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 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.

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.

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 Formulation and Evaluation of A Nanoparticle Laden in Situ Gel System for Enhancing the Ocular Delivery of Ciprofloxacin

2021 ◽  
Vol 70 (2) ◽  
Author(s):  
Sourav Datta ◽  
Ratul Bhowmik ◽  
Ranajit Nath ◽  
Rajarshi Chakraborty ◽  
Apala Chakraborty
Keyword(s):  
Particle Size ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Topical Administration ◽  
Average Particle ◽  
Eye Drops ◽  
Physiological Factors ◽  
In Situ Gel ◽  
Gel System

The human eye can be a tricky issue for topical administration of the drugs due to its unique anatomical arrangements of surface tissue and corneal impermeability. Topical instillation of drugs in the form of eye drops is the major and well-accepted route of administration for the treatment of varied eye disorders. Conventional ophthalmic drug delivery systems often lead to poor bioavailability and thus reduced therapeutic response. Several new preparations are developed to enhance the contact time of the medicament on the surface of the eye. Successful results have been obtained in the form of inserts and collagen shields. However, these preparations have also some disadvantages, such as poor patient compliance, particularly in the case of elderly patients. These problems could be solved by using nanoparticles laden in situ gel-forming systems that exhibit phase transition from solution to gel. These nanoparticle in situ gel systems may be formulated as eye drops suitable for administration through instillation into the eye, which upon exposure to the eye, stimulated by various ocular physiological factors, converts to the gel phase. The advantage of those formulations is that unlike inserts and films they do not require complicated equipment for manufacture and that they are scalable without any difficulty. The objective of the present study was to prepare a pH-dependent nanoparticle-laden in situ gel system for Ciprofloxacin, to prolong the release of the drug into the ocular compartment. No incompatibility was found between the drug and the excipients. Nanoparticles were developed using the nanoprecipitation technique. Eudragit RL 100 was used as the polymer. While the in situ gel solution was formulated using chitosan as polymer. The Ciprofloxacin nanoparticles were measured for particle size and the average particle size was ranged from 295.3-458.7 nm. Entrapment efficiency ranged from 13.83% to 6.29%. Nanoparticleladen in situ gels had the pH of the formulati

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.

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.

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.

scholarly journals IN SITU GEL AS PLATFORM FOR KETOCONAZOLE SLOW RELEASE DOSAGE FORM

2018 ◽  
Vol 10 (5) ◽  
pp. 76
Author(s):  
Methaq Hamad Sabar ◽  
Iman Sabah Jaafar ◽  
Masar Basim Mohsin Mohamed
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
High Viscosity ◽  
In Situ Gel ◽  
Alginate Concentration

Objective: The aim of this study was to formulate ketoconazole (keto) as oral floating in situ gel to slow the release of keto in the stomach.Methods: Sodium alginate (Na alginate) was used as a primary polymer in the preparation of the in situ gel and was supported by the following polymers: guar gum (GG), hydroxypropyl methylcellulose (HPMC) K4M, K15M and carbapol 940 as viscosity enhancing agents. As a consequence, and to complete the gelation process of above formulations was by adding the calcium carbonate (CaCO3). The in situ gels were investigated by the following tests: floating lag time, floating duration, viscosity, drug content, in vitro gelling studies and in vitro release study.Results: The study showed that the faster release was obtained with F1 which contained Na alginate alone. Additionally, reduction in Na alginate concentration resulted in significant increase in drug release. It was also noted that the increase in GG (viscosity enhancing polymer) concentration resulted in non-significant decrease in percent drug release and the reduction in CaCO3 concentration led to significant increase in drug release. Moreover, the release of drug was also affected by grade of viscosity enhancing polymer, the faster release was observed with the formula which contained a polymer of low viscosity (HPMC K4M) and an opposite result was with the high viscosity polymer (HPMCK15M).Conclusion: This study showed the formulation of Na alginate with GG and CaCO3, led to gain floating in situ gel and a sustained release of keto. 

scholarly journals Effect of soil textural characteristics on longitudinal dispersion in saturated porous media

2021 ◽  
Vol 69 (2) ◽  
pp. 161-170
Author(s):  
Mojtaba G. Mahmoodlu ◽  
Amir Raoof ◽  
Martinus Th. van Genuchten
Keyword(s):  
Particle Size ◽  
Dispersion Coefficient ◽  
Average Particle Size ◽  
Longitudinal Dispersion ◽  
Average Particle ◽  
Sand Sample ◽  
Average Pore ◽  
Advection Dispersion ◽  
Strong Positive Relationship

Abstract This study focuses on the effects of soil textural heterogeneity on longitudinal dispersion under saturation conditions. A series of solute transport experiments were carried out using saturated soil columns packed with two filter sands and two mixtures of these sands, having d50 values of 95, 324, 402, and 480 µm, subjected to four different steady flow rates. Values of the dispersion coefficient (D) were estimated from observed in-situ distributions of calcium chlo-ride, injected as a short nonreactive tracer pulse, at four different locations (11, 18, 25, 36 cm). Analyses of the observed distributions in terms of the standard advection-dispersion equation (ADE) showed that D increased nonlinearly with travel distance and higher Peclet numbers+. The dispersion coefficient of sand sample S1 with its largest average particle size (d 50) was more affected by the average pore-water velocity than sample S4 having the smallest d 50. Results revealed that for a constant velocity, D values of sample S1 were much higher than those of sample S4, which had the smallest d 50. A correlation matrix of parameters controlling the dispersion coefficient showed a relatively strong positive relationship between D and the Peclet number. In contrast, almost no correlation was evident between D and porosity as well as grain size. The results obtained with the four sandy matrices were consistent and proved that the dispersion coefficient depends mainly on the particle size.

scholarly journals Water-Dispersible Phytosterol Nanoparticles: Preparation, Characterization, and in vitro Digestion

2022 ◽  
Vol 8 ◽  
Author(s):  
Ao Li ◽  
Aixia Zhu ◽  
Di Kong ◽  
Chunwei Wang ◽  
Shiping Liu ◽  
...  
Keyword(s):  
Particle Size ◽  
Soybean Lecithin ◽  
Average Particle Size ◽  
Soy Protein Isolate ◽  
In Vitro Digestion ◽  
Bimodal Distribution ◽  
Average Particle ◽  
Food Ingredients ◽  
The Impact

For improving solubility and bioaccessibility of phytosterols (PS), phytosterol nanoparticles (PNPs) were prepared by emulsification–evaporation combined high-pressure homogenization method. The organic phase was formed with the dissolved PS and soybean lecithin (SL) in anhydrous ethanol, then mixed with soy protein isolate (SPI) solution, and homogenized into nanoparticles, followed by the evaporation of ethanol. The optimum fabrication conditions were determined as PS (1%, w/v): SL of 1:4, SPI content of 0.75% (w/v), and ethanol volume of 16 ml. PNPs were characterized to have average particle size 93.35 nm, polydispersity index (PDI) 0.179, zeta potential −29.3 mV, and encapsulation efficiency (EE) 97.3%. The impact of temperature, pH, and ionic strength on the stability of fabricated PNPs was determined. After 3-h in vitro digestion, the bioaccessibility of PS in nanoparticles reached 70.8%, significantly higher than the 18.2% of raw PS. Upon freeze-drying, the particle size of PNPs increased to 199.1 nm, resulting in a bimodal distribution. The solubility of PS in water could reach up to 2.122 mg/ml, ~155 times higher than that of raw PS. Therefore, this study contributes to the development of functional PS-food ingredients.

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