Development of Chitosan Nanoparticles for Gene Delivery Using Electrohydrodynamic Spraying Techniques

2011 ◽  
Vol 194-196 ◽  
pp. 541-544
Author(s):  
Orapan Paecharoenchai ◽  
Tittaya Suksamran ◽  
Tanasait Ngawhirunpat ◽  
Theerasak Rojanarata ◽  
Praneet Opanasopit

Chitosan nanoparticles were prepared by crosslinking chitosan (CS) with tripolyphosphate (TPP) solution using electrohydrodynamic spraying technique. The effects of CS and TPP concentration as well as electrical potential on particle size and shape were investigated. Appropriated formulations for preparing nanoparticles were chosen to encapsulate DNA. In vitro evaluation of the obtained nanoparticles as gene carrier such as entrapment efficiency and DNA release was performed. The results showed that 2 mg/ml TPP was dropped at 10 kV into 1 mg/ml CS (MW 20 kDa (F1) and 200 kDa (F2)) yielded the spherical shape and small particles of 227.67 and 240.33 nm, respectively. In DNA entrapment study, all formulations were tested by altering DNA loading to 10, 25 and 50 mg/g of CS. The results revealed that F1 with initial DNA 10 mg/g of CS showed the highest entrapment efficiency of 95.31%. While F2 with initial DNA of 25 mg/g of CS showed the highest entrapment efficiency of 89.16%. The DNA release study from CS nanoparticles indicated that the increasing of DNA amount slowed down the release rate. F1 and F2 with the initial DNA of 10 mg/g of CS had faster release rate than those with 25 and 50 mg/g of CS. It can be concluded that F1 yielded the nanoparticles with the smallest size, high DNA entrapment efficiency and enabled DNA sustained release.

2019 ◽  
Vol 19 (6) ◽  
pp. 3616-3620 ◽  
Author(s):  
Zhen Jiao ◽  
Xianjun Zha ◽  
Ziyi Wang ◽  
Xiudong Wang ◽  
Wenjing Fan

The nanoscale drug-loaded micelles can be prepared by the supercritical carbon dioxide evaporation method. Here, response surface methodology is used to optimize this process. The effects of pressure, ScCO2 release rate and the volume ratio of water against ScCO2 on the drug entrapment efficiency (EE) of the obtained micelles are discussed in detail. The obtained second-order polynomial equation can successfully predict the drug EE of the drug-loaded micelles. The maximum EE can reach 70.1% under optimal conditions in which the pressure is 12.27 MPa, the release rate is 10 L min−1 and the volume ratio of water against ScCO2 is 3.67:1. The prepared micelles exhibit a narrow size distribution and relatively regularly spherical shape. In vitro drug release study reveals that the release of paclitaxel from the micelles is slow and sustained.


2019 ◽  
Vol 9 (2) ◽  
pp. 89-96
Author(s):  
Abbaraju Krishna Sailaja ◽  
Juveria Banu

Aim: The aim of this investigation was to develop and characterize naproxen loaded chitosan nanoparticles by emulsion interfacial reaction method. Methodology: For emulsion interfacial reaction method chitosan was used as a polymer. In this method, eight formulations were prepared by varying drug to polymer concentration. Discussion: Out of eight formulations prepared using emulsion interfacial reaction method EI8 formulation was found to be the best formulation. The drug content was observed as 94.4%, entrapment efficiency and loading capacity were found to be 87.5% and 75%, respectively. The mean particle diameter was measured as 324.6nm and the Zeta potential value was found to be -42.4mv. In vitro drug release data showed 97.2% of drug release rate sustained up to 12hrs. Conclusion: The results clearly reveal that EI8 formulation having the highest amount of drug was considered as the best formulation because of its small mean particle diameter, good entrapment efficiency, and stability.


Author(s):  
Leena Jacob ◽  
Abhilash Tv ◽  
Shajan Abraham

Objective: The study was carried out with an objective to achieve a potential sustained release oral drug delivery system of an antihypertensive drug, Perindopril which is a ACE inhibitor having half life of 2 hours. Perindopril is water soluble drug, so we can control or delay the release rate of drug by using release retarding polymers. This may also decrease the toxic side effects by preventing the high initial concentration in the blood.Method: Microcapsules were prepared by solvent evaporation technique using Eudragit L100 and Ethyl cellulose as a retarding agent to control the release rate and magnesium stearate as an inert dispersing carrier to decrease the interfacial tension between lipophilic and hydrophilic phase. Results: Prepared microcapsules were evaluated for the particle size, percentage yield, drug entrapment efficiency, flow property and in vitro drug release for 12 h. Results indicated that the percentage yield, mean particle size, drug entrapment efficiency and the micrometric properties of the microcapsules was influenced by various drug: polymer ratio. The release rate of microcapsules could be controlled as desired by adjusting the combination ratio of dispersing agents to retarding agents.Conclusion:Perindopril microcapsules can be successfully designed to develop sustained drug delivery, that reduces the dosing frequency and their by one can increase the patient compliance.


