scholarly journals Sodium Alginate Nanoparticles of Isoniazid: Preparation and Evaluation

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
Sumit Kumar ◽  
Dinesh Chandra Bhatt
Keyword(s):  
Particle Size ◽  
Sodium Alginate ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Average Particle ◽  
In Vitro Drug Release ◽  
Ionotropic Gelation ◽  
Preparation And Evaluation

Fabrication and evaluation of the Isoniazid loaded sodium alginate nanoparticles (NPs) was main objective of current investigation. These NPs were engineered using ionotropic gelation technique. The NPs fabricated, were evaluated for average particle size, encapsulation efficiency, drug loading, and FTIR spectroscopy along with in vitro drug release. The particle size, drug loading and encapsulation efficiency of fabricated nanoparticles were ranging from 230.7 to 532.1 nm, 5.88% to 11.37% and 30.29% to 59.70% respectively. Amongst all batches studied formulation F-8 showed the best sustained release of drug at the end of 24 hours.

Preparation of Poly[lactic-co-glycolic] Acid Nanospheres and Its Role in Hepatoma Cells

2021 ◽  
Vol 21 (2) ◽  
pp. 977-986
Author(s):  
Zhongxing Shi ◽  
Jinping Li ◽  
Hongwei Liang ◽  
Hongbo Hu ◽  
Huijie Jiang
Keyword(s):  
Particle Size ◽  
Release Rate ◽  
Hepg2 Cells ◽  
Glycolic Acid ◽  
Drug Loading ◽  
Average Particle Size ◽  
Plga Nanoparticles ◽  
Toxin Gene ◽  
Average Particle

Poly[lactic-co-glycolic] acid (PLGA) targeting nanoparticles AFP/PLGA/Dt386, loaded with Dt386 plasmid of diphtheria toxin gene, modified by Alpha fetoprotein (AFP) monoclonal antibody, is prepared. Its physical and chemical properties and its effect on HepG2 cells are studied. Firstly, Dt386 expression plasmid pET11a/Dt386 is constructed and PLGA nanoparticles are prepared by emulsion solvent evaporation (ESE). Scanning electron microscope (SEM) is used to observe its morphology. Laser Particle Sizer is used to measure the particle size. In addition, the encapsulation efficiency, drug loading and in vitro release rate of PLGA nanoparticles are measured. Carboxy fluorescein and rhodamine fluorescein are used to double label IgG/PLGA/Dt386 and AFP/PLGA/Dt386 nanospheres, respectively, the entry of nanospheres into HepG2 cells are observed at 3 h and 12 h. The effect of AFP/PLGA/Dt386 nanospheres on the migration of HepG2 cells is examined by wounding healing assay. Transwell chamber experiment is used to detect the effect of AFP/PLGA/Dt386 nanospheres on the invasion of HepG2 cells. MTT method is utilized to determine the inhibitory activity of nanoparticles on HepG2 cell proliferation. After treated with IgG/PLGA/Dt386 and AFP/PLGA/Dt386 nanoparticles for 48 hours, flow cytometry is used to detect the apoptosis rate and cell cycle of HepG2 cells in each group. The results show that the prepared nanospheres have regular morphology, flat surface, average particle size of 265.72±12.46 nm, zeta potential of −18.15 mV. The average entrapment efficiency and drug loading are 78.48±1.71% and 3.16±0.35%, respectively. The nanoparticles release slowly and stably in vitro. At the 10th day, the release rate reaches 75.13%. PLGA nanospheres can effectively protect DNA from nuclease degradation. The results show that AFP/PLGA/Dt386 nanospheres have biological targeting effect and can be enriched in cells. AFP/PLGA/Dt386 nanoparticles can significantly inhibit the migration, invasion and proliferation of HepG2 cells, and promote apoptosis.

scholarly journals Formulation and Evaluation of sustained release Microspheres of Atorvastatin using Chitosan and Alginate

2017 ◽  
Vol 9 (3) ◽  
Author(s):  
Y. M. Charde ◽  
S. G. Dhage ◽  
G. K. Lohiya ◽  
J. G. Avari
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Sodium Alginate ◽  
Calcium Binding ◽  
Encapsulation Efficiency ◽  
Low Cost ◽  
Entrapment Efficiency ◽  
In Vitro Drug Release ◽  
Ionotropic Gelation

