in vitro digestibility tests for rapid digestible starch (RDS) and resistant starch (RS) contents. X-ray diffraction patterns showed that cross-linking with STMP/STPP occurred primarily in the amorphous regions and did not change the crystalline region of the potato starch granules. The swelling factor and light transmittance of the cross-linked potato starch (CLPS) was significantly lower than that of the native potato starch (NPS). The in vitro digestibility results showed that cross-linking with STMP/STPP decreased the RDS contents significantly and increased the RS contents significantly compared with those of NPS. The RS contents of potato starch increased significantly with the increasing degree of crosslinking. Potato starch cross-linked using STMP/STPP can be used a source of dietary fiber in the food industry.


1971 ◽  
Vol 17 (10) ◽  
pp. 998-1001 ◽  
Author(s):  
A E Clarke ◽  
M A Denborough

Abstract Chlorpromazine causes precipitation both of the glycoprotein and protein components of bile in vitro. The reaction depends on an electrostatic interaction between the negatively charged carboxyl groups on the bile components and the positively charged amine groups on the drug molecules in solution. The optimum conditions for the interaction between chlorpromazine and bile components have been established, and the suggestion is made that this precipitation may be responsible in part, for cholestatic jaundice associated with the administration of chlorpromazine.


Author(s):  
Madhuri T Deshmukh ◽  
Shrinivas K Mohite

Objective: The objective of this research was to formulate and evaluate olanzapine (OLE) mucoadhesive microsphere prepared using carbopol and sodium combination. OLE having extensive hepatic first pass metabolism and low bioavailability problem, determined the need for the development of sustained release formulation.Methods: OLE mucoadhesive microspheres were prepared by ionic gelation method. OLE mucoadhesive microspheres were prepared byionic gelation method by using calcium chloride as crosslinking agent. The OLE mucoadhesive microsphere was characterized by particle sizemeasurement, process yield, morphology of microsphere, drug entrapment efficiency, mucoadhesion test, differential scanning calorimetry, powder X-ray diffraction, Fourier transforms infrared (FTIR) study and in-vitro drug release.Results: The OLE mucoadhesive microsphere having mean particle size ranged from 546.0 µm to 554.3 µm, and the entrapment efficiencies ranged from 73% to 96%. All the olanzapine (OLE) microsphere batches showed good in-vitro mucoadhesive property ranging from 75.89% to 96.47% and in the in-vitro wash off test ranging from 68.12% to 81.3%. FTIR studies indicated the no drug-polymer interactions in the ideal formulation F9. Therewere no compatibility issues, and the crystallinity of OLE was found to be reduced shoeing less intense peak in prepared mucoadhesive microspheres, which were confirmed by differential scanning calorimeter and X-ray diffraction studies. Among different formulations, the OLE microspheres of batch F9 had shown the optimum percent drug entrapment of microspheres. Release pattern of OLE from F9 microspheres batch followed Higuchi kinetic model. Stability studies were carried out for F9 formulation at 4°C/ambient, 25±2°C/60±5%, 40±2°C/75±5% relative humidity revealed that the drug entrapment, mucoadhesive behavior, and drug release were within permissible limits.Conclusion: The results obtained in this work demonstrate the use of carbopol and sodium alginate polymer for preparation of mucoadhesive microsphere.Keywords: Ionic gelation method, Gastroretentive delivery, Mucoadhesive microsphere, Carbopol.


Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 180 ◽  
Author(s):  
Simona Giarra ◽  
Silvia Zappavigna ◽  
Virginia Campani ◽  
Marianna Abate ◽  
Alessia Cossu ◽  
...  

This study aimed to develop nanovectors co-encapsulating doxorubicin (Doxo) and zoledronic acid (Zol) for a combined therapy against Doxo-resistant tumors. Chitosan (CHI)-based polyelectrolyte complexes (PECs) prepared by ionotropic gelation technique were proposed. The influence of some experimental parameters was evaluated in order to optimize the PECs in terms of size and polydispersity index (PI). PEC stability was studied by monitoring size and zeta potential over time. In vitro studies were carried out on wild-type and Doxo-resistant cell lines, to assess both the synergism between Doxo and Zol, as well as the restoring of Doxo sensitivity. Polymer concentration, incubation time, and use of a surfactant were found to be crucial to achieving small size and monodisperse PECs. Doxo and Zol, only when encapsulated in PECs, showed a synergistic antiproliferative effect in all the tested cell lines. Importantly, the incubation of Doxo-resistant cell lines with Doxo/Zol co-encapsulating PECs resulted in the restoration of Doxo sensitivity.


