Development of Ligand Incorporated Chitosan Nanoparticles for the Selective Delivery of 5-Fluorouracil to Colon

2011 ◽  
Vol 197-198 ◽  
pp. 238-241 ◽  
Author(s):  
Pu Wang Li ◽  
Zheng Peng ◽  
F.H. She ◽  
L.X. Kong
Keyword(s):  
Particle Size ◽  
Drug Delivery Systems ◽  
Average Particle Size ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Active Targeting ◽  
Average Particle ◽  
Selective Delivery ◽  
Vitro Release

Drug delivery systems with active targeting ligand provide improved therapeutic efficiency due to the selectivity towards tumor cells. In this paper we prepared drug loaded nanoparticles (NPs) using folate (FA) incorporated chitosan (FA-CS) based on ionic gelation technology. FA-CS NPs were spherical in shape with an average particle size of 100 nm, while 5-fluorouracil (5-FU) loaded NPs became less circular with average particle size of 100-500 nm. NPs made from FA-CS conjugates exhibited improved capability to encapsulate hydrophilic 5-FU. It was found 5-FU distributed in FA-CS NPs in solid solution state. In vitro release results demonstrated the release of 5-FU from FA-CS NPs was more controllable as compared to that of CS NPs.

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 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.

ROSUVASTATIN CALCIUM LOADED CHITOSAN NANOPARTICLES: PREPARATION EVALUATION AND IN VITRO RELEASE STUDIES

2020 ◽  
pp. 95-102
Author(s):  
SUVARNA G. BHOKARE ◽  
RAJENDRA P. MARATHE
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Sustained Release ◽  
Sodium Tripolyphosphate ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Particle Diameter ◽  
Vitro Release ◽  
Rosuvastatin Calcium

Objective: The objective of the present study was to develop sustained release biodegradable polymeric nanoparticles of rosuvastatin calcium. Methods: Nanoparticles were prepared by modified ionotropic gelation method using 3² full factorial designs. From the preliminary trials, the constraints for independent variables X1 (concentration. of chitosan) and X2 (concentration. of sodium tripolyphosphate) have been fixed. Factors included concentration of chitosan and sodium tripolyphosphate, have been examined to investigate effect on particle size, encapsulation efficiency, zeta potential, % release, scanning electron microscopy, Fourier transfer infrared study and X-ray diffraction and release study of rosuvastatin calcium nanoparticles. 0 Results: The prepared nanoparticles were white, free-flowing and spherical in shape. The infrared spectra showed stable character of rosuvastatin calcium in the drug-loaded nanoparticles and revealed the absence of drug polymer interactions. The chitosan nanoparticles have a particle diameter ranging approximately 114.5±3.61 to 724±.2.51 nm and a zeta potential-13.12 to-52.63 mV. The in vitro release behavior from all the drug loaded batches were found to follow first order and provided sustained release over a period of 10 h. The Zeta potential of all the batches were in the range of-13.12 to-52.63 mv. The release profiles of all batches were very well fitted by Korsmeyer Peppas model. Conclusion: The best-fit release kinetics was achieved with Korsmeyer peppas model. The release of rosuvastatin calcium was influenced by the drug to polymer ratio and particle size. These results indicate that rosuvastatin calcium nanoparticles could be effective in sustaining drug release for a prolonged period.

scholarly journals Preparation, characterization, and in vitro evaluation of amphiphilic peptide P12 and P12-DOX nanomicelles as antitumor drug carriers

2020 ◽  
Vol 10 ◽  
pp. 184798042091151 ◽  
Author(s):  
Ping Song ◽  
Wuchen Du ◽  
Wanzhen Li ◽  
Longbao Zhu ◽  
Weiwei Zhang ◽  
...  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Phase ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Drug Carriers ◽  
Average Particle ◽  
Polymer Micelles ◽  
Amphiphilic Peptide

