scholarly journals Formulation and Evaluation of Nanosuspension as an Alternative Approach for Solubility Enhancement of Simvastatin

2021 ◽  
Vol 71 (1) ◽  
Author(s):  
Mohini E. Shinde ◽  
Mitesh P. Sonawane ◽  
Avish D. Maru
Keyword(s):  
Particle Size ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Water Soluble ◽  
Average Particle ◽  
Particle Size Reduction ◽  
Drug Effectiveness ◽  
Saturation Solubility ◽  
Drug Content ◽  
Poorly Water Soluble

Solubility is an essential factor for drug effectiveness. Simvastatin is poorly water-soluble drug and its bioavailability is very low. Nanosuspension is one of those approach which can tremendously enhance the effective surface area of drug particles by reducing the particle size and there by increases the rate of dissolution and hence improve bioavailability. The main purpose of the present investigation was to increase the saturation solubility of simvastatin by preparation of nanosuspension. Nanosuspension of simvastatin were prepared by nanoprecipitation method using hydroxypropyl cellulose as stabilizer and sodium lauryl sulphate as surfactant. Prepared nanosuspension was evaluated for its particle size, total drug content, entrapment efficiency and saturation solubility study. On the basis of the evaluation, the best batch F8 formulation demonstrated highest drug content and entrapment efficiency with average particle size of 0.004µm. The saturation solubility studies show the solubility of the prepared nanosuspension has increased as compared to the pure drug due to the particle size reduction. The nanosuspension of simvastatin could be successfully prepared and can be concluded that the nanosuspension formulation is a promising approach to enhance the solubility. The nanoprecipitation is a simple and effective method to produce nano sized particles of poorly water-soluble drugs with enhance solubility.

scholarly journals BETAMETHASONE DIPROPIONATE GEL FOR TREATMENT OF LOCALIZED PLAQUE PSORIASIS

2017 ◽  
Vol 9 (8) ◽  
pp. 173 ◽  
Author(s):  
Sanaa El Gizaway ◽  
Maha Fadel ◽  
Basma Mourad ◽  
Fatma El-zahraa Abd Elnaby
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Betamethasone Dipropionate ◽  
Average Particle ◽  
Topical Formulation ◽  
Content Type ◽  
Drug Content

Objective: The main aim of this study was to design and characterise betamethasone di-propionate loaded transfersomes (BD-T); as a topical formulation for the treatment of localized plaque psoriasis.Methods: A full factorial design (23) was applied to study the effects of three independent variables: drug content, type of surfactants and surfactant contents on particle size (PS), entrapment efficiency (EE %), zeta potential (ZP), polydispersity index (PI) and drug release profiles. The optimized BD-T was formulated as a hydrogel using 5% sodium carboxymethyl cellulose. The gel was characterized for viscosity, drug content, in vitro drug release and stability. A comparative clinical study was performed on 20 patients with psoriasis to investigate the effect of BD-T gel and the marketed betamethasone dipropionate (BD) cream.Results: The optimized BD-T formulation containing 50 mg betamethasone dipropionate (BD) and 5 mg tween 80 showed spherical unilamellar vesicles with an average particle size of 242.80, % EE of 90.19%, ZP of-15.00 mV, PI of 0.407 and K0 of 4.290 mg/hr. The formulation showed good stability at 4 °C and 25 °C for 6 mo. The results revealed significant clinical improvement and a significant increase in safety and tolerability with BD-T gel compared with BD cream.Conclusion: As a conclusion, BD-T was found to be more effective, safe and tolerable for the treatment of psoriasis compared with the marketed product.