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.


NANO ◽  
2013 ◽  
Vol 08 (04) ◽  
pp. 1350042 ◽  
Author(s):  
JING WANG ◽  
LI GUO ◽  
LI FANG MA

In this paper, we firstly synthesized glycyrrhetinic acid-modified double amino-terminated poloxamer 188 (GA–NH–POLO–NH–GA). The structure of the synthesized compound was confirmed by 1H-NMR and Fourier transform infrared (FT-IR) spectroscopy. Then the nanoparticles composed of GA–NH–POLO–NH–GA/chitosan (GA–NH–POLO–NH–GA/CTS) were prepared by an ionic gelation process. The characterization of the nanoparticles was measured by dynamic light scattering (DLS) and scanning electron microscope (SEM). The results showed that the nanoparticles were well dispersed with a spherical shape and the particle size was distributed between 100 nm and 300 nm. The cytotoxicity based on MTT assay against cells (QGY-7703 cells and L929 cells) showed that the nanoparticles had low toxicity and good biocompatibility. The encapsulation efficiency and drug loading of 5-fluorouracil-loaded nanoparticles (5-FU nanoparticles) were measured by high-performance liquid chromatography (HPLC) and fluorescence spectroscopy, ultraviolet-visible (UV-vis) absorbance. The encapsulation of 5-Fu-loaded CTS nanoparticles was 12.8% and the drug loading was 2.9%, while the encapsulation of 5-Fu-loaded GA–NH–POLO–NH–GA/CTS nanoparticles was 20.9% and the drug loading was 3.36%. The release profile showed that the GA–NH–POLO–NH–GA/CTS nanoparticles were available for sustained release of 5-Fu. The GA–NH–POLO–NH–GA/CTS nanoparticles have a higher affinity to the QGY-7703 cells, so indicated that the GA–NH–POLO–NH–GA/CTS nanoparticles have the capacity of liver-targeting in vitro.


2017 ◽  
Vol 6 (3) ◽  
pp. 16-22 ◽  
Author(s):  
Satish K. Mandlik ◽  
Nisharani S. Ranpise

The present study investigated the implementation of 32 factorial design of experiment and statistical analysis for the optimization of chitosan nanoparticles containing zolmitriptan an antimigraine drug. The influence of chitosan concentration (X1) and sodium tripoly phosphate (X2) on responses namely nanoparticle size (Y1), and entrapment efficiency (Y2), was studied. As per design, nine runs of nanoparticles were prepared by modified ionic gelation method using high speed vortex mixing. The particle size was found in the range of 151-880 nm and entrapment efficiency was 72.3-81.2%. A statistical analysis was performed using licensed design expert software V.8.0 with respect to ANOVA, regression analysis. The contour plots and response surface plots showed visual representation of relationship between the experimental responses and the set of independent variables. Regression model equations were validated by a numerical and graphical optimization method. Further, optimized drug loaded nanoparticles showed +23.7mV zeta potential indicating storage stability, electron micrograph reflects spherical shape and mixed type of drug release followed by Fickian diffusion (n=0.266) was observed. Thus, using systematic factorial design approach, desirable goals can be achieved in shortest possible time with lesser number of experiments which was proven to be an effective tool in quality by design.Mandlik and Ranpise, International Current Pharmaceutical Journal, February 2017, 6(3): 16-22http://www.icpjonline.com/documents/Vol6Issue3/01.pdf


2014 ◽  
Vol 50 (4) ◽  
pp. 869-876 ◽  
Author(s):  
Neha Gulati ◽  
Upendra Nagaich ◽  
Shubhini Saraf

