Experimental Investigation on the Lipid-Lowering Activity of Three Novel Antilipidemic Materials In Vitro

2011 ◽  
Vol 399-401 ◽  
pp. 1568-1572 ◽  
Author(s):  
Si Rong Tan ◽  
Si Hui Wu ◽  
Bing Gao ◽  
Jun Rui Xiao ◽  
Zi Yue Guo ◽  
...  

Chitosan is a new kind of material in life-science, it can be used in lipid-lowering. Chitosan microspheres (CTS-MP) were prepared by spray-drying, chitosan nanoparticles (CTS-NP) and chitosan-capsaicin microspheres (CTS-CAP-MP) were prepared by ionic gelation process. The effect of these samples on lowering lipids was evaluated by measuring its’ binding capacities with lipids under the conditions mimicking the gastrointestinal tract in vitro. Also, the particle sizes of chitosan preparations were examined by scanning electron microscopy (SEM) and particle size analyzer. The results showed that the lipids-binding capacities of CTS-MP and CTS-NP were far more higher than that of CTS and CTS-CAP-MP. In conclusion, CTS-MP and CTS-NP will be better fat-lowing food additives to replace chitosan. The mechanism of lipids-binding in vitro is not only physical adsorption. Particle size is not the determinant factor, electrostatic action is maybe another factor of lipids-binding.

2011 ◽  
Vol 217-218 ◽  
pp. 306-310 ◽  
Author(s):  
Bing Gao ◽  
Si Hui Wu ◽  
Hong Liang Zhang ◽  
Yi Tao ◽  
Zheng Quan Su

Objective: To prepare water-soluble chitosan(WSC) nanoparticles(WSC-NPs) and microspheres(WSC-MPs) , exam the morphology and particle sizes of them and study their effect on lowering lipids . Methods: WSC-NPs and WSC-MPs were prepared by ionic gelation process and spray-drying methods respectively. The effect of WSC-NPs and WSC-MPs on lowering lipids was evaluated by measuring its binding capacities of lipids in the conditions simulating human gastrointestinal tract in vitro. Also, the morphology and particle sizes of WSC-NPs and WSC-MPs were examined under scanning electron microscopy (SEM) and particle sizer. Resluts: WSC-NPs and WSC-MPs were nearly spherical in shape and the mean particles size varied from 200-400 nm and 3-7 μm respectively; The lipids-binding capacities of WSC-NPs and WSC-MPs were more effective compared with water-soluble chiosan. The lipids-binding capacity were enhenced when the particle size were decreased. Conclusion: WSC-NPs and WSC-MPs will be better fat-lowing food additives to replace water-soluble chitosan.


Author(s):  
Ernoviya ◽  
Afriadi

This study was aimed to formulate ketoconazole into nanoemulsion form and to compared the penetration ability of each formula with ketoconazole cream on the market as control. Formulation of nanoemulsion uses spontaneous methods and and also measurement of particle using the Particle Size Analyzer (PSA). In vitro penetration test used Franz diffusion cells. The results showed that nanoemulsion of each formula had different particle  sizes, it was due to the distress of homogenizing two different systems, the duration and speed of stirring also affect the homogenity. The higher concentration of surfactant (tween 80) in the nanoemulation preparation could increasing the penetration ability of the preparation, but if the concentration exceeds the critical micelle concentration (CMC), a tight surfactant matrix (tween 80) will be formed which causes the release of ketoconazole to be slowed. Based on the observation, the highest penetration test was formula F3 as many as 4,268.01 µg/cm.


2011 ◽  
Vol 83 (11) ◽  
pp. 2027-2040 ◽  
Author(s):  
Neralakere Ramanna Ravikumara ◽  
Basavaraj Madhusudhan

In this study, tamoxifen citrate-loaded chitosan nanoparticles (tamoxcL-ChtNPs) and tamoxifen citrate-free chitosan nanoparticles (tamoxcF-ChtNPs) were prepared by an ionic gelation (IG) method. The physicochemical properties of the nanoparticles were analyzed for particle size, zeta (ζ) potential, and other characteristics using photon correlation spectroscopy (PCS), zeta phase analysis light scattering (PALS), scanning electron microscopy (SEM), Fourier transform infrared (FTIR), and differential scanning calorimetry (DSC). The variation in particle size was assessed by changing the concentration of chitosan, pentasodium tripolyphosphate (TPP), and the pH of the solution. The optimized tamoxcL-ChtNPs showed mean diameter of 187 nm, polydispersity of 0.125, and ζ-potential of +19.1 mV. The encapsulation efficiency (EE) of tamoxifen citrate (tamoxc) increased at higher concentrations, and release of tamoxc from the chitosan matrix displayed controlled biphasic behavior. Those tamoxcL-ChtNPs tested for chemosensitivity showed dose- and time-dependent antiproliferative activity of tamoxc. Further, tamoxcL-ChtNPs were found to be hemocompatible with human red blood cells (RBCs) and safe by in vitro cytotoxicity tests, suggesting that they offer promise as drug delivery systems in therapy.


