scholarly journals In Vitro Evaluation of Curcumin-Encapsulated Chitosan Nanoparticles against Feline Infectious Peritonitis Virus and Pharmacokinetics Study in Cats

2020 ◽  
Vol 2020 ◽  
pp. 1-18 ◽  
Author(s):  
Shing Wei Ng ◽  
Gayathri Thevi Selvarajah ◽  
Mohd Zobir Hussein ◽  
Swee Keong Yeap ◽  
Abdul Rahman Omar

Feline infectious peritonitis (FIP) is an important feline viral disease, causing an overridden inflammatory response that results in a high mortality rate, primarily in young cats. Curcumin is notable for its biological activities against various viral diseases; however, its poor bioavailability has hindered its potential in therapeutic application. In this study, curcumin was encapsulated in chitosan nanoparticles to improve its bioavailability. Curcumin-encapsulated chitosan (Cur-CS) nanoparticles were synthesised based on the ionic gelation technique and were spherical and cuboidal in shape, with an average particle size of 330 nm and +42 mV in zeta potential. The nanoparticles exerted lower toxicity in Crandell-Rees feline kidney (CrFK) cells and enhanced antiviral activities with a selective index (SI) value three times higher than that of curcumin. Feline-specific bead-based multiplex immunoassay and qPCR were used to examine their modulatory effects on proinflammatory cytokines, including tumour necrosis factor (TNF)α, interleukin- (IL-) 6, and IL-1β. There were significant decrements in IL-1β, IL-6, and TNFα expression in both curcumin and Cur-CS nanoparticles. Based on the multiplex immunoassay, curcumin and the Cur-CS nanoparticles could lower the immune-related proteins in FIP virus (FIPV) infection. The single- and multiple-dose pharmacokinetics profiles of curcumin and the Cur-CS nanoparticles were determined by high-performance liquid chromatography (HPLC). Oral delivery of the Cur-CS nanoparticles to cats showed enhanced bioavailability with a maximum plasma concentration (Cmax) value of 621.5 ng/mL. Incorporating chitosan nanoparticles to deliver curcumin improved the oral bioavailability and antiviral effects of curcumin against FIPV infection. This study provides evidence for the potential of Cur-CS nanoparticles as a supplementary treatment of FIP.

2018 ◽  
Vol 13 (2) ◽  
pp. 111 ◽  
Author(s):  
Yadi Suryadi ◽  
Tri Puji Priyatno ◽  
I Made Samudra ◽  
Dwi Ningsih Susilowati ◽  
Tuti Septi Sriharyani ◽  
...  

<p>Anthracnose (Colletotrichum gloeosporioides) is one of the important diseases of fruit crops that need to be controlled. This study was aimed to obtain the best formula of hydrolyzed nano chitosan and its potensial in controlling anthracnose. The hydrolyzed chitosan was prepared using chitinase enzyme extracted from Burkholderia cepacia isolate E76. Chitosan nanoparticles were synthesized using ionic gelation method by reacting hydrolyzed chitosan (0.2%) with Sodium tripolyphosphate (STPP) (0.1%) as cross-linking agent using 30&amp;ndash;60 minutes stirring condition. The bioactivity of the nano chitosan formula was tested to C. gloeosporioides under in vitro and in vivo assays. The specific enzymatic activity of the purified chitinase was higher (0.19 U/mg) than that of crude enzyme (supernatant) with the purity increased by 3.8 times. Of the four formula tested, Formula A (hydrolyzed chitosan to STPP volume ratio of 5 : 1 with 60 minutes stirring condition) was found good in terms of physical characteristic of the particle. The formula nano chitosan particle had the spherical-like shape with an average particle size of 126.2+3.8 nm, polydispersity index (PI) of 0.4+0.02, and zeta potential (ZP) value of 27.8+0.2 mV. Nano chitosan had an inhibitory activity to C. gloeosporioides in vitro up to 85.7%. Moreover, it could inhibit 61.2% of C. gloeosporioides spores germination. It was shown that nano chitosan was also effective to reduce anthracnose disease severity in vivo when applied as a preventive measure on chili and papaya fruits. This study could be used as a reference for further fruit coating application using nano chitosan as a promising postharvest biocontrol agent to C. gloeosporioides.</p>


2019 ◽  
Vol 9 (10) ◽  
pp. 275 ◽  
Author(s):  
Shadab Md ◽  
Nabil A. Alhakamy ◽  
Hibah M. Aldawsari ◽  
Hani Zakaria Asfour