Development, Characterization and Evaluation of Ritonavir Nanosuspension Treatment of Antiretroviral Therapy

2021 ◽  
pp. 297-304
Author(s):  
Shital V. Sonawane ◽  
Avish D. Maru ◽  
Mitesh P. Sonawane
Keyword(s):  
Particle Size ◽  
Dissolution Rate ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Poloxamer 407 ◽  
Precipitation Method ◽  
Average Particle ◽  
Solubility Study ◽  
Drug Content ◽  
Antisolvent Precipitation

Oral nanosuspension of ritonavir was prepared by antisolvent precipitation method using various polymers such as Eudragit RS100, Poloxamer 407, SLS and Methanol.The effect of eudragit RS100 and poloxamer 407 used stabilizer and SLS is surfactant was investigated on particle size and distribution, drug content, entrapment efficiency was observed. Ritonavir is having low solubility and low permeability drug belonging to class-IV according to BCS. Drug-excipient compatibility and amorphous nature of ritonavir drug is prepared nanosuspension was confirmed by FTIR, DSC and Motic microscope studies, respectively. The nanosuspension was further evaluated for drug content, saturation solubility study and entrapment efficiency. The average particle size of ritonavir nanaosuspensions formulas was observed from 0.006 µm to 0.017 µm. The studied in the solubility and dissolution rate there are the increase solubility and dissolution rate of ritonavir nanosuspension.

Azithromycin nanosuspension preparation using evaporative precipitation into aqueous solution (EPAS) method and its comparative dissolution study

2020 ◽  
Vol 17 ◽  
Author(s):  
Mohammad Hossain Shariare ◽  
Tonmoy Kumar Mondal ◽  
Hani Alothaid ◽  
Md. Didaruzzaman Sohel ◽  
MD Wadud ◽  
...  
Keyword(s):  
Aqueous Solution ◽  
Particle Size ◽  
Dissolution Rate ◽  
Average Particle Size ◽  
Scale Up ◽  
Average Particle ◽  
Total Drug ◽  
Residual Solvent ◽  
Dissolution Study ◽  
Drug Content

Aim: EPAS (evaporative precipitation into aqueous solution) was used in the current studies to prepare azithromycin nanosuspensions and investigate the physicochemical characteristics for the nanosuspension batches with the aim of enhancing the dissolution rate of the nanopreparation to improve bioavailability. Methods: EPAS method used in this study for preparing azithromycin nanosuspension was achieved through developing an in-house instrumentation method. Particle size distribution was measured using Zetasizer Nano S without sample dilution. Dissolved azithromycin nanosuspensions were also compared with raw azithromycin powder and commercially available products. Total drug content of nanosuspension batches were measured using an Ultra-Performance Liquid Chromatography (UPLC) system with Photodiode Array (PDA) detector while residual solvent was measured using gas chromatography (GC). Results: The average particle size of azithromycin nanosuspension was 447.2 nm and total drug content was measured to be 97.81% upon recovery. Dissolution study data showed significant increase in dissolution rate for nanosuspension batch when compared to raw azithromycin and commercial version (microsuspension). The residual solvent found for azithromycin nanosuspension is 0.000098023 mg/ mL or 98.023 ppb. Conclusion: EPAS was successfully used to prepare azithromycin nanoparticles that exhibited significantly enhanced dissolution rate. Further studies are required to scale up the process and determine long term stability of the nanoparticles.

Synthesis and Characterization of Water-Soluble Monolayer-Protected Gold Nanoparticles

2011 ◽  
Vol 415-417 ◽  
pp. 617-620 ◽  
Author(s):  
Yan Su ◽  
Ying Yun Lin ◽  
Yu Li Fu ◽  
Fan Qian ◽  
Xiu Pei Yang ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Transmission Electron Microscopy ◽  
Particle Size ◽  
Gold Nanoparticles ◽  
Average Particle Size ◽  
Water Soluble ◽  
Synthesis And Characterization ◽  
Average Particle ◽  
Transmission Electron

Water-soluble gold nanoparticles (AuNPs) were prepared using 2-mercapto-4-methyl-5- thiazoleacetic acid (MMTA) as a stabilizing agent and sodium borohydride (NaBH4) as a reducing agent. The AuNPs product was analyzed by transmission electron microscopy (TEM), UV-vis absorption spectroscopy and Fourier transform infrared spectroscopy (FTIR). The TEM image shows that the particles were well-dispersed and their average particle size is about 5 nm. The UV-vis absorption and FTIR spectra confirm that the MMTA-AuNPs was stabilized by the carboxylate ions present on the surface of the AuNPs.

