scholarly journals Ex Vivo Evaluation of Insulin Nanoparticles Using Chitosan and Arabic Gum

2011 ◽  
Vol 2011 ◽  
pp. 1-6 ◽  
Author(s):  
M. R. Avadi ◽  
A. M. M. Sadeghi ◽  
Naser Mohamadpour Dounighi ◽  
R. Dinarvand ◽  
F. Atyabi ◽  
...  

Polymeric delivery systems based on nanoparticles have emerged as a promising approach for peroral insulin delivery. The aim of the present study was to investigate the release of insulin nanoparticulate systems and ex vivo studies. The nanoparticles were prepared by the ion gelation method. Particle size distribution, zeta potential, and polydispersity index of the nanoparticles were determined. It was found that the nanoparticles carried positive charges and showed a size distribution in the range of 170–200 nm. The electrostatic interactions between the positively charged group of chitosan and negatively charged groups of Arabic gum play an important role in the association efficiency of insulin in nanoparticles. In vitro insulin release studies showed an initial burst followed by a slow release of insulin. The mucoadhesion of the nanosystem was evaluated using excised rat jejunum. Ex vivo studies have shown a significant increase in absorption of insulin in the presence of chitosan nanoparticles in comparison with free insulin.


2021 ◽  
pp. 088391152199784
Author(s):  
Loveleen Kaur ◽  
Ajay Kumar Thakur ◽  
Pradeep Kumar ◽  
Inderbir Singh

Present study was aimed to synthesize and characterize Chitosan-Catechol conjugates and to design and develop mucoadhesive pellets loaded with lafutidine. SEM images indicated the presence of fibrous structures responsible for enhanced mucoadhesive potential of Chitosan-Catechol conjugates. Thermodynamic stability and amorphous nature of conjugates was confirmed by DSC and XRD studies respectively. Rheological studies were used to evaluate polymer mucin interactions wherein strong interactions between Chitosan-Catechol conjugate and mucin was observed in comparison to pristine chitosan and mucin. The mucoadhesion potential of Chitosan-Catechol (Cht-C) versus Chitosan (Cht) was assessed in silico using molecular mechanics simulations and the results obtained were compared with the in vitro and ex vivo results. Cht-C/mucin demonstrated much higher energy stabilization (∆E ≈ −65 kcal/mol) as compared to Cht/mucin molecular complex. Lafutidine-loaded pellets were prepared from Chitosan (LPC) and Chitosan-Catechol conjugates (LPCC) and were evaluated for various physical properties viz. flow, circularity, roundness, friability, drug content, particle size and percent mucoadhesion. In vitro drug release studies on LPC and LPCC pellets were performed for computing t50%, t90% and mean dissolution time. The values of release exponent from Korsmeyer-Peppas model was reported to be 0.443 and 0.759 for LPC and LPCC pellets suggesting Fickian and non-Fickian mechanism representing drug release, respectively. In vivo results depicted significant controlled release and enhanced residence of the drug after being released from the chitosan-catechol coated pellets. Chitosan-Catechol conjugates were found to be a promising biooadhesive polymer for the development of various mucoadhesive formulations.



2017 ◽  
Vol 9 (3-4) ◽  
Author(s):  
Asmaa S. El-Houssiny ◽  
Azza A. Ward ◽  
Dina M. Mostafa ◽  
Salwa L. Abd-El-Messieh ◽  
Kamal N. Abdel-Nour ◽  
...  

AbstractGlucosamine sulfate (GS) has been used orally for the treatment of osteoarthritis (OA). However, it may be susceptible to the liver first pass phenomenon, which greatly affects its bioavailability, in addition to its side effects on the gastrointestinal tract. Alginate nanoparticles (Alg NPs) were investigated as a new drug carrier for transdermal delivery of GS to improve its effectiveness and reduce side effects. GS-Alg NPs were characterized by encapsulation efficiency, NP yield, particle size and surface charge properties. The in vitro release studies of GS and the ex vivo permeability through rat skin were determined using a UV-Vis spectrophotometer. GS-Alg NPs are within the nanometer range of size. High negative surface charge values are obtained and indicate the high suspension stability of the prepared formulation. The in vitro release studies showed that GS is released from Alg NPs in a sustained and prolonged manner. The ex vivo permeability of GS through rat skin is enhanced significantly after encapsulation in the negatively charged Alg NPs. We successfully reported a highly stable nanoparticlulate system using Alg NPs that permits the encapsulation of GS for topical administration, overcoming the disadvantages of oral administration.



2020 ◽  
Vol 11 (1) ◽  
pp. 567-580
Author(s):  
Venugopalaiah Penabaka ◽  
Kumar B ◽  
Prasad N.B.L

Many factors affect the pulmonary drug delivery and stability of the nanoparticles an acupuncture consisting of bronchial asthma. Present research envisages on the development of dry powder nanoparticles as insufflation a acupuncture consisting of bronchial asthma (allergy due to Aspergillus fumigatus) using physical mixing and spray drying. Different founding are prepared and characterized with suitable excipients like lactose and trehalose. The particle size distribution of nano milled and spray-dried particles of Terbutaline Sulphate and Itraconazole showed unimodal size distribution. The formulations prepared with trehalose as the carrier showed less Dv90, Dv50 and Dv10 values due to the fineness in the particles of trehalose when compared to lactose. The Dv50  and Dv10 values were in the range of mountains of 0.43-0.89 µm and 0.21–0.49 µm for all formulations, which shows the primary particle size in the nanometer scale. Smooth and nearly spherical particles were produced for spray-dried formulations when compared to milled formulations. Zeta potential comes across until be between +17±0.13 to +32±0.12, which explains the particles as moderately stable. MMAD values ranges from 3.19 µm to 4.78 µm for milled nanoparticles and 3.45 µm to 4.21 µm for spray-dried particles. Formulated nanoparticles exhibited good spreading properties, which will allow all the particles to deposition palmy profusion territories consisting of the lung. In-vitro drug release studies explains that spray-dried formulations of Terbutaline sulpahte and Itraconazole using lactose as excipients released the drug upto 98.9% and 99.1% in 180mts.