Parkinson’s disease (PD) is a neurodegenerative disorder resulting in a decreased nigrostriatal availability of dopamine. Oxidative stress is one factor contributing to PD. Naringenin (NAR), a flavonoid, is a potent antioxidant shown to be beneficial in experimental PD. The clinical development of NAR has been hampered due to its low bioavailability resulting from gastrointestinal degradation, inefficient permeability, and low aqueous solubility. The objective of the present research was to formulate and characterize naringenin-loaded chitosan nanoparticles (NAR NPs) for nose-to-brain delivery. The cellular uptake, cytotoxicity, and neuroprotective effects of NAR NPs were determined using the SH-SY5Y cell line in vitro. NAR NPs were prepared using the ionic gelation method and characterized by zetasizer, transmission electron microscopy (TEM), and field emission microscopy (FESEM). The average particle size, polydispersity index (PDI), zeta potential, entrapment efficiency, and 24 h in vitro release profile were 87.6 ± 8.47 nm, 0.31 ± 0.04, 15.36 ± 2.05 mV, 91.12 ± 2.99%, and 54.80 ± 4.22%, respectively. The percentage NAR permeation through nasal mucosa from NPs was found to be 67.90 ± 0.72%. Cellular uptake of prepared NPs was confirmed by fluorescence microscopy. Neuroprotective activity of NAR NPs was evaluated through viability assays and by estimating reactive oxygen species (ROS) levels. NAR NPs showed enhanced neuroprotective ability and antioxidant effect against 6-OHDA-induced neurotoxicity in SH-SY5Y cells. However, animal studies are necessary to establish the potential of NAR NPs to be an effective carrier for the treatment of PD for nose-to-brain delivery.


2018 ◽  
Vol 8 (5-s) ◽  
pp. 400-406 ◽  
Author(s):  
Subhendu Sekhar Mishra ◽  
Ashish Sharma

The aim of this study was to prepare and evaluate nanoparticles containing insulin in different polymer ratio by ionotropic gelation method. The average particle size was found to be 130.4±3.4 -155.5±6.4nm. SEM indicates that nanoparticles have shown smooth and spherical shape. The zeta potential of optimized formulation was 35.5 mv which indicates moderate stability with no agglomeration. The average drug content was found to be 130.4±3.4 -155.5±6.4nm. The in vitro drug release data was analyzed using zero order, first order, Higuchi, and Korsmeyer-Peppas models. It was observed the best fit model for nanoparticles was higuchi model. The developed formulation in situ polymeric gel is designed in such a way that the gel will load insulin in higher concentration and it will also contain penetration enhancer which will enhance the absorption of release drug from gel to systemic circulation. Keywords: Insulin, Nanoparticle, invitro drug release study.


2020 ◽  
Vol 16 (2) ◽  
pp. 104-121
Author(s):  
Serda Kecel-Gunduz ◽  
Yasemin Budama-Kilinc ◽  
Rabia Cakir-Koc ◽  
Tolga Zorlu ◽  
Bilge Bicak ◽  
...  

Background: Sulpiride, which has selective dopaminergic blocking activity, is a substituted benzamide antipsychotic drug playing a prominent role in the treatment of schizophrenia, which more selective and primarily blocks dopamine D2 and D3 receptor. Objective: This study has two main objectives, firstly; the molecular modeling studies (MD and Docking, ADME) were conducted to define the molecular profile of sulpiride and sulpiridereceptor interactions, another to synthesize polymeric nanoparticles with chitosan, having the advantage of slow/controlled drug release, to improve drug solubility and stability, to enhance utility and reduce toxicity. Method: Molecular dynamic simulation was carried out to determine the conformational change and stability (in water) of the drug and the binding profile of D3 dopamine receptor was determined by molecular docking calculations. The pharmacological properties of the drug were revealed by ADME analysis. The ionic gelation method was used to prepare sulpiride loaded chitosan nanoparticles (CS NPs). The Dynamic Light Scattering (DLS), UV-vis absorption (UV), Scanning Electron Microscopy (SEM), Fourier transform infrared (FT-IR) spectroscopy techniques were carried out to characterize the nanoparticles. In vitro cell cytotoxicity experiments examined with MTT assay on mouse fibroblast (L929), human neuroblastoma (SH-SY5Y) and glioblastoma cells (U-87). The statistical evaluations were produced by ANOVA. Results: The residues (ASP-119, PHE-417) of D3 receptor provided a stable docking with the drug, and the important pharmacological values (blood brain barrier, Caco-2 permeability and human oral absorption) were also determined. The average particle size, PdI and zeta potential value of sulpiride- loaded chitosan NPs having a spherical morphology were calculated as 96.93 nm, 0.202 and +7.91 mV. The NPs with 92.8% encapsulation and 28% loading efficiency were found as a slow release profile with 38.49% at the end of the 10th day. Due to the formation of encapsulation, the prominent shifted wave numbers for C-O, S-O, S-N stretching, S-N-H bending of Sulpiride were also identified. Mitochondrial activity of U87, SHSY-5Y and L929 cell line were assayed and evaluated using the SPSS program. Conclusion: To provide more efficient use of Sulpiride having a low bioavailability of the gastrointestinal tract, the nanoparticle formulation with high solubility and bioavailability was designed and synthesized for the first time in this study for the treatment of schizophrenia. In addition to all pharmacological properties of drug, the dopamine blocking activity was also revealed. The toxic effect on different cell lines have also been interpreted.


