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.

Enhanced oral bioavailability of nisoldipine-piperine-loaded poly-lactic-co-glycolic acid nanoparticles

2017 ◽  
Vol 6 (6) ◽  
pp. 517-526 ◽  
Author(s):  
Permender Rathee ◽  
Anjoo Kamboj ◽  
Shabir Sidhu
Keyword(s):  
Oral Bioavailability ◽  
Drug Loading ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Pharmacokinetic Interaction ◽  
Precipitation Method ◽  
Pharmacokinetic Studies ◽  
Average Particle

AbstractBackground:Piperine helps in the improvement of bioavailability through pharmacokinetic interaction by modulating metabolism when administered with other drugs. Nisoldipine is a substrate for cytochrome P4503A4 enzymes. The study was undertaken to assess the influence of piperine on the pharmacokinetics and pharmacodynamics of nisoldipine nanoparticles in rats.Methods:Optimization studies of nanoparticles were performed using Taguchi L9 orthogonal array, and the nanoparticles were formulated by the precipitation method. The influence of piperine and nanoparticles was evaluated by means of in vivo kinetic and dynamic studies by oral administration in rats.Results:The entrapment efficiency, drug loading, ζ potential, and average particle size of optimized nisoldipine-piperine nanoparticles was 89.77±1.06%, 13.6±0.56%, −26.5 mV, and 132±7.21 nm, respectively. The in vitro release in 0.1 n HCl and 6.8 pH phosphate buffer was 96.9±0.48% and 98.3±0.26%, respectively. Pharmacokinetic studies showed a 4.9-fold increase in oral bioavailability and a >28.376±1.32% reduction in systemic blood pressure by using nanoparticles as compared to control (nisoldipine suspension) in Wistar rats.Conclusion:The results revealed that piperine being an inhibitor of cytochrome P4503A4 enzymes enhanced the bioavailability of nisoldipine by 4.9-fold in nanoparticles.

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 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 PCL/PHBV Microparticles as Innovative Carriers for Oral Controlled Release of Manidipine Dihydrochloride

2014 ◽  
Vol 2014 ◽  
pp. 1-10 ◽  
Author(s):  
Fernanda Malaquias Barboza ◽  
Willian Moreira Machado ◽  
Luiz Renato Olchanheski Junior ◽  
Josiane Padilha de Paula ◽  
Sônia Faria Zawadzki ◽  
...  
Keyword(s):  
Controlled Release ◽  
Animal Studies ◽  
Average Particle Size ◽  
Spherical Shape ◽  
Average Particle ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Chemically Modified ◽  
Diffraction Patterns

Microparticles of poly(ε-caprolactone) (PCL) and poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) containing manidipine dihydrochloride (MAN) were successfully prepared by the simple emulsion/solvent evaporation method. All formulations showed loading efficiency rates greater than 80% and average particle size less than 8 μm. Formulations had spherical shape with smooth and porous surface for PCL and PHBV, respectively. According to Fourier-transform infrared spectroscopy, initial components were not chemically modified during microencapsulation. X-ray diffraction patterns and differential scanning calorimetry demonstrated that this process led to drug amorphization.In vitrodissolution studies showed that all microparticles prolonged MAN release, mainly which one obtained using PCL that contained 5% of drug loaded (PCL-M5). Animal studies demonstrated that formulationPCL-M5was able to keep the variation of mean arterial pressure after phenylephrine administration up to 24 hours. These data confirmed the sustained antihypertensive effect of the investigated microparticles. Results provided an experimental basis for using formulationPCL-M5as a feasible carrier for oral controlled release of MAN intended for treating high blood pressure.

scholarly journals In-Vitro Cytotoxicity and Anticancer Drug Release Behavior of Methionine - Coated Magnetite Nanoparticles As Carriers.