2011 ◽  
Vol 25 (27) ◽  
pp. 3647-3653
Author(s):  
R. EMADI ◽  
K. RAEISSI

Ag/TiO2coating was prepared by anodizing the surface of Ti followed by electrodeposition of silver. By X-ray diffraction (XRD) analyses, that indicated the crystalline size of Ag deposit onto the oxidized surface of Ti was around 32 nm. Scanning electron microscopy (SEM) images of the oxidized surface with and without Ag deposit show that TiO2is formed uniformly but Ag deposit consisted of numerous spherical structures. The Escherichia coli and Staphylococcus aureus bacteria were utilized to test the antibacterial effect of Ag/TiO2coating which showed more than 99% of bacteria were killed after 24 h incubation. The results of in vitro test showed Ag/TiO2coating is also biocompatible.


2021 ◽  
Vol 11 (6) ◽  
pp. 48-57
Author(s):  
Vivekanandan S. ◽  
Lindholm Berit ◽  
.Raghunandan Reddy K ◽  
Venkatesan P.

Dexibuprofen is a pharmacologically active enantiomer of racemic ibuprofen (NSAID), which is used to treat pain and inflammation. Like common NSAIDs, Dexibuprofen is an active enantiomer of ibuprofen that suppresses the prostanoid synthesis in the inflammatory cells via inhibition of the COX-2 isoform of the arachidonic acid COX. The therapeutic use of Dexibuprofen is limited by the rapidity of the onset of its action and its short biological half-life. Hence, our aim was to develop Dexibuprofen nanoparticles formulation to overcome these disadvantages using optimized concentration of polymers by appropriate methods for nanoparticle preparation. The drug and the nanoparticle formulation of Dexibuprofen F11 were comparatively assessed for FT IR spectrums by using FT-IR method. The DSC study was used as one of the tool to assess the compatibility between drug and the excipients. As per DSC thermograms, the drug as well as drug with mixture of excipients chitosan, sodium tripolyphosphate had shown no interactions with dexibuprofen. The ionotropic gelation method was used to prepare Dexibuprofen nanoparticles. The chitosan and sodium tripolyphosphate (TPP) of different concentrations were used as polymers to prepare Dexibuprofen nanoparticles. Total eleven different formulations were explored with different concentrations of drug : polymer ratios using ionotropic gelation method to identify optimal concentrations of polymer. Among different formulations, F11 formulation with optimized concentration of 5% chitosan and 1% Sodium tripolyphosphate polymers along with Dexibuprofen showed maximum drug release. The objective was to evaluate the developed Dexibuprofen nanoparticles. In-vitro drug release was evaluated in 0.05M phosphate buffer pH7.2 and found that the drug release of F11 formulation of Dexibuprofen nanoparticle had shown release till 24 hours more than that of other trials. Hence, F11 formulation was considered as the optimized nanoparticle formulation to control drug release till 24 hours. The entrapment efficacy of the formulated Nanoparticles was found to be in the range of 75.48%-91.22% respectively.


2021 ◽  
pp. 096739112110473
Author(s):  
Huma Hameed ◽  
Khurram Rehman ◽  
Anam Hameed ◽  
Abdul Qayuum