2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Amiya kumar Prusty ◽  
Susanta Kumar Sahu

The current study was designed to prepare and characterize insulin incorporated nanoparticles by complex coacervation process followed by antidiabetic study of orally administered insulin incorporated nanoparticles in diabetic rats. The nanoparticles were characterized for particle size, loading and entrapment efficiency as well as in vitro release of incorporated insulin. The prepared nanoparticles were found to have an average particle size of 551.67 nm ±45.5. The highest entrapment efficiency and loading capacity values were found to be of 52.48±1.98 and 47.01±1.21, respectively. Oral administration of 10 IU/Kg of insulin loaded nanoparticles to diabetic rats showed a maximum blood glucose change of 53.46±2.19 at 5-hours time period. The results obtained indicate the potential of prepared nanoparticulate system as a carrier for oral delivery of insulin.


2011 ◽  
Vol 197-198 ◽  
pp. 238-241 ◽  
Author(s):  
Pu Wang Li ◽  
Zheng Peng ◽  
F.H. She ◽  
L.X. Kong

Drug delivery systems with active targeting ligand provide improved therapeutic efficiency due to the selectivity towards tumor cells. In this paper we prepared drug loaded nanoparticles (NPs) using folate (FA) incorporated chitosan (FA-CS) based on ionic gelation technology. FA-CS NPs were spherical in shape with an average particle size of 100 nm, while 5-fluorouracil (5-FU) loaded NPs became less circular with average particle size of 100-500 nm. NPs made from FA-CS conjugates exhibited improved capability to encapsulate hydrophilic 5-FU. It was found 5-FU distributed in FA-CS NPs in solid solution state. In vitro release results demonstrated the release of 5-FU from FA-CS NPs was more controllable as compared to that of CS NPs.


2021 ◽  
Vol 8 (1) ◽  
pp. 201331
Author(s):  
Yue Tang ◽  
Jun Wu ◽  
Yuan Zhang ◽  
Lingpeng Ju ◽  
Xiangyang Qu ◽  
...  

We prepared the superparamagnetic chitosan nanoparticles (SPCIONPs) to study the application of them as gene vectors using a magnetic transfection system for the targeted treatment of lung metastasis of osteosarcoma. The SPCIONPs were characterized by transmission electron microscopy, Fourier transform infrared spectrometry, superconducting quantum interference device and atomic force microscopy. Their biosafety was determined by cell counting kit-8 (CCK8) and live–dead staining assays. The transfection in vitro was detected by laser confocal microscopy. SPCIONPs, which can bind closely to plasmids and protect them from DNA enzyme degradation, were prepared with an average particle size of approximately 22 nm and zeta potential of 11.3 mV. The results of the CCK8 and live–dead staining assays showed that superparamagnetic chitosan nanoparticles loaded with insulin-like growth factor-binding protein 5 (SPCIONPs/pIGFBP 5 ) induced no significant cytotoxicity compared to the control group. The result of transfection in vitro suggested that pIGFBP 5 emitted a greater amount of red fluorescence in the SPCIONPs/pIGFBP 5 group than that in the chitosan-loaded IGFBP 5 (CS/pIGFBP 5 ) group. In conclusion, the prepared SPCIONPs had good biosafety and could be effectively used to transfer pIGFBP 5 into 143B cells, and they thus have good application prospects for the treatment of lung metastasis of osteosarcoma.