Author(s):  
Charu Tyagi

Gelatin-eudragit L100 nanoparticles of wet size range 170-563nm were prepared by two step dissolvation method and the effect of different concentrations of eudragit L100 and emulsifying agent - sodium lauryl sulphate (SLS) - on the particle size were studied. Synthesized nanoparticles were characterized by attenuated total reflectance-fourier transform infrared spectroscopy (ATRFTIR) and the mean size distribution. Insulin loading was done at a pH 7.4 and the in vitro insulin release studies of nanoparticles were carried out by simulating gastrointestinal tract condition which showed the minimal insulin release at pH 2.5 (20% in 90min) while appreciable release (40% in first 30min) at pH of 7.4. This pH responsive release pattern of the synthesized nanoparticles confers on the insulin protection from proteolytic degradation in acidic environment of stomach and upper intestinal part while enhancing bioavailability in the later part of intestine.





2020 ◽  
Vol 16 ◽  
Author(s):  
Erdal Eroğlu ◽  
Hüseyin Saygın Portakal ◽  
Ayşenur Pamukçu

Background: Despite great hopes for small interfering RNA (siRNA)-based gene therapies, restrictions, including the presence of nucleases, reticuloendothelial system and undesired electrostatic interactions between nucleic acids and the cell membrane, limit the success of these approaches. In the last few decades, non-viral nucleic acid delivery vectors in nano size with high biocompatibility, low toxicity and proton sponge effect have emerged as magic bullets to overcome these drawbacks. Objective: This study aimed to develop poly(2-hydroxyethyl methacrylate) (pHEMA)-chitosan nanoparticles (PCNp), and to transfect green fluorescent protein (GFP)-silencing siRNA (GsiR) in vitro. Method: First, PCNp displaying core-shell structure was synthesized and thereafter GsiR was encapsulated into the core of PCNp. The synthesized PCNp with/without GsiR were characterized using ultraviolet-visible (UV-vis)-spectroscopy, Fourier-transform infrared (FTIR) spectroscopy, thermal decomposition, atomic force microscopy (AFM), scanning electron microscopy (SEM), zeta potential and dynamic light scattering (DLS) measurements. Encapsulation of siRNA into the pHEMA core coated with chitosan shell was demonstrated using fluorescence and FTIR spectroscopy. Results: The surface charge of PCNSs and PCNSs-GsiR were found to be +39.5 and +40.2, respectively. In DLS analysis, an insignificant shift in the Z-average diameter of PCNp was observed from 109 nm to 133 nm using encapsulation of GsiR. In comparison to other studied nanomaterials and a commercial transfection reagent, our findings suggest a promising GFP-silencing effect of 45%. Conclusion: To our knowledge, we have obtained comparable silencing activity with the other studied equivalents despite using the lowest concentration of siRNA in existing literature.





2016 ◽  
Vol 42 (5) ◽  
pp. 1145-1166 ◽  
Author(s):  
Andrew John Healey ◽  
Per Christian Sontum ◽  
Svein Kvåle ◽  
Morten Eriksen ◽  
Ragnar Bendiksen ◽  
...  


Polymers ◽  
2018 ◽  
Vol 10 (11) ◽  
pp. 1226 ◽  
Author(s):  
Kuo-Yu Chen ◽  
Si-Ying Zeng

Various amounts of 2-((acryloyloxy)ethyl)trimethylammonium chloride were grafted onto chitosan (CS) via redox polymerization method to obtain water-soluble quaternized CS (QCS). The QCS nanoparticles loaded with bovine serum albumin (BSA) were then produced by ionic gelation with tripolyphosphate (TPP) and further covalently cross-linked with genipin. The formation of QCS nanoparticles was optimized as a function of monomer grafting yield, QCS/TPP weight ratio, and QCS/genipin weight ratio by Box-Behnken design and response surface methodology. The results showed that QCS nanoparticles prepared with a grafting yield of 50%, QCS/TPP weight ratio of 7.67, and QCS/genipin weight ratio of 60 had a particle size of 193.68 ± 44.92 nm, polydispersity of 0.232, zeta potential of +23.97 mV and BSA encapsulation efficiency of 46.37 ± 2.89%, which were close to the predicted values from mathematical models. In vitro drug release studies at pH 1.2 and pH 7.4 exhibited that the release rate of BSA was significantly decreased and the release period was significantly prolonged after QCS nanoparticles cross-linking with genipin. Therefore, QCS nanoparticles cross-linked with TPP/genipin dual cross-linkers may be a promising protein drug carrier for a prolonged and sustained delivery.



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