Preparation and Characterization of Folate-Decorated Chitosan Microspheres as a Sustained-Release Drugs Carrier

2013 ◽  
Vol 684 ◽  
pp. 57-62 ◽  
Author(s):  
Zhi Hua Xing
Keyword(s):  
Encapsulation Efficiency ◽  
Average Particle Size ◽  
Morphological Characteristics ◽  
Average Particle ◽  
Loading Capacity ◽  
Chitosan Microspheres ◽  
Ionic Crosslinking ◽  
Artificial Gastric Juice

Folic acid-chitosan (FA-CTS) and 10-hydroxycamptothecin (HCPT)-loaded folate-conjugated chitosan (FA-CTS/HCPT) microspheres were prepared by the ionic crosslinking method.The morphological characteristics of microspheres were examined using a scanning electron microscope (SEM). The average particle size and size distribution were determined by dynamic light scattering. The drug encapsulation efficiency (EE) , loading capacity (LC)and release characteristics in vitro were determined using ultraviolet spectrophotometer.The results shown that the microspheres are uniform spherical and regular with a size between 19.79 and81.40μm.Optimized preparation parameters lead to the successful preparation of hydroxycamptothecin-loaded folate-conjugated chitosan microspheres characterized with encapsulation efficiency and loading capacity up to (86.8±0.1)% and 20.6±0.3 % respectively. More then 90% of 10-hydroxycamptothecin was released from microspheres in 4 h at artificial gastric juice, 8h at artificial small intestinal fluid with a good delayed release effect.

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.

scholarly journals Preparation and characterization of domperidone nanoparticles for dissolution improvement

2018 ◽  
Vol 27 (1) ◽  
pp. 39-52
Author(s):  
Mohammed Sabar Al-lami ◽  
Malath H. Oudah ◽  
Firas A. Rahi
Keyword(s):  
Particle Size ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Precipitation Method ◽  
Average Particle ◽  
Antisolvent Precipitation ◽  
Stirring Time

This study was carried out to prepare and characterize domperidone nanoparticles to enhance solubility and the release rate. Domperidone is practically insoluble in water and has low and an erratic bioavailability range from 13%-17%. The domperidone nanoparticles were prepared by solvent/antisolvent precipitation method at different polymer:drug ratios of 1:1 and 2:1 using different polymers and grades of poly vinyl pyrolidone, hydroxy propyl methyl cellulose and sodium carboxymethyl cellulose as stabilizers. The effect of polymer type, ratio of polymer:drug, solvent:antisolvent ratio, stirring rate and stirring time on the particle size, were investigated and found to have a significant (p? 0.05) effect on particle size. The best formula was obtained with lowest average particle size of 84.05. This formula was studied for compatibility by FTIR and DSC, surface morphology by FESEM and crystalline state by XRPD. Then domperidone nanoparticles were formulated into a simple capsule dosage form in order to study of the in vitro release of drug from nanoparticles in comparison raw drug and mixture of polymer:drug ratios of 2:1. The release of domperidone from best formula was highly improved with a significant (p? 0.05) increase.

Development of propolis nanoparticles for the treatment of bovine mastitis: in vitro studies on antimicrobial and cytotoxic activities

2019 ◽  
Vol 99 (4) ◽  
pp. 713-723 ◽  
Author(s):  
Gabriela Tasso Pinheiro Machado ◽  
Maria Beatriz Veleirinho ◽  
Letícia Mazzarino ◽  
Luiz Carlos Pinheiro Machado Filho ◽  
Marcelo Maraschin ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Encapsulation Efficiency ◽  
Average Particle Size ◽  
Physical Stability ◽  
Bovine Mastitis ◽  
Total Phenolic ◽  
Cytotoxic Activities ◽  
Average Particle ◽  
Propolis Extract

This study describes the development of propolis nanoparticles (PNP) to treat bovine mastitis. Three PNP prepared with varying concentrations of propolis (5% and 7%, w/v) and the surfactants [poloxamer (1%, 3%, and 4%, w/v) and soy lecithin (0.25%, 0.7%, and 1%, w/v)]. PNP were characterized according to their size, polydispersity, zeta potential, pH, morphology, and physical stability. PNP were evaluated for their in vitro antimicrobial and cytotoxic effects. PNP obtained were spherical with a monodisperse distribution (polydispersity index < 0.2) and an average particle size between 181 and 201 nm. Stability studies showed that PNP were stable over 150 d. The encapsulation efficiency of total phenolic content varied between 73% and 91%. The chromatographic profile of phenolic compounds from PNP showed selective encapsulation efficiency according to the polarity of compounds. All PNP showed antimicrobial activity against Staphylococcus aureus with a minimum inhibitory concentration ranging from 156 to 310 μg mL−1. The IC50 (the concentration responsible for reduction of cellular viability by half) for epithelial cells of bovine mammary gland (MAC-T, mammary alveolar cell-T) varied from 122.2 to 268.4 μg mL−1. Results showed that PNP represent a promising nanocarrier for high concentrations of propolis extract in a stable aqueous medium, while, at the same time, presenting antimicrobial activity accompanied by moderate cytotoxicity to the MAC-T cells.