Polymerized polypeptide nanomicelles have attracted much attention as novel drug carriers because of their good biocompatibility and degradability. To prepare doxorubicin (DOX)-loaded nanomicelles, an amphiphilic peptide, FFHFFH-KKGRGD (P12), was synthesized by solid-phase synthesis, and the physicochemical and drug-release properties, as well as the cytotoxicity of the nanomicelles, were evaluated in vitro. The P12-DOX polymer micelles were prepared by dialysis. The morphology and particle size were characterized by transmission electron microscopy and dynamic light scattering. The critical micelle concentration (CMC) of the polymer was determined by the probe method, and the drug-release characteristics of the micelles were studied by dynamic dialysis. The cytotoxicity and uptake of the P12-DOX micelles were evaluated against mouse breast cancer cells (4T1) and human umbilical vein endothelial cells. The peptide polymer micelles containing DOX were uniformly sized and had a spherical core–shell structure with an average particle size of 128.6 nm. The CMC of the polymer was low (0.0357 mg/mL). The in vitro release of DOX from the micelles is slow and is consistent with first-order kinetics. The copolymer micelles of the P12 polypeptide and DOX can be used as nanoscale spherical carriers of hydrophobic drugs and have broad applicability.

scholarly journals Design of a Reversible Cholinesterase Inhibitor Mamentine HCL Nanogel: Formulation and In-vitro Evaluation

2021 ◽  
pp. 352-359
Author(s):  
Subhasri Mohapatra ◽  
Sourabh Jain ◽  
Karunakar Shukla
Keyword(s):  
Particle Size ◽  
Cholinesterase Inhibitor ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Storage Period ◽  
Spherical Particles ◽  
Average Particle ◽  
In Situ Gel

Memantine hydrochloride is a is a reversible cholinesterase inhibitor used in the treatment of Alzheimer’s disease, low-moderate affinity, uncompetitive n-methyl-d-aspartate (NMDA) receptor antagonist, with strong voltage dependency and rapid blocking/unblocking kinetics. The present study was explore the potential of thermosensitive nanogel of mamentine loaded nanoparticle. In situ gel choosing due to restrict unwanted exposure in blood and other healthy tissues, thus eliminate hemolytic side effects of the drug and offer easy administration in vivo. Nanoparticle prepared by ionic gelation method and further the dried nanoparticle incorporates with in situ gel.  The in situ gel prepared by cold method using the solutions of Poloxamer-188 and Carbopol-934. The Transmission electron microscopy showed the spherical particles  with  smooth surface which was in conformity  with the SEM and Zetasizer  data for particle size. The pH of the formulations was found to be satisfactory and was in the range of 6.8±0.039 -7.4±0.053 and also mucoadhesive strength was show in table. The mucoadhesive strength of all formulations was varies from 2398±0.0004 to 4945±0.0002 dynes/cm2. In-vitro diffusion study of the in situ gel (N1-N8) was performed using modified Franz diffusion cell with dialysis membrane in phosphate buffer pH 6.5 for a period of 24 hours. The in vitro release study were fitted into various kinetic models viz zero order, first order, higuchi model and korsmeyer peppas equation. Stability studies for optimized formulations were carried out at 4.0 ± 0.5°C and 37 ± 0.5ºC for a period of four weeks. There was no significant variation found in physical appearance, average particle size and % drug content of the in situ nanogel N2. No visible changes in the appearance of the gel formulation were observed at the end of the storage period.

scholarly journals Formulation and Evaluation of Ketoconazole Nanosponge gel

2021 ◽  
Vol 23 (2) ◽  
Author(s):  
Vijay R Chakote ◽  
◽  
Ms.Deepali R. Wagh ◽  
Mr. Rahul S. Waghmare ◽  
Umesh T. Jadhao ◽  
...  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Average Particle ◽  
Sustained Drug Release ◽  
Percentage Yield ◽  
Viscosity Study ◽  
Cross Linker