Synthesis of Nanostructured Magnetic Mixed-Oxide Ferrite Powders by Using A Novel Chemical Method

2002 ◽  
Vol 720 ◽  
Author(s):  
N N Ghosh
Keyword(s):  
Particle Size ◽  
Mixed Oxide ◽  
Chemical Method ◽  
Average Particle Size ◽  
Cost Effective ◽  
Water Soluble ◽  
Average Particle ◽  
Chemical Route ◽  
Water Soluble Polymer ◽  
Different Temperatures

AbstractIn the present investigation, an attempt has been made to establish a new chemical route for synthesis of the nanostructured mixed oxide ferrite powders. By using this chemical method a variety of ferrite powders having spinel structure and doped with Co, Ni, Mn, Zn etc has been prepared. In this method nitrate salts of the different metals were used as starting materials. The aqueous solutions of the metal nitrates were mixed according to the molar ration of the compositions. Then the mixtures were mixed with an aqueous solution of water soluble polymer (polyvinyl alcohol). This mixture after drying yield fluffy brown powders. These powders were then calcined at different temperatures ranging from 400 °C to 700 °C. Nanostructured powders were obtained from the thermal decomposition of the brown powders. The powders, prepared by calcinations at different temperatures, were characterized by using X-Ray diffraction analysis, IR spectroscopy, TGA/DTA, and TEM. It was observed that the average particle size of the powders are in nanometer scale with a narrow size distribution. The average particle size of the powders was increased with the increase of calcinations temperature.This chemical method has proved to provide a convenient process for the preparation of nanostructured ceramic powders at comparatively low temperatures and offers the potential of being a simple and cost-effective route.

scholarly journals Modeling of Miniemulsion Polymerization of Styrene with Macro-RAFT Agents to Theoretically Compare Slow Fragmentation, Ideal Exchange and Cross-Termination Cases

Polymers ◽  
2019 ◽  
Vol 11 (2) ◽  
pp. 320 ◽  
Author(s):  
Dries Devlaminck ◽  
Paul Van Steenberge ◽  
Marie-Françoise Reyniers ◽  
Dagmar D’hooge
Keyword(s):  
Particle Size ◽  
Average Particle Size ◽  
Miniemulsion Polymerization ◽  
Monomer Conversion ◽  
Water Soluble ◽  
Explicit Calculation ◽  
Average Particle ◽  
Intermediate Radical ◽  
Raft Agent ◽  
The Impact

A 5-dimensional Smith-Ewart based model is developed to understand differences for reversible addition-fragmentation chain transfer (RAFT) miniemulsion polymerization with theoretical agents mimicking cases of slow fragmentation, cross-termination, and ideal exchange while accounting for chain length and monomer conversion dependencies due to diffusional limitations. The focus is on styrene as a monomer, a water soluble initiator, and a macro-RAFT agent to avoid exit/entry of the RAFT leaving group radical. It is shown that with a too low RAFT fragmentation rate coefficient it is generally not afforded to consider zero-one kinetics (for the related intermediate radical type) and that with significant RAFT cross-termination the dead polymer product is dominantly originating from the RAFT intermediate radical. To allow the identification of the nature of the RAFT retardation it is recommended to experimentally investigate in the future the impact of the average particle size (dp) on both the monomer conversion profile and the average polymer properties for a sufficiently broad dp range, ideally including the bulk limit. With decreasing particle size both a slow RAFT fragmentation and a fast RAFT cross-termination result in a stronger segregation and thus rate acceleration. The particle size dependency is different, allowing further differentiation based on the variation of the dispersity and end-group functionality. Significant RAFT cross-termination is specifically associated with a strong dispersity increase at higher average particle sizes. Only with an ideal exchange it is afforded in the modeling to avoid the explicit calculation of the RAFT intermediate concentration evolution.