2021 ◽  
Vol 99 (Supplement_3) ◽  
pp. 287-287
Author(s):  
Cheyanne A Myers ◽  
Mario de Haro Marti ◽  
Mireille Chahine ◽  
Gwinyai E Chibisa

Abstract Clinoptilolite (CLN), could potentially improve nitrogen (N) utilization when fed to beef cattle as it can bind ruminal-ammonia-N (NH3-N), limiting its loss and subsequent detoxification into urea-N, which is released into blood and is excreted in urine. However, the effectiveness of CLN is influenced by physical properties such as particle size. Although decreasing the particle size has been shown to increase the binding of ammonium in-vitro, this remains to be evaluated in vivo. Therefore, the objective of this study was to determine the effects of feeding CLN of two different particle sizes (30 and 400 µm) on ruminal NH3-N and plasma-urea-N (PUN) concentrations, ruminal pH, and nutrient intake and apparent total-tract digestibility. Six ruminally-cannulated beef heifers (mean initial BW± SD, 620.8 ± 30.15) were used in a replicated 3 × 3 Latin square design with 21 d periods (sample collection from d 15 to 21). Dietary treatments were: 1) finishing ration with no supplement (CON), 2) CON +30-µm CLN (CL-30), and 3) CON + 400-µm CLN (CL-400). Clinoptilolite was top-dressed (2.5% of diet DM) during morning feeding. Intake was measured daily. Ruminal fluid was collected on d 19 for NH3-N analysis and blood was collected 3 h post-feeding on d 21 for PUN analysis. Indwelling pH loggers were used to measure ruminal pH (d 15 to 21) and grab fecal samples were collected from d 19 to 21 to determine total-tract nutrient digestibility. Statistical analysis was conducted using PROC MIXED in SAS. There was no treatment effect (P ≥ 0.13) on ruminal NH3-N and PUN concentrations, ruminal pH, and nutrient (DM, OM, NDF, ADF and CP) intake and apparent total tract digestibility. In conclusion, feeding CLN to finishing heifers had no effect on measures of N utilization, ruminal pH and nutrient intake and apparent total-tract digestibility.


Author(s):  
S. PATHAK ◽  
S. P. VYAS ◽  
A. PANDEY

Objective: The objective of the present study was to develop, optimize, and evaluate Ibandronate-sodium loaded chitosan nanoparticles (Ib-CS NPs) to treat osteoporosis. Methods: NPs were prepared by the Ionic gelation method and optimized for various parameters such as the effect of concentration of chitosan, sodium tripolyphosphate (TPP), and pH effect on particle size polydispersity index (PDI), zeta potential, and entrapment efficiency. The prepared nanoparticles were characterized using particle size analyzer (DLS), transmission electron microscopy (TEM), scanning electron microscopy (SEM), and Fourier-Transform Infrared spectroscopy (FTIR).  Results: Formulated NPs were obtained in the average nano size in the range below 200 nm in TEM, SEM, and DLS studies. The particle size and encapsulation efficiency of the optimized formulation were 176.1 nm and 63.28%, respectively. The release profile of NPs was depended on the dissolution medium and followed the First-order release kinetics. Conclusion: Bisphosphonates are the most commonly prescribed drugs for treating osteoporosis in the US and many other countries, including India. Ibandronate is a widely used anti-osteoporosis drug, exhibits a strong inhibitory effect on bone resorption performed by osteoclast cells. Our results indicated that Ibandronate sodium-loaded chitosan nanoparticles provide an effective medication for the treatment of osteoporosis.


2015 ◽  
Vol 51 (2) ◽  
pp. 467-477 ◽  
Author(s):  
Abdul Baquee Ahmed ◽  
Ranjit Konwar ◽  
Rupa Sengupta

<p>In this study, we prepared atorvastatin calcium (AVST) loaded chitosan nanoparticles to improve the oral bioavailability of the drug. Nanoparticles were prepared by solvent evaporation technique and evaluated for its particle size, entrapment efficiency, zeta potential, <italic>in vitro</italic> release and surface morphology by scanning electron microscopy (SEM). In addition, the pharmacokinetics of AVST from the optimized formulation (FT5) was compared with marketed immediate release formulation (Atorva<sup>(r))</sup> in rabbits. Particle size of prepared nanoparticles was ranged between 179.3 ± 7.12 to 256.8 ± 8.24 nm with a low polydispersity index (PI) value. Zeta potential study showed that the particles are stable with positive values between 13.03 ± 0.32 to 46.90 ± 0.49 mV. FT-IR studies confirmed the absence of incompatibility of AVST with excipient used in the formulations. <italic>In vitro</italic> release study showed that the drug release was sustained for 48 h. Results of pharmacokinetics study showed significant changes in the pharmacokinetic parameter (2.2 fold increase in AUC) of the optimized formulation as compared to marketed formulation (Atorva<sup>(r))</sup>. Thus, the developed nanoparticles evidenced the improvement of oral bioavailability of AVST in rabbit model.</p>