Certain problems regarding the drugs like high first pass metabolism, also the bioavailability of the certain drugs varies due to instability in acidic environment of stomach. Hence, to resolve such problems the drug should be incorporated in the microspheres for sustained release using a suitable polymer. Natural polymer like chitosan gained great interest in pharmaceutical sector because of its advantages like biodegradability, biocompatibility, non-toxicity, non-immunogenicity and low cost. In the present study, formulation and evaluation of polymeric microspheres of Atorvastatin Calcium was carried out and the release profile of such drug using the alginate and chitosan was studied. Microspheres were prepared for sustained release of drug using chitosan and alginate polymers by ionotropic gelation method. Microspheres were spherical in shape, having good flow properties and further its encapsulation efficiency, swelling index, micromeritic study, in- vitro drug release study and stability studies were performed in order to characterize microspheres. Three different concentrations of sodium alginate (1%, 2% and 3%) were used. The higher encapsulation efficiency was observed as the concentration of alginate increased. This is due to the greater availability of active calcium binding sites in the polymeric chains and consequently the greater degree of cross linking. The highest encapsulation efficiency (88.36) was achieved with 2% w/v sodium alginate in combination with 3% chitosan (F6). Among the prepared formulations with respect to the entrapment efficiency, swelling studies and in vitro drug release, the alginate-chitosan microspheres prepared by ionotropic gelation using calcium chloride found to be better than ionically cross linked alginate spheres alone. Therefore, dual cross-linked, microspheres are promising carrier for sustained release of drug.

scholarly journals Casein Micelles as Nanocarriers for Benzydamine Delivery

Polymers ◽  
2021 ◽  
Vol 13 (24) ◽  
pp. 4357
Author(s):  
Nikolay Zahariev ◽  
Maria Marudova ◽  
Sophia Milenkova ◽  
Yordanka Uzunova ◽  
Bissera Pilicheva
Keyword(s):  
Particle Size ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Crosslinking Agent ◽  
Morphological Characteristics ◽  
Average Particle ◽  
Scanning Calorimetry ◽  
Casein Micelles ◽  
Fourier Transformed Infrared Spectroscopy

The aim of the present work was to optimize the process parameters of the nano spray drying technique for the formulation of benzydamine-loaded casein nanoparticles and to investigate the effect of some process variables on the structural and morphological characteristics and release behavior. The obtained particles were characterized in terms of particle size and size distribution, surface morphology, production yield and encapsulation efficiency, drug-polymer compatibility, etc., using dynamic light scattering, scanning electron microscopy, differential scanning calorimetry, and Fourier transformed infrared spectroscopy. Production yields of the blank nanoparticles were significantly influenced by the concentration of both casein and the crosslinking agent. The formulated drug-loaded nanoparticles had an average particle size of 135.9 nm to 994.2 nm. Drug loading varied from 16.02% to 57.41% and the encapsulation efficiency was in the range 34.61% to 78.82%. Our study has demonstrated that all the investigated parameters depended greatly on the polymer/drug ratio and the drug release study confirmed the feasibility of the developed nanocarriers for prolonged delivery of benzydamine.

scholarly journals Development of a novel intraarticular injection of diclofenac for the treatment of arthritis: a preclinical study in the rabbit model

2021 ◽  
Author(s):  
Xinyuan Wen ◽  
Xiaoqing Huang ◽  
Huosheng Wu
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Rabbit Model ◽  
Intraarticular Injection ◽  
Average Particle ◽  
Prepared Nanoparticles

Purpose: To develop a novel intraarticular injection of diclofenac for the treatment of arthritis. Method: Diclofenac loaded nanoparticles were prepared by a nanoprecipitation technique using Eudragit L 100 as the polymer and polyvinyl alcohol as the surfactant. The nanoparticles were evaluated for particle size, zeta potential, scanning electron microscopy, drug release, encapsulation efficiency, and loading efficiency studies. The optimized nanoparticulate formulation was developed for intra articular injection. Intraarticulate injection was evaluated for pH, appearance, viscosity, osmolarity and syringability studies. The optimized injection formulation was tested in an arthritic model consisting of 25 rabbits. Result: Nanoprecipitation method was found to be suitable for diclofenac nanoparticles. The shape of the prepared nanoparticles was found to be spherical and devoid of any cracks and crevices. The average particle size of a diclofenac nanoparticle was found to range from 87±0.47 to 103±0.26 nm. The zeta potential of the prepared nanoparticles was found to be in the range of 0.598±0.34 to 0.826±0.25 mV. The encapsulation efficiency was found to be between 73.45% to 99.03%, while the drug loading was observed between 10.34 to 35.32%. The percentage drug release at 12 hours was found to range from 73.45% to 99.03%. Conclusion: The developed intraarticular injection was found to be within the physically and chemically accepted limits. Animals treated with the intra articular injection of diclofenac showed a significant reduction in swelling as compares to the other groups.