Synthesis and properties of novel self-crosslinked cationic fluorinated acrylic latex prepared with novel emulsified system

2016 ◽  
Vol 45 (4) ◽  
pp. 259-264
Author(s):  
Wen Li ◽  
Zhongbin Bao ◽  
Lijun Chen ◽  
Dongshun Deng
Keyword(s):  
Particle Size ◽  
Gemini Surfactants ◽  
Average Particle Size ◽  
Water Soluble ◽  
Average Particle ◽  
Mixed Surfactants ◽  
The Novel ◽  
Content Type ◽  
Acrylic Latex ◽  
Emulsion Polymerisation

Purpose At present, the conventional method of preparing cationic fluorinated acrylic latex is to emulsify copolymerised monomers with cationic surfactants. However, there has been a wide concern about using Gemini surfactants to prepare cationic polymer latex to improve its properties. The purpose of this paper was to focus on the synthesis of novel self-crosslinked cationic fluorinated acrylic latex (SCFAL), during which the copolymerised monomers were initiated with a water soluble azo initiator and emulsified with mixed surfactants of Gemini emulsifier and alkyl polyglycoside (APG). Design/methodology/approach The novel SCFAL was prepared successfully by the semi-continuous seeded emulsion polymerisation of butyl acrylate, methyl methacrylate, hexafluorobutyl methacrylate (HFMA) and hydroxy propyl methacrylate (HPMA) in aqueous medium. Findings The conversion is the maximum and the coagulation percentage the minimum when the amounts of emulsifier and initiator are 8 and 0.6 per cent, respectively. The average particle size of the latex is significantly reduced with the increase of the amount of emulsifiers used. However, the average particle size of the latex is increased with the increase of the amount of HPMA. The particle size of the latex is of a unimodal distribution, which means that the particle size was reasonably uniform. Contact angle is increased with the increase of the amount of the HFMA. Practical implications The novel SCFAL can be widely used as significant components in the field of coatings, leather, textile, paper, adhesives and so on. Originality/value SCFAL, which was emulsified with novel mixed surfactants of Gemini surfactant and APG, has been prepared successfully. Influences of amount of initiator, emulsifier, HPMA and HFMA on emulsion polymerisation and/or properties of novel latex are investigated in detail.

scholarly journals INVESTIGATION ON DISSOLUTION PATTERN AND MATHEMATICAL MODELING OF DRUG RELEASE OF QUERCETIN BY COMPLEXATION WITH CYCLODEXTRIN NANOSPONGES

2019 ◽  
pp. 260-264
Author(s):  
SOBITHARANI P ◽  
ANANDAM S ◽  
MOHAN VARMA M ◽  
VIJAYA RATNA J ◽  
SHAILAJA P
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Average Particle Size ◽  
Particle Size Analysis ◽  
Water Soluble ◽  
Size Analysis ◽  
Average Particle ◽  
Scattering Method ◽  
Release Pattern ◽  
Cyclodextrin Nanosponges

Objective: The main objective of this study was to investigate the release pattern of a poorly water-soluble drug quercetin (QU) by fabricating its cyclodextrin nanosponges. Methods: Characterization of the original QU powder and QU-loaded nanosponges was carried out by the Fourier-transformed infrared (FTIR) spectroscopy, transmission electron microscopy (TEM), and dissolution tester. The drug release pattern was subjected to various kinetic models. Results: FTIR studies confirmed the formation of inclusion complex of drug. The particle size analysis revealed that the average particle size measured by laser light scattering method is around 400–420 nm with low polydispersity index. The particle size distribution is unimodal and having a narrow range. A sufficiently high zeta potential indicates that the complexes would be stable and the tendency to agglomerate would be miniscule. TEM image revealed the porous nature of nanosponges. The dissolution of the QU nanosponges was significantly higher compared with the pure drug. Conclusion: From the kinetic study, it is apparent that the regression coefficient value closer to unity in case of Korsmeyer-Peppas model indicates that the drug release exponentially to the elapsed time. n value obtained from the Korsmeyer-Peppas plots, i.e., 0.9911 indicating non-Fickian (anomalous) transport ; thus, it projected that delivered its active ingredient by coupled diffusion and erosion.

scholarly journals Preparation and Characterization of Fenofibrate Microparticles with Surface-Active Additives: Application of a Supercritical Fluid-Assisted Spray-Drying Process

Pharmaceutics ◽  
2021 ◽  
Vol 13 (12) ◽  
pp. 2061
Author(s):  
Jeong-Soo Kim ◽  
Heejun Park ◽  
Eun-Sol Ha ◽  
Kyu-Tae Kang ◽  
Min-Soo Kim ◽  
...  
Keyword(s):  
Particle Size ◽  
Surface Layer ◽  
Dissolution Rate ◽  
Spray Drying ◽  
Supercritical Fluid ◽  
Water Soluble ◽  
Size Reduction ◽  
Particle Size Reduction ◽  
Surface Active ◽  
Poorly Water Soluble