2021 ◽  
Author(s):  
Faten Eshrati Yeganeh ◽  
Amir Eshrati Yeganeh ◽  
Bahareh Farasati Far ◽  
Iman Akbarzadeh ◽  
Sameer Quazi ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Amino Acid ◽  
Drug Release ◽  
Drug Loading ◽  
Average Particle Size ◽  
Mcf10a Cell ◽  
Core Shell ◽  
Average Particle ◽  
Release Behavior

Abstract An innovative and customized drug delivery system for in vitro cancer treatment has been developed successfully by a simple one-step method. A CoFe2O4@Methionine core-shell nanoparticle was prepared by the reflux assay, in which amino acid on the surface makes the ferrite biocompatible, enhances the chemical stability of the compound, and increases the drug loading capacity. The synthesized nanoparticles were evaluated using SEM, TEM, FTIR, and VSM, while XRD and TGA analysis verified the presence of a coating amino acid on the surface of CoFe2O4. The appearance of a new peak for C≡N in the FTIR spectrum validates the synthesis of a letrozole-loaded carrier. Both uncoated CoFe2O4 and methionine-coated CoFe2O4 nanoparticles behave super-paramagnetically at room temperature, with saturation values of 46 emu/g and 16.8 emu/g, respectively. SEM and TEM were used to characterize the morphology and size of samples, revealing that the average particle size was around 28–29 nm. The loading of Letrozole and the effect of pH (5, 7.4) on the release behavior of the carrier were studied. The result of the drug release in pH (5) was about 88% higher than pH (7.4). Also, the preparation has been evaluated for determining its cytotoxicity using MCF-7, MDA-MB-231, and MCF10A cell lines as an in vitro model, and the results of in vitro experiments showed that CoFe2O4@Methionine could significantly reduce cancer in the cell model. These results demonstrate that core-shell nanoparticles were prepared that are biocompatible and have potential use as drug delivery.

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 Bioadhesive Matrix Tablets Loaded with Lipophilic Nanoparticles as Vehicles for Drugs for Periodontitis Treatment: Development and Characterization

Polymers ◽  
2019 ◽  
Vol 11 (11) ◽  
pp. 1801 ◽  
Author(s):  
Denise Murgia ◽  
Giuseppe Angellotti ◽  
Fabio D’Agostino ◽  
Viviana De Caro
Keyword(s):  
Periodontal Diseases ◽  
Drug Loading ◽  
Average Particle Size ◽  
Spherical Shape ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Average Particle ◽  
Glycyrrhetic Acid ◽  
Nanoparticle Dispersion ◽  
Periodontal Pathogens

Periodontitis treatment is usually focused on the reduction or eradication of periodontal pathogens using antibiotics against anaerobic bacteria, such as metronidazole (MTR). Moreover, recently the correlation between periodontal diseases and overexpression of reactive oxygen species (ROS) led to the introduction of antioxidant biomolecules in therapy. In this work, bioadhesive buccal tablets, consisting of a hydrophilic matrix loaded with metronidazole and lipophilic nanoparticles as a vehicle of curcumin, were developed. Curcumin (CUR)-loaded nanostructured lipid carriers (NLC) were prepared using glycyrrhetic acid, hexadecanol, isopropyl palmitate and Tween®80 as a surfactant. As method, homogenization followed by high-frequency sonication was used. After dialysis, CUR-NLC dispersion was evaluated in terms of drug loading (DL, 2.2% w/w) and drug recovery (DR, 88% w/w). NLC, characterized by dynamic light scattering and scanning electron microscopy (SEM), exhibited a spherical shape, an average particle size of 121.6 nm and PDI and PZ values considered optimal for a colloidal nanoparticle dispersion indicating good stability of the system. Subsequently, a hydrophilic sponge was obtained by lyophilization of a gel based on trehalose, Natrosol and PVP-K90, loaded with CUR-NLC and MTR. By compression of the sponge, matrix tablets were obtained and characterized in term of porosity, swelling index, mucoadhesion and drugs release. The ability of the matrix tablets to release CUR and MTR when applied on buccal mucosa and the aptitude of actives to penetrate and/or permeate the tissue were evaluated. The data demonstrate the ability of NLC to promote the penetration of CUR into the lipophilic domains of the mucosal membrane, while MTR can penetrate and permeate the mucosal tissue, where it can perform a loco-regional antibacterial activity. These results strongly support the possibility of using this novel matrix tablet for delivering MTR together with CUR for topical treatment of periodontal diseases.

scholarly journals Preparation and Characterization of Chitosan Coated PLGA Nanoparticles of Resveratrol: Improved Stability, Antioxidant and Apoptotic Activities in H1299 Lung Cancer Cells