scholarly journals Formulation and Evaluation of Mucoadhesive Acarbose Microspheres

2016 ◽  
Vol 1 (1) ◽  
Author(s):  
Manish Kumar Sharma
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Guar Gum ◽  
Hydroxypropyl Methylcellulose ◽  
Average Particle Size ◽  
Prolonged Release ◽  
Average Particle ◽  
In Vitro Drug Release ◽  
In Vitro Adhesion

The purpose of the present investigation was the formulation and characterization of mucoadhesive sustained release microsphere of antidibetic drug Acarbose that would adhere in mucosa and release continuously to provide long term effect. There was various formulations of Acarbose were prepared by solvent evaporation technique using hydroxypropyl methylcellulose (HPMC), Sodium Alginate, Carbopol, Xanthan gum, Guar gum as a polymer. The prepared mucoadhesive microspheres were evaluated for particle size, surface morphology, drug entrapment efficiency, Drug content, buoyancy percentage and In-vitro drug release, In-vitro adhesion test and stability studies. The particle was found to be discrete and spherical with the average particle size in the range of 105.5 to 413.5μm. As the concentration of polymers increases it affects the various evaluation parameters like particle size, in-vitro drug release and In-vitro adhesion. The floating microspheres of optimized formulation exhibited the prolonged release of 85.8% in continuous manner up to 12 hrs. It is concluded that the optimized formulation of Acarbose mucoadhesive microspheres can be selected for sustained drug delivery system for improved bioavailability.

scholarly journals Preparation, Characteristics, and Controlled Release Efficiency of the Novel PCL-PEG/EM Rod Micelles

2021 ◽  
Vol 2021 ◽  
pp. 1-10
Author(s):  
Huiling Song ◽  
Yu Yin ◽  
Jiahui Peng ◽  
Zixiu Du ◽  
Wei Bao
Keyword(s):  
Staphylococcus Aureus ◽  
Controlled Release ◽  
Encapsulation Efficiency ◽  
Orthogonal Design ◽  
Drug Loading ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Average Particle ◽  
Model Drug

In order to achieve sustained and controlled release of the hydrophobic cargoes, improve the bioavailability, and reduce the side effects of antibiotics, the model drug erythromycin (EM) was used to prepare polycaprolactone-polyethylene glycol (PCL-PEG)/EM micelles. PCL-PEG, a biocompatible and biodegradable amphiphilic polymer, was used as carrier material of micelles to optimize the formulation and preparation process by orthogonal design. The morphology, stability, drug loading, and encapsulation efficiency and the in vitro release behavior of the micelles were investigated. In addition, activity assays of anti-Staphylococcus aureus were performed. The results indicated that PCL-PEG/EM were rod-like micelles with an average particle size of 220 ± 2.6  nm and a zeta potential of +19 mV. The average drug loading and encapsulation efficiency were approximately 6.5% and 97.0%, respectively. The micelles were stable in the serum within three days. At the effective concentration of the drug, the formulation indicated no apparent toxicity to the cells. The micelles were able to rapidly enter Staphylococcus aureus (S. aureus) and to provide sustained release cargoes that effectively inhibited S. aureus proliferation. The present study provided a new platform for the rational and effective use of hydrophobic antibiotics to treat infections.

Preparation of Epidermal Growth Factor-Modified Targeted Doxorubicin Nanoliposomes and Therapy of Liver Cancer

2021 ◽  
Vol 21 (9) ◽  
pp. 4565-4572
Author(s):  
Yongan Chen ◽  
Lei Cheng ◽  
Dan Yu ◽  
Jie Shen ◽  
Zhengrong Zhou ◽  
...  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Rate ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Hepatoma Cells ◽  
Average Particle ◽  
Therapeutic Effects ◽  
Drug Release Rate