The objective of the research was to formulate and evaluate selegiline hydrochloride loaded chitosan nanoparticles for the Parkinson's therapy in order to improve its therapeutic effect and reducing dosing frequency. Taguchi method of design of experiments (L9 orthogonal array) was used to get optimized formulation. The selegiline hydrochloride loaded chitosan nanoparticles (SHPs) were prepared by ionic gelation of chitosan with tripolyphosphate anions (TPP) and tween 80 as surfactant. The SHPs had a mean size of (303.39 ± 2.01) nm, a zeta potential of +32.50mV, and entrapment efficiency of SHPs was 86.200 ± 1.38%. The in vitro drug release of SHPs was evaluated in phosphate buffer saline (pH 5.5) using goat nasal mucosa and found to be 82.529% ± 1.308 up to 28 h. Release kinetics studies showed that the release of drug from nanoparticles was anomalous (non-fickian) diffusion indicating the drug release is controlled by more than one process i.e. superposition of both phenomenon, the diffusion controlled as well as swelling controlled release. SHPs showed good stability results as found during stability studies at different temperatures as mentioned in ICH guidelines. The results revealed that selegiline hydrochloride loaded chitosan nanoparticles are most suitable mode of delivery of drug for promising therapeutic action.


Pharmaceutics ◽  
2020 ◽  
Vol 12 (10) ◽  
pp. 973
Author(s):  
Giulia Pitzanti ◽  
Antonella Rosa ◽  
Mariella Nieddu ◽  
Donatella Valenti ◽  
Rosa Pireddu ◽  
...  

Topical psoralens plus ultraviolet A radiation (PUVA) therapy consists in the topical application of 8-methoxypsoralen (8-MOP) followed by the skin irradiation with ultraviolet A radiation. The employment of classical 8-MOP vehicles in topical PUVA therapy is associated with poor skin deposition and weak skin permeability of psoralens, thus requiring frequent drug administration. The aim of the present work was to formulate solid lipid nanoparticles (SLNs) able to increase the skin permeation of 8-MOP. For this purpose, the penetration enhancer Transcutol® P (TRC) was added to the SLN formulation. SLNs were characterized with respect to size, polydispersity index, zeta potential, entrapment efficiency, morphology, stability, and biocompatibility. Finally, 8-MOP skin diffusion and distribution within the skin layers was investigated using Franz cells and newborn pig skin. Freshly prepared nanoparticles showed spherical shape, mean diameters ranging between 120 and 133 nm, a fairly narrow size distribution, highly negative ζ potential values, and high entrapment efficiency. Empty and loaded formulations were almost stable over 30 days. In vitro penetration and permeation studies demonstrated a greater 8-MOP accumulation in each skin layer after SLN TRC 2% and TRC 4% application than that after SLN TRC 0% application. Finally, the results of experiments on 3T3 fibroblasts showed that the incorporation of TRC into SLNs could enhance the cellular uptake of nanoparticles, but it did not increase their cytotoxicity.


Author(s):  
GITA CHAURASIA ◽  
NARENDRA LARIYA

Objective: Ivabradine hydrochloride (IH), a benzazepine derivative used to treat cardiovascular disease angina pectoris. In this study IH-loaded novel carrier systems transfersomes (TFs) and conventional liposomes (CLs) were developed and compared for their efficacy to enhance the stability of drugs from degradation. Methods: TFs formulations (TF-1, TF-2 and TF-3) were prepared by using different biocompatible surfactants; tween-80 (TW), span-80(S) and sodium deoxycholate (SC) in the concentration ratio of 15 parts with 85 parts of soy phosphatidylcholine as phospholipid by thin-film hydration method. These vesicles were compared with CLs formulation (L-1) prepared in 7:3 molar ratio of soy phosphatidylcholine: cholesterol by following the same method. These vesicles were compared for physical appearance, vesicle shape, and size, percentage drug entrapment efficiency (%DEE), deformability index (DI), in vitro percentage cumulative drug release study, and physical stability studies. The chosen optimized novel carriers were observed under scanning electron microscopy. Results: The compared data demonstrated that the physical appearance for all vesicles was turbid and had a spherical shape. The size distribution was in the range of 129.0 nm to 273.5 nm in vesicles. The %DEE (79.0±0.94) and DI (35.0±1.9) was found maximum in TF-1 formulation that was 2.3 times higher than L-1 formulation. The in vitro percentage cumulative drug release study followed second-order polynomial kinetics that was 2.0 times higher than L-1and 2.9 times higher than the plain drug in 30 min (90.4±0.06%) from TF-1. The vesicles were found to be stable at refrigeration conditions. Conclusion: Thus, amongst of all vesicles TW loaded TFs (TF-1) was chosen as an excellent novel vesicular carrier for hydrophilic drugs due to its higher deformability behavior than CLs that protects the certain drugs from biodegradation and provides stability.


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.


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