scholarly journals Physico-Chemical, In Vitro and Ex Vivo Characterization of Meloxicam Potassium-Cyclodextrin Nanospheres

Pharmaceutics ◽  
2021 ◽  
Vol 13 (11) ◽  
pp. 1883
Author(s):  
Patrícia Varga ◽  
Rita Ambrus ◽  
Piroska Szabó-Révész ◽  
Dávid Kókai ◽  
Katalin Burián ◽  
...  
Keyword(s):  
Spray Drying ◽  
Ex Vivo ◽  
Average Particle Size ◽  
Rapid Onset ◽  
Average Particle ◽  
Nasal Drug Delivery ◽  
Onset Of Action ◽  
Physico Chemical

Nasal drug delivery has many beneficial properties, such as avoiding the first pass metabolism and rapid onset of action. However, the limited residence time on the mucosa and limited absorption of certain molecules make the use of various excipients necessary to achieve high bioavailability. The application of mucoadhesive polymers can increase the contact time with the nasal mucosa, and permeation enhancers can enhance the absorption of the drug. We aimed to produce nanoparticles containing meloxicam potassium (MEL-P) by spray drying intended for nasal application. Various cyclodextrins (hydroxypropyl-β-cyclodextrin, α-cyclodextrin) and biocompatible polymers (hyaluronic acid, poly(vinylalcohol)) were used as excipients to increase the permeation of the drug and to prepare mucoadhesive products. Physico-chemical, in vitro and ex vivo biopharmaceutical characterization of the formulations were performed. As a result of spray drying, mucoadhesive nanospheres (average particle size <1 µm) were prepared which contained amorphous MEL-P. Cyclodextrin-MEL-P complexes were formed and the applied excipients increased the in vitro and ex vivo permeability of MEL-P. The highest amount of MEL-P permeated from the α-cyclodextrin-based poly(vinylalcohol)-containing samples in vitro (209 μg/cm2) and ex vivo (1.47 μg/mm2) as well. After further optimization, the resulting formulations may be promising for eliciting a rapid analgesic effect through the nasal route.

scholarly journals Preparation of PLGA Nanoparticles Encapsulated with Fluorescent Probe Coumarin-6

2019 ◽  
Author(s):  
Elizebeth Purr ◽  
Jacob Marshall ◽  
John Smith
Keyword(s):  
Fluorescent Probe ◽  
Encapsulation Efficiency ◽  
Average Particle Size ◽  
Double Emulsion ◽  
Plga Nanoparticles ◽  
Utilization Rate ◽  
Average Particle ◽  
Acid Copolymer ◽  
Coumarin 6

AbstractIn this report, we provided a novel platform to prepare fluorescent probe coumarin-6 nanoparticles by using biodegradable material polylactic acid-glycolic acid copolymer (PLGA) as material. The coumarin-6-PLGA nanoparticles were prepared by double emulsion and solvent evaporation. The encapsulation efficiency and releasing kinetics were also investigated. Results indicate that the encapsulation efficiency of coumarin-6 nanoparticles was 51.6%, the utilization rate was 81.9%, the average particle size was 135 nm, and the leakage rate of coumarin-6 in vitro was lower than 72 h. 2%. Our experimental results provide evidence that PLGA nanoparticles can effectively encapsulate fluorescent probe Coumarin-6 and release the probe in a controlled manner.

Synthesis and Characterization of Alginate-Based Hydrogel Microbeads for Magnesium Release

2016 ◽  
Author(s):  
Shalil Khanal ◽  
Udhab Adhikari ◽  
Nava P. Rijal ◽  
Devdas Pai ◽  
Jagannathan Sankar ◽  
...  
Keyword(s):  
Particle Size ◽  
Tissue Injury ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Synthesis And Characterization ◽  
Average Particle ◽  
Release Study ◽  
Vitro Release

Magnesium injection is a suitable approach for replenishment of its ions (Mg++) during neural or tissue injury and stroke to avoids risks associated with abnormally low level of Mg++ in blood. In this study, alginate encapsulated magnesium sulfate microbeads were fabricated by the electrospraying technique for Mg++ delivery. Microbeads were evaluated for particle size and surface morphology using inverted optical microscopy and scanning electron microscopy (SEM) respectively. Average particle size of 200–500 μm for hydrated and 50–200 μm for dry beads were observed. An in vitro release study of Mg++ was performed; revealing a cumulative release of ∼50% within first 24 h. This strategy can potentially be useful for the targeted local delivery of magnesium at required concentrations and subsequently enhance the therapeutic efficacy of magnesium in treating tissue injury or stroke.