The objective of this study was to prepare doxorubicin-loaded EGF modified PEG-nanoparticles and evaluate its targeting capability and therapeutic effects with EGFR-expressing hepatocellular carcinoma cells. The morphology, particle size distribution, and doxorubicin content of the nanoparticles were measured, and the drug loading and encapsulation efficiency were calculated. The doxorubicin nanoparticles prepared were regular circular, with good dispersibility, no adhesion, and the average particle size was (136.7±9.3) nm. The average encapsulation efficiency was (76.67±8.63)%, the average drug loading was (3.86±0.55)%; the drug release rate of doxorubicin was 100% for 12 h, and the doxorubicin nanometer was loaded. The drug release rate of the granules was 52.9% at 24 h and 81.2% at 144 h. The inhibition rate of the proliferation of hepatocarcinoma cells by the doxorubicin-containing nanoparticles was slower than that of doxorubicin, and the IC50 of the two cells was 1.844 and 0.345 μg/mL, respectively. At the same time, apoptosis and cycle analysis showed that the doxorubicin nanoparticles could significantly inhibit the cell cycle of hepatoma cells and promote the apoptosis of hepatoma cells. This study successfully produced nanoparticles loaded with doxorubicin targeting EGFR, which has a good sustained release effect, and its antitumor effect is stronger than free doxorubicin.

scholarly journals DEVELOPMENT AND IN VITRO EVALUATION OF 5-FLUOROURACIL NANOPARTICLES BY SALTING OUT TECHNIQUE

2020 ◽  
pp. 166-171
Author(s):  
SAILAJA PB ◽  
JEEVANA JYOTHI B
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Average Particle Size ◽  
Average Particle ◽  
Salting Out ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
S 100 ◽  
Percentage Release

Objectives: At the current miserable state of the prevalence of cancers, there is a need for the development of simple technologies to prepare formulations of anticancer drugs with less economy and investment. Hence, the aim of the present work is to prepare nanoparticles of 5-fluorouracil (5-FU) by simple technique, such as salting out method. Methods: Nanoparticles containing 10 mg of 5-FU were prepared by salting out method using Eudragit-100 as polymer. The prepared nanoparticles were evaluated by particle size, zeta potential, in vitro drug release studies, and drug-excipient interaction studies. Results: Nanoparticles prepared by salting out methods showed higher dissolution rate for formulation F3 and F5 revealed high percentage release of 98.6±0.24 in 60 min and 86.5±0.39% in 120 min. Fourier transform infrared (FTIR) spectra revealed no interaction between drug and excipients used for preparation. Conclusion: 5-FU nanoparticles can be produced successfully by salting out method using drug to polymer (Eudragit S-100) ratio of 1:3 to possess ideal drug release characteristics and average particle size of 205.1 nm.

scholarly journals Preparation of Folic Acid-conjugated Albumin Nanoparticles Containing Paclitaxel using High-pressure Homogenisation Coagulation Method

2021 ◽  
Author(s):  
Yan Chu ◽  
Shuo Chai ◽  
Hong Pan ◽  
Jiayi Qian ◽  
Cuiyan Han ◽  
...  
Keyword(s):  
Particle Size ◽  
High Pressure ◽  
Folic Acid ◽  
Conversion Rate ◽  
Encapsulation Efficiency ◽  
Average Particle Size ◽  
Great Influence ◽  
Average Particle ◽  
Freeze Dried

Abstract In this study, we prepared and evaluated folic acid-conjugated albumin-paclitaxel (FA-BSA-PTX) nanoparticles using a new green technique, called the high-pressure homogenisation coagulation method (HPHCM). The effect of process parameters such as BSA concentration, coagulant concentration, homogenisation time, homogenisation pressure, water/ethanol ratio, and BSA/PTX ratio was analysed to optimise nanoparticle size, albumin conversion rate, and encapsulation efficiency. BSA concentration was found to exert a great influence on albumin conversion rate and particle size. Meanwhile, the BSA/PTX ratio significantly affected the nanoparticle encapsulation efficiency. Electron microscopy showed that the freeze-dried particles mostly existed in the form of dimers and trimers with an average particle size of 300–400 nm. Infrared spectroscopy indicated that PTX was well encapsulated in BSA. Raman spectra of the synthesised nanoparticles indicated changes in the disulphide bond configuration and protein structure. In vitro drug-release analysis showed that crosslinked nanoparticles exhibited a sustained release. Furthermore, in vitro cell-uptake studies on HeLa cells showed that FA can be used as a targeting ligand for albumin carriers to enhance the active targeting effect of the nanoparticles with a high FR expression. These results suggest that HPHCM is an effective method to prepare FA-BSA-PTX drug-delivery systems.

Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

2020 ◽  
Vol 12 (2) ◽  
pp. 4474-4491
Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Tem Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

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