In this study, supercritical fluid-assisted spray-drying (SA-SD) was applied to achieve the micronization of fenofibrate particles possessing surface-active additives, such as d-α-tocopheryl polyethylene glycol 1000 succinate (TPGS), sucrose mono palmitate (Sucroester 15), and polyoxyethylene 52 stearate (Myrj 52), to improve the pharmacokinetic and pharmacodynamic properties of fenofibrate. For comparison, the same formulation was prepared using a spray-drying (SD) process, and then both methods were compared. The SA-SD process resulted in a significantly smaller mean particle size (approximately 2 μm) compared to that of unprocessed fenofibrate (approximately 20 μm) and SD-processed particles (approximately 40 μm). There was no significant difference in the effect on the particle size reduction among the selected surface-active additives. The microcomposite particles prepared with surface-active additives using SA-SD exhibited remarkable enhancement in their dissolution rate due to the synergistic effect of comparably moderate wettability improvement and significant particle size reduction. In contrast, the SD samples with the surface-active additives exhibited a decrease in dissolution rate compared to that of the unprocessed fenofibrate due to the absence of particle size reduction, although wettability was greatly improved. The results of zeta potential and XPS analyses indicated that the surface-active additive coverage on the surface layer of the SD-processed particles with a better wettability was higher than that of the SA-SD-processed composite particles. Additionally, after rapid depletion of hydrophilic additives that were excessively distributed on the surfaces of SD-processed particles, the creation of a surface layer rich in poorly water-soluble fenofibrate resulted in a decrease in the dissolution rate. In contrast, the surface-active molecules were dispersed homogeneously throughout the particle matrix in the SA-SD-processed microparticles. Furthermore, improved pharmacokinetic and pharmacodynamic characteristics were observed for the SA-SD-processed fenofibrate microparticles compared to those for the SD-processed fenofibrate particles. Therefore, the SA-SD process incorporating surface-active additives can efficiently micronize poorly water-soluble drugs and optimize their physicochemical and biopharmaceutical characteristics.

scholarly journals Development and Evaluation of Floating Microspheres of Sumatriptan Succinate using Ethyl Cellulose and Mucilage Extracted from Vigna Mungo

2021 ◽  
pp. 24-36
Author(s):  
Nilesh S. Kulkarni ◽  
Mukta A. Kulkarni ◽  
Rahul H. Khiste ◽  
Mohini C. Upadhye ◽  
Shashikant N. Dhole
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Polymer Concentration ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Vigna Mungo ◽  
Average Particle ◽  
Sumatriptan Succinate

Aim: The present investigation is to formulate and evaluate gastroretentive floating microspheres for sumatriptan succinate. Gastric retention is widely used approach to retain dosage form in stomach and to enhance absorption of drugs. Methods: The gastroretentive floating microspheres was prepared by two different techniques as solvent evaporation and W/O/W multiple emulsion technique. Ethyl cellulose, HPMC K4M polymer and mucilage extracted from Vigna Mungo in various proportions were used for formulation of microspheres. Combination of ethyl acetate and acetone in different proportion was used as organic phase and the microspheres were characterized for particle size, shape, morphology, percentage yield, entrapment efficiency, drug loading, In-Vitro Floating/Buoyancy study, In-vitro Floating/Buoyancy study and release kinetics. Results: The average particle size of all batches was found in the range 100 to 210 μm and the entrapment efficiency of all formulations was found in the range of 17.46 % to 59.28 %.Total floating time for Sumatriptan succinate floating microspheres was observed more than 12 h. The In-Vitro drug release study was performed for all formulations showed drug release in controlled manner. Conclusion: The particle size was increased with increased polymer concentration and it showed that polymer concentration has an impact on the entrapment efficiency. Ethyl cellulose microspheres showed more entrapment and sustained delivery of sumatriptan Succinate than microspheres prepared by combination of Ethyl cellulose: HPMC K4M and Ethyl cellulose: Vigna mungo mucilage.

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