Author(s):  
Kumar Nishchaya ◽  
Swatantra K.S. Kushwaha ◽  
Awani Kumar Rai

Background: Present malignant cancer medicines has the advancement of magnetic nanoparticles as delivery carriers to magnetically accumulate anticancer medication in malignant growth tissue. Aim: In the present investigation, a silica nanoparticles (MSNs) stacked with hydroxyurea were combined and was optimized for dependent and independent variables. Method: In this study, microporous silica nanoparticle stacked with neoplastic medication had been prepared through emulsification followed with solvent evaporation method. Prepared MSNs were optimized for dependent and independent variables. Different formulations were prepared with varying ratio of polymer, lipid and surfactant which affects drug release and kinetics of drug release pattern. The obtained MSNs were identified by FTIR, SEM, drug entrapment, in-vitro drug release, drug release kinetics study, stability testing in order to investigate the nanoparticle characteristics. Results: The percentage drug entrapment of the drug for the formulations F1, F2, F3, was found to be 27.78%, 65.52% and 48.26%. The average particle size for F2 formulation was found to be 520 nm through SEM. The cumulative drug release for the formulations F1, F2, F3 was found to be 64.17%, 71.82% and 32.68%. The formulations were found to be stable which gives controlled drug delivery for 6 hours. Conclusion: From the stability studies data it can be culminated that formulations are most stable when stored at lower temperature or in refrigerator i.e. 5˚C ± 3˚C. It can be concluded that MSN’s loaded with hydroxyurea is a promising approach towards the management of cancer due to its sustained release and less side effects.


Nanomaterials ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 808
Author(s):  
Ahmed Al Saqr ◽  
El-Sayed Khafagy ◽  
Ahmed Alalaiwe ◽  
Mohammed F. Aldawsari ◽  
Saad M. Alshahrani ◽  
...  

Green synthesis of gold nanoparticles (GNPs) with plant extracts has gained considerable interest in the field of biomedicine. Recently, the bioreduction nature of herbal extracts has helped to synthesize spherical GNPs of different potential from gold salt. In this study, a fast ecofriendly method was adopted for the synthesis of GNPs using fresh peel (aqueous) extracts of Benincasa hispida, which acted as reducing and stabilizing agents. The biosynthesized GNPs were characterized by UV–VIS and Fourier transform infrared spectroscopy, transmission electron microscopy (TEM), and dynamic light scattering. In addition, the in vitro antibacterial and anticancer activities of synthesized GNPs were investigated. The formation of gold nanoparticles was confirmed by the existence of a sharp absorption peak at 520 nm, corresponding to the surface plasmon resonance (SPR) band of the GNPs. TEM analysis revealed that the prepared GNPs were spherical in shape and had an average particle size of 22.18 ± 2 nm. Most importantly, the synthesized GNPs exhibited considerable antibacterial activity against different Gram-positive and Gram-negative bacteria. Furthermore, the biosynthesized GNPs exerted remarkable in vitro cytotoxicity against human cervical cancer cell line, while sparing normal human primary osteoblast cells. Such cytotoxic effect was attributed to the increased production of reactive oxygen species (ROS) that contributed to the damage of HeLa cells. Collectively, peel extracts of B. hispida can be efficiently used for the synthesis of GNPs, which can be adopted as a natural source of antimicrobial and anticancer agent.


2019 ◽  
Vol 829 ◽  
pp. 263-269
Author(s):  
Denny Nurdin ◽  
Andri Hardiansyah ◽  
Elsy Rahimi Chaldun ◽  
Anti Khoerul Fikkriyah ◽  
Hendra Dian Adhita Dharsono ◽  
...  

Exploration of natural compound for the treatment of dental-related problems are gaining of interest for enhancing therapeutic efficacy of the drugs delivery system. In this study, we have prepared terpenoid, which have been isolated from Myrmecodia pendens Merr & Perry from Papua Island, Indonesia, to be encapsulated in Polylactic-co-glycolic acid (PLGA), as the most widely used biodegradable polymer for biomedical applications, through one step single-emulsion method followed by subsequent coating by poly (vinyl alcohol) (PVA). The resultant of terpenoid-loaded PLGA microparticles were characterized systematically through scanning electron microscope and Fourier-transform infrared spectroscopy. In vitro drug release test was evaluated through dialysis method. Antibacterial test was conducted against Enterococcus faecalis as a model for persistent bacteria that causes root canal infections. The results showed that terpenoid-loaded PLGA microparticles were developed in spherical morphology with an average particle size of around 1-2μm. Terpenoid released from PLGA compartment at pH 6.5 and temperature of 37°C through a controlled-release profile mechanism with enhanced prolonged release. The bacterial assay result showed that terpenoid-loaded PLGA microparticles could reduce Enterococcus faecalis, effectively. Eventually, these result show that terpenoid-loaded PLGA microparticles as unique natural product-based extract could be developed as a potential naturally-based drug for dental-related diseases applications.


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