Ketoconazole Nanosponges were prepared by using Hyper cross linked β-cyclodextrin method by using different concentration of cross-linker. Diphenyl carbonate was used as the cross linking polymer. Nanosponge formulations were prepared by using β-CD: cross linker ratios of 1:15, 1:10, 1:5 and 1:3.Thepreparednanosponges were evaluated for percentage yield, incorporation efficiency, particle size, drug polymer compatibility, scanning electron microscopy andin-vitrodrugrelease.SEM studies confirmed their porous structure with number of nano channels. The FTIR spectra showed stable character of Ketoconazole in mixture of polymers and revealed the absence of drug polymer interactions. DSC study revealed that drug was involved in complexation with nanosponges. The average particle size of Ketoconazole nanoparticles was found to be in the range of 78.81± 0.20 nm to336.02 ± 0.124nm.The drug release from nanosponges was found to extended upto 8hr. 82 to 92%.The nano sponges were formulated into gel using Carbopol 940Batches G1 to G4 were prepared by incorporating nanosponges equivalent to 6%w/w of ketoconazole in different polymer concentrations respectively and evaluated for Percent drug content, Viscosity study, Spreadability study, In vitro diffusion studies. Nanosponge gel G1 showed the optimum pH, viscosity, Spread ability and In vitro release. Drug diffusion from the nanosponge loaded gel formulations was show sustained rate. A sustained release topical drug delivery of Ketoconazole developed as a nanosponge loaded gel offers solubilizing matrix for the drug, served as a local depot for sustained drug release and provided a rate limiting matrix barrier for modulation of drug release.

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.

scholarly journals Neuroprotective and Antioxidant Effect of Naringenin-Loaded Nanoparticles for Nose-to-Brain Delivery

2019 ◽  
Vol 9 (10) ◽  
pp. 275 ◽  
Author(s):  
Shadab Md ◽  
Nabil A. Alhakamy ◽  
Hibah M. Aldawsari ◽  
Hani Zakaria Asfour
Keyword(s):  
Cellular Uptake ◽  
Neurodegenerative Disorder ◽  
Average Particle Size ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Antioxidant Effect ◽  
Neuroprotective Activity ◽  
Average Particle ◽  
Brain Delivery

Parkinson’s disease (PD) is a neurodegenerative disorder resulting in a decreased nigrostriatal availability of dopamine. Oxidative stress is one factor contributing to PD. Naringenin (NAR), a flavonoid, is a potent antioxidant shown to be beneficial in experimental PD. The clinical development of NAR has been hampered due to its low bioavailability resulting from gastrointestinal degradation, inefficient permeability, and low aqueous solubility. The objective of the present research was to formulate and characterize naringenin-loaded chitosan nanoparticles (NAR NPs) for nose-to-brain delivery. The cellular uptake, cytotoxicity, and neuroprotective effects of NAR NPs were determined using the SH-SY5Y cell line in vitro. NAR NPs were prepared using the ionic gelation method and characterized by zetasizer, transmission electron microscopy (TEM), and field emission microscopy (FESEM). The average particle size, polydispersity index (PDI), zeta potential, entrapment efficiency, and 24 h in vitro release profile were 87.6 ± 8.47 nm, 0.31 ± 0.04, 15.36 ± 2.05 mV, 91.12 ± 2.99%, and 54.80 ± 4.22%, respectively. The percentage NAR permeation through nasal mucosa from NPs was found to be 67.90 ± 0.72%. Cellular uptake of prepared NPs was confirmed by fluorescence microscopy. Neuroprotective activity of NAR NPs was evaluated through viability assays and by estimating reactive oxygen species (ROS) levels. NAR NPs showed enhanced neuroprotective ability and antioxidant effect against 6-OHDA-induced neurotoxicity in SH-SY5Y cells. However, animal studies are necessary to establish the potential of NAR NPs to be an effective carrier for the treatment of PD for nose-to-brain delivery.