The objective of this study was the preparation of ionically crosslinked 6-mercaptopurine (6-MP) monohydrate microparticles through preparing polyelectrolyte complexes of drug and polymers. Polymers such as chitosan, casein, and carrageenan were used to prepare crosslinked microparticles, and sodium tripolyphosphate was used as crosslinker. Microparticles were characterized for their flow behavior, compressibility, percentage yield, micromeritic, and entrapment efficiency. Scanning electron microscopy was conducted to understand the surface morphology of the microparticles, and the result was correlated with the swelling index and percentage drug release. Mathematical modeling of drug release in order to determine the drug release kinetics was also determined to understand the mechanism involving the release of 6-mercaptopurine from the microparticles. The ionic crosslinked microparticles were in the range of 664 μm–798 μm particle size having good flow and compressibility properties with percentage yield were found to be from 77.5% to 87.5% in range. The entrapment efficiency for the formulations were found to be from 63.5% to 83.5%, with MCP-5 gave maximum entrapment efficiency of 83.5%. In vitro swelling and drug release studies were in accordance with the polymer properties following zero-order model with super-case transport II.


2019 ◽  
Vol 20 (9) ◽  
pp. 2247 ◽  
Author(s):  
Farhatun Najat Maluin ◽  
Mohd Zobir Hussein ◽  
Nor Azah Yusof ◽  
Sharida Fakurazi ◽  
Abu Seman Idris ◽  
...  

The use of nanotechnology could play a significant role in the agriculture sector, especially in the preparation of new-generation agronanochemicals. Currently, the economically important plant of Malaysia, the oil palm, faces the threat of a devastating disease which is particularly caused by a pathogenic fungus, Ganoderma boninense. For the development of an effective antifungal agent, a series of chitosan nanoparticles loaded with a fumigant, dazomet, were prepared using various concentrations of sodium tripolyphosphate (TPP)—2.5, 5, 10, and 20 mg/mL, abbreviated as CDEN2.5, CDEN5, CDEN10, and CDEN20, respectively. The effect of TPP as a crosslinking agent on the resulting particle size of the synthesized nanoparticles was investigated using a particle size analyzer and high-resolution transmission electron microscopy (HRTEM). Both methods confirmed that increasing the TPP concentration resulted in smaller particles. In addition, in vitro fumigant release at pH 5.5 showed that the release of the fumigant from the nanoparticles was of a sustained manner, with a prolonged release time up to 24 h. Furthermore, the relationship between the chitosan-dazomet nanoparticles and the in vitro antifungal activity against G. boninense was also explored, where the nanoparticles of the smallest size, CDEN20, gave the highest antifungal efficacy with the lowest half maximum effective concentration (EC50) value of 13.7 ± 1.76 ppb. This indicates that the smaller-sized agronanoparticles were more effective as an antifungal agent. The size can be altered, which plays a crucial role in combatting the Ganoderma disease. The agronanoparticles have controlled release properties and high antifungal efficacy on G. boninense, thus making them a promising candidate to be applied in the field for Ganoderma treatment.


Materials ◽  
2019 ◽  
Vol 12 (3) ◽  
pp. 381 ◽  
Author(s):  
Aura-Cătălina Mocanu ◽  
George E. Stan ◽  
Andreea Maidaniuc ◽  
Marian Miculescu ◽  
Iulian Vasile Antoniac ◽  
...  

Calcium carbonate from marble and seashells is an eco-friendly, sustainable, and largely available bioresource for producing natural bone-like calcium phosphates (CaPs). Based on three main objectives, this research targeted the: (i) adaptation of an indirect synthesis route by modulating the amount of phosphorus used in the chemical reaction, (ii) comprehensive structural, morphological, and surface characterization, and (iii) biocompatibility assessment of the synthesized powdered samples. The morphological characterization was performed on digitally processed scanning electron microscopy (SEM) images. The complementary 3D image augmentation of SEM results also allowed the quantification of roughness parameters. The results revealed that both morphology and roughness were modulated through the induced variation of the synthesis parameters. Structural investigation of the samples was performed by Fourier transform infrared spectroscopy and X-ray diffraction. Depending on the phosphorus amount from the chemical reaction, the structural studies revealed the formation of biphasic CaPs based on hydroxyapatite/brushite or brushite/monetite. The in vitro assessment of the powdered samples demonstrated their capacity to support MC3T3-E1 pre-osteoblast viability and proliferation at comparable levels to the negative cytotoxicity control and the reference material (commercial hydroxyapatite). Therefore, these samples hold great promise for biomedical applications.


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