Author(s):  
SIRIPORN KITTIWISUT ◽  
PAKORN KRAISIT

Objective: This study aimed to characterize the physicochemical properties, including pH, zeta potential, and particle size of propranolol-loaded nanoparticles that were incorporated into a buccal transmucosal drug-delivery system. Methods: An ionotropic gelation technique was used to formulate propranolol-loaded chitosan nanoparticles. Chitosan used as the nanoparticle base, using tripolyphosphate (TPP) as a cross-linking agent. The effects on nanoparticle physical properties, including pH, zeta potential, and particle size were examined when various chitosan [0.150-0.300 % (w/v)] and propranolol contents (0-40 mg) were used during the preparation. The effects of using chitosan solutions with different pH values on nanoparticle properties were also determined. Results: The pH values of all nanoparticles ranged between 4.14–4.55. The zeta potentials of the prepared nanoparticles ranged between 22.6–52.6 mV, with positive charges. The nanoparticle sizes ranged from 107–140 nm, which are within the range of suitable particle sizes for transmucosal preparations. Conclusion: The pH values, zeta potentials, and particle sizes of the nanoparticle formulations were influenced by the concentrations of chitosan and propranolol and by the pH of the initial chitosan solution. The relationships between nanoparticle properties and all factors primarily depended on the ionic charges of the components, especially chitosan. Our study provides beneficial physicochemical knowledge for the further development of chitosan-based nanoparticles containing propranolol for buccal drug delivery systems.


2012 ◽  
Vol 2012 ◽  
pp. 1-11 ◽  
Author(s):  
Haliza Katas ◽  
Zahid Hussain ◽  
Tay Chai Ling

Hydrocortisone (HC) has formed the mainstay for the management of atopic dermatitis. Hence, HC-loaded chitosan nanoparticles were prepared by ionic crosslinking of high, low molecular weight chitosan (HMwt, LMwt CS) and N-trimethyl chitosan (TMC) with tripolyphosphate. HC loading into CS nanoparticles was confirmed by FT-IR. The particle size of HC-loaded HMwt, LMwt, and TMC nanoparticles was increased from243±12,147±11,and124±9 nm to337±13,222±14,and195±7 nm, respectively, by increasing the pH of CS solution. Their respective zeta potential and entrapment efficiency (EE) were significantly decreased by increasing the pH of CS solution. The swelling ratios of HC loaded HMwt, LMwt, and TMC NPs were increased when the pH of incubating media (PBS) was increased. The same increasing trend was observed in particle size and EE of HC loaded as the CS concentration was increased. The HC loaded CS NPs were generally nonspherical.In-vitropermeation studies showed that HC was efficiently released from the CS NPs in QV cream while in aqueous cream CS NPs provided a sustained release for HC. Thus, it is anticipated that CS NPs are the promising delivery system for anti-inflammatory drugs.


2011 ◽  
Vol 282-283 ◽  
pp. 539-544 ◽  
Author(s):  
Jia Lei Li ◽  
Yuan Gang Zu ◽  
Xiu Hua Zhao ◽  
Zhi Gang An ◽  
Xiao Yu Sui ◽  
...  

Epigallocatechin-3-gallate (EGCG), a principal polyphenolic, which is most abundant and active component in tea. It is considered key to these healthful qualities. However, EGCG used in clinical application which is still shortcomings of short half-life and low bioavailability. Chitosan (CS) has been widely used in pharmaceutical and medical areas, particularly for its potential in the development of controlled release drug delivery systems due to its well properties. In this study, we prepared EGCG-loaded chitosan nanoparticles by ionic polymeric method using sodium tripolyphosphate(TPP) as ionic polymeric agent successfully. Results controlled conditions (concentration of CS, 2 mg/mL; pH = 5.4; volume of TPP(0.5 mg/mL), 6.6 mL; amount of EGCG, 15 mg; ionic polymeric time, 24 h at room temperature (0.5 mL/min))volume of TPP(0.5 mg/mL), 6.6 mL; amount of EGCG, 15 mg; ionic polymeric time, 24 h at room temperature (0.5 mL/min)) for entrapment efficiency, loading efficiency, mean particle size and Zeta potential, were found to be 62.3 %, 33.8 %, 141.5 ± 0.4 nm and -31.21 ± 0.54 mV, respectively, and CS-EGCG-NPS have well property of sustained release.


2010 ◽  
Vol 7 (3) ◽  
pp. 317-322 ◽  
Author(s):  
Vishnu Kumar ◽  
Mohammad Mubin Khan ◽  
Ashok Kumar Khanna ◽  
Ranjana Singh ◽  
Sushma Singh ◽  
...  

The lipid lowering activity ofAnthocephalus indicus(family Rubiaceae; Hindi name Kadamba) root extract has been studied in triton WR-1339 induced hyperlipidemia in rats. In this model, feeding with root extract (500 mg kg−1b.w.) lowered plasma lipids and reactivated post-heparin lipolytic activity in hyperlipidemic rats. Furthermore, the root extract (50–500 μM) inhibited the generation of superoxide anions and hydroxyl radicals, in both enzymic and non-enzymic systems,in vitro. The results of the present study demonstrated both lipid lowering and antioxidant activities in root extract ofA. indicus, which could help prevention of hyperlipidemia and related diseases.


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