scholarly journals DEVELOPMENT AND IN-VITRO CHARACTERISATION OF CHITOSAN LOADED PACLITAXEL NANOPARTICLE

2016 ◽  
Vol 9 (9) ◽  
pp. 145 ◽  
Author(s):  
Tumpa Sarkar ◽  
Abdul Baquee Ahmed
Keyword(s):  
Particle Size ◽  
High Speed ◽  
Chitosan Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Ionic Crosslinking ◽  
Glutaraldehyde Solution ◽  
Drug Entrapment Efficiency ◽  
Vitro Release

ABSTRACTObjectives: To meet the above aim the following objectives are undertaken: (1) Preparation of paclitaxel (PTX) loaded nanoparticles by differenttechniques, (2) In-vitro evaluations of the drug loaded nanoparticles and selection of optimized batch.Methods: PTX loaded chitosan nanoparticles were prepared by Ionic-crosslinking technique. In this technique, chitosan was dissolved in 0.25%v/vacetic acid solution. To this above solution 0.84%v/v, glutaraldehyde solution was added dropwise under high-speed homogenizer at 17000 rpm for1 hr.Result: Particle size of prepared nanoparticle formulations was found to be 345.175±5.66-815.125±8.355 nm with low PDI between 0.456. Themaximum entrapment of drug was found to be 88.57±2.533% with formulation F5. In-vitro release studies of the F5 formulation showed 57.8±1.735%release of drug after 24 hrs.Conclusion: The prepared nanoparticles were evaluated for its particle size, zeta potential, drug entrapment efficiency, in-vitro drug release study,and surface morphology studies by scanning electron microscopy. The results of Fourier transform infrared studies of 1:1 physical mixture of drug andexcipients confirmed the absence of incompatibility. Thus, the study concludes that PTX loaded nanoparticles were developed successfully by ioniccrosslinking method, which is expected to enhance the oral bioavailability of PTX.Keywords: Paclitaxel, Nanoparticles, Chitosan, Ionic-crosslinking, In-vitro release.

Indinavir-Loaded Nanostructured Lipid Carriers to Brain Drug Delivery: Optimization, Characterization and Neuropharmacokinetic Evaluation

2019 ◽  
Vol 16 (4) ◽  
pp. 341-354 ◽  
Author(s):  
Mohammad Nasiri ◽  
Amir Azadi ◽  
Mohammad Reza Saghatchi Zanjani ◽  
Mehrdad Hamidi
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Zeta Potential ◽  
Average Particle Size ◽  
In Vitro Release ◽  
Free Drug ◽  
Average Particle ◽  
The Brain

Purpose: As an anti-retroviral Protease Inhibitor (PI), Indinavir (IDV) is part of the regimen known as Highly Active Anti-Retroviral Therapy (HAART) widely used for Human Immunodeficiency Virus (HIV) infection. The drug efficiency in treatment of the brain manifestations of HIV is, however, limited which is mainly due to the efflux by P-glycoprotein (P-gp) expressed at the Blood-Brain Barrier (BBB). Methods: To overcome the BBB obstacle, NLCs were used in this study as carriers for IDV, which were optimized through two steps: a “one-factor-at-a-time” screening followed by a systematic multiobjective optimization. Spherical smooth-surfaced Nanoparticles (NPs), average particle size of 161.02±4.8 nm, Poly-Dispersity Index (PDI) of 0.293±0.07, zeta potential of -40.62±2.21 mV, entrapment efficiency of 93±1.58%, and loading capacity of 9.15±0.15% were obtained after optimization which were, collectively, appropriate in terms of the objective of this study. Result: The surface of the optimized NPs was, then, modified with human Transferrin (TR) to improve the drug delivery. The particle size, zeta potential, and PDI of the TR-modified NLCs were 185.29±6.7nm, -28.68±3.37 mV, and 0.247±0.06, respectively. The in vitro release of IDV molecules from the NPs was best fitted to the Weibull model indicating hybrid diffusion/erosion behavior. Conclusion: As the major in vivo findings, compared to the free drug, the NLCs and TR-NLCs displayed significantly higher and augmented concentrations in the brain. In this case, NLC and TR-NLC were 6.5- and 32.75-fold in their values of the brain uptake clearance compared to free drug.

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