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 Preparation and in vitro release of fluorouracil polylactide glycolide-polyethylene glycol monomethyl ether nanoparticles

2019 ◽  
Author(s):  
Anil Shumroni ◽  
David Gupta
Keyword(s):  
Polyethylene Glycol ◽  
Encapsulation Efficiency ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Monomethyl Ether ◽  
Burst Release ◽  
Average Particle ◽  
Glycol Monomethyl Ether ◽  
Vitro Release

AbstractThis report demonstrates a novel strategy to prepare fluorouracil polylactide glycolide-polyethylene glycol monomethyl ether (PLGA-mPEG) nanoparticles and study their in vitro release characteristics. Fluorouracil PLGA-mPEG nanoparticles were prepared by nanoprecipitation method. The encapsulation efficiency was determined by high performance liquid chromatography. Based on the single factor experiment, the prescription and preparation process were optimized by orthogonal experiments. The in vitro release characteristics of nanoparticles were studied by dynamic membrane dialysis. Results The prepared nanoparticles were relatively uniform spheroidal particles with an average particle size of about 124. 3 nm, a Zeta potential of - 20. 6 mV, and an average encapsulation efficiency of (44.72 ± 0.38%). In vitro drug release experiments showed that the particle burst release was less than 30% at 2 h, and the drug was slowly released within 48 h after burst release.

Transferrin Modified Dioscin Loaded PEGylated Liposomes: Characterization and In Vitro Antitumor Effect

2020 ◽  
Vol 20 (3) ◽  
pp. 1321-1331 ◽  
Author(s):  
Yuanyuan Wang ◽  
Yining Yang ◽  
Yibin Yu ◽  
Jinyu Li ◽  
Weisan Pan ◽  
...  
Keyword(s):  
Laser Scanning ◽  
Drug Loading ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Laser Scanning Confocal Microscopy ◽  
Average Particle ◽  
Scanning Confocal Microscopy ◽  
Drug Entrapment Efficiency

In this study, a novel transferrin modified liposomal dioscin was prepared by the film dispersion method. The transferrin modified dioscin loaded liposomes (Tf-Lip/Dio) were near-spherical in morphology and had an average particle size of 140.07±1.33 nm, a narrow polydispersity index of <0.2 and a relatively stable zeta potential of -23.7±1.16 mV. The drug entrapment efficiency (EE) and drug loading (DL) of Tf-Lip/Dio were 88.94±1.02% and 4.16±0.05%, respectively. Tf-Lip/Dio exhibited a sustained release characterization of approximately 30% of the total dioscin content after 72 h at 37 °C. Tf-Lip/Dio showed higher cytotoxic efficacy after incubation for 24 h in both HeLa cells and HepG2 cells than in nonmodified liposomes. The enhanced antitumor activity of Tf-Lip/Dio might be due to the increased intracellular uptake, which was corroborated by laser scanning confocal microscopy and flow cytometry. Furthermore, hemolysis experiments preliminarily verified the safety of its intravenous injection. Overall, this study demonstrates Tf-Lip/Dio to be a favorable delivery vehicle for dioscin in future cancer therapy.

scholarly journals Biomimetic Growth of Hydroxyapatite on SiO2 Microspheres to Improve Its Biocompatibility and Gentamicin Loading Capacity

Materials ◽  
2021 ◽  
Vol 14 (22) ◽  
pp. 6941
Author(s):  
Alejandra E. Herrera-Alonso ◽  
María C. Ibarra-Alonso ◽  
Sandra C. Esparza-González ◽  
Sofía Estrada-Flores ◽  
Luis A. García-Cerda ◽  
...  
Keyword(s):  
Drug Loading ◽  
Average Particle Size ◽  
Sodium Dodecyl ◽  
Mechanical Damage ◽  
Spherical Shape ◽  
Average Particle ◽  
Loading Capacity ◽  
Bioactive Materials ◽  
Sio2 Microspheres

The interest in multifunctional biomaterials to be implanted are also able to release drugs that reduce pain and inflammation or prevent a possible infection has increased. Bioactive materials such as silica (SiO2) containing surface silanol groups contribute to the nucleation and growth of hydroxyapatite (HAp) in a physiological environment. Regarding biocompatibility, the spherical shape of particles is the desirable one, since it does not cause mechanical damage to the cell membrane. In this work, the synthesis of SiO2 microspheres was performed by the modified Stöber method and they were used for the biomimetic growth of HAp on their surface. The effect of the type of surfactant (sodium dodecyl sulphate (SDS), cetyltrimethylammonium bromide (CTAB), and polyethylene glycol (PEG)), and heat treatment on the morphology and size of SiO2 particles was investigated. Monodisperse, spherical-shaped SiO2 microparticles with an average particle size of 179 nm, were obtained when using PEG (SiO2-PEG). The biomimetic growth of HAp was performed on this sample to improve its biocompatibility and drug-loading capacity using gentamicin as a model drug. Biomimetic growth of HAp was confirmed by FTIR-ATR, SEM-EDX and TEM techniques. SiO2-PEG/HAp sample had a better biocompatibility in vitro and gentamicin loading capacity than SiO2-PEG sample.

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