Coatings ◽  
2020 ◽  
Vol 10 (5) ◽  
pp. 439 ◽  
Author(s):  
Hibah M. Aldawsari ◽  
Nabil A. Alhakamy ◽  
Rayees Padder ◽  
Mohammad Husain ◽  
Shadab Md
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Average Particle Size ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Aqueous Solubility ◽  
Plga Nanoparticles ◽  
Steady Increase ◽  
Average Particle

Resveratrol (RES) is a polyphenolic compound which has shown beneficial pharmacological effects such as anti-inflammatory, antioxidant, and anti-cancer effects. However, poor aqueous solubility, bioavailability, and low stability are the major limitations to the clinical application of RES. Therefore, in the present study, chitosan (CS) coated PLGA nanoparticles of RES (CS-RES-PLGA NPs) was developed, characterized and its anticancer activity was evaluated in the H1299 lung carcinoma cell line. The effects of the increase in CS coating and cryoprotectant concentration on particle size, polydispersity index (PDI) and zeta potential (ZP) were determined. The particle size, PDI, ZP and entrapment efficiency of the optimized CS-RES-PLGA NPs were found to be 341.56 ± 7.90 nm, 0.117 ± 0.01, 26.88 ± 2.69 mV and 75.13% ± 1.02% respectively. The average particle size and ZP showed a steady increase with an increase in CS concentration. The increase in positive zeta potential is evident for higher CS concentrations. The effect of trehalose as cryoprotectant on average particle size was decreased significantly (p < 0.05) when it was increased from 1%−5% w/v. TEM and SEM showed uniform particle distribution with a smooth surface and spherical shape. The CS coating provides modulation of in vitro drug release and showed a sustained release pattern. The stability of RES loaded PLGA NPs was improved by CS coating. CS-coated NPs showed greater cytotoxicity and apoptotic activities compared to free RES. The CS coated NPs had a higher antioxidant effect than the free RES. Therefore, CS coated PLGA NPs could be a potential nanocarrier of RES to improve drug solubility, entrapment, sustain release, stability and therapeutic application.

scholarly journals Preparation of progesterone nanoparticles and evaluation of its effect on the capacitation of Bovine spermatozoa used in the in Vitro Fertilization

2018 ◽  
Vol 9 (4) ◽  
pp. 125
Author(s):  
Saber Abd-Allah ◽  
Mai Ralan ◽  
Hanaa Suliman ◽  
Tamer Essam ◽  
Heba F Salem
Keyword(s):  
Average Particle Size ◽  
Spherical Shape ◽  
Aqueous Solubility ◽  
Average Particle ◽  
Sperm Capacitation ◽  
Vitro Fertilization ◽  
Transmission Electron ◽  
Bovine Spermatozoa ◽  
Sperm Functions

<p class="Default">Progesterone (P) has been reported to affect several sperm functions especially capacitation and acrosome reaction<strong>. </strong>The main problem of (P) is its low aqueous solubility. So formulation of progesterone nanoparticles (PN) will enhance its solubility. This study was conducted to produce nanosized progesterone (NP) and assess its biocompatibility. Therefore, nine progesterone formulations were prepared and characterized. Data analysis revealed only one formula of P<span lang="EN-GB"> showed nanosized particle (1-100 nm) with an average particle size (</span><span>95±</span><span lang="EN-GB">5 nm), and spherical shape as seen by Transmission Electron Microscope(TEM).</span> Motile spermatozoa were separated from frozen-thawed semen by a swim-up procedure and capacitated in IVF-TALP medium with NP or P or without treatments (control) and incubated for 3h at 38°C and evaluated every 1 hour (h) interval. Ovarian oocytes were matured and fertilized <em>in vitro </em>with frozen-thawed bull sperm capacitated in vitro<strong> </strong>with NP or P or control (without NP, P) and incubated at 39C in 5% CO2 incubator for 24h and then examined for evidence of fertilization. In conclusion, this study demonstrates that nanosized progesterone is highly efficient for sperm capacitation. In addition to the use of nanosized progesterone in sperm capacitation produces more fertilized oocytes than the progesterone after<em> In Vitro </em>Fertilization (IVF).</p>

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.

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