scholarly journals Formulation, optimization and characterization of nanostructured lipid carrier of nitrofurantoin

2020 ◽  
pp. 227-237
Author(s):  
Nilam Goswami ◽  
Rakesh P. Patel
Keyword(s):  
Particle Size ◽  
High Speed ◽  
Entrapment Efficiency ◽  
Narrow Particle Size Distribution ◽  
Nanostructured Lipid Carrier ◽  
Characteristic Peak ◽  
Hot Plate ◽  
Glyceryl Monostearate ◽  
Mean Particle Size

Nitrofurantoin is effective against many urinary tract pathogens. It acts as bacteriostatic and/or bactericidal by inhibiting DNA-RNA protein& cell wall synthesis. Nanostructured Lipid Carriers (NLCs) of NFT was prepared by Hot Homogenization Process. Glyceryl Monostearate and Miglyol 812 were heated at 80ºC temperature on hot plate. In the melted lipid, drug was added with continuous stirring at high speed homogenization. Formulation NLC12B has % Entrapment efficiency 89.1 ± 0.5, PDI 0.11 ± 0.01 and mean particle size 237 ± 7nm represents narrow particle size distribution.  Spherical feature of NLCs with better uniformity without aggregation of Nitrofurantoin loaded NLC was confirmed by TEM. Moreover, efficient miscibility of drug in lipids was confirmed by the absence of intense and characteristic peak of NFT in XRPD. After 6 month storage at 2-8°C there was no significant changes in the PDI as well as mean particle size.

Optimization of Solid Lipid Nanoparticles of Ezetimibe in Combination with Simvastatin Using Quality by Design (QbD)

2020 ◽  
Vol 10 (4) ◽  
pp. 404-418
Author(s):  
Kruti Borderwala ◽  
Ganesh Swain ◽  
Namrata Mange ◽  
Jaimini Gandhi ◽  
Manisha Lalan ◽  
...  
Keyword(s):  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
High Speed ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Water Soluble ◽  
Lipid Matrix ◽  
Solid Lipid ◽  
32 Factorial Design ◽  
Full Factorial Experimental Design

Background: The objective of this study was to develop solid lipid nanoparticles (SLNs) of poorly water soluble anti-hyperlipidemic drugs-Ezetimibe in combination with Simvastatin. Methods: This study describes a 32 full factorial experimental design to optimize the formulation of drug loaded lipid nanoparticles (SLN) by the high speed homogenization technique. The independent variables amount of lipid (GMS) and amount of surfactant (Poloxamer 188) were studied at three levels and arranged in a 32 factorial design to study the influence on the response variables- particle size, % entrapment efficiency (%EE) and cumulative drug release (% CDR) at 24 h. Results: The particle size, % EE and % CDR at 24 h for the 9 batches (B1 to B9) showed a wide variation of 104.6-496.6 nm, 47.80-82.05% (Simvastatin); 48.60-84.23% (Ezetimibe) and 54.64-92.27% (Simvastatin); 43.8-97.1% (Ezetimibe), respectively. The responses of the design were analysed using Design Expert 10.0.2. (Stat-Ease, Inc, USA), and the analytical tools of software were used to draw response surface plots. From the statistical analysis of data, polynomial equations were generated. Optimized formulation showed particle size of 169.5 nm, % EE of 75.43% (Simvastatin); 79.10% (Ezetimibe) and 74.13% (Simvastatin); 77.11% (Ezetimibe) %CDR after 24 h. Thermal analysis of prepared solid lipid nanoparticles gave indication of solubilisation of drugs within lipid matrix. Conclusion: Fourier Transformation Infrared Spectroscopy (FTIR) showed the absence of new bands for loaded solid lipid nanoparticles indicating no interaction between drugs and lipid matrix and being only dissolved in it. Electron microscope of transmission techniques indicated sphere form of prepared solid lipid nanoparticles with smooth surface with size approximately around 100 nm.

scholarly journals Ex-vivo Ex-Vivo Absorption Study of a Novel Dabigatran Etexilate Loaded Nanostructured Lipid Carrier Using Non-Everted Intestinal Sac Model

2019 ◽  
Vol 28 (2) ◽  
pp. 37-45
Author(s):  
Haithem N Abed ◽  
Ahmed A. Hussein
Keyword(s):  
Particle Size ◽  
Oleic Acid ◽  
Zeta Potential ◽  
Oral Absorption ◽  
Ex Vivo ◽  
Dabigatran Etexilate ◽  
Entrapment Efficiency ◽  
Nanostructured Lipid Carrier ◽  
Loading Capacity ◽  
Intestinal Permeation

Abstract The purpose of our study was to develop Dabigatran Etexilate loaded nanostructured lipid carriers (DE-NLCs) using Glyceryl monostearate and Oleic acid as lipid matrix, and to estimate the potential of the developed delivery system to improve oral absorption of low bioavailability drug, different Oleic acid ratios effect on particle size, zeta potential, entrapment efficiency and loading capacity were studied, the optimized DE-NLCs shows a particle size within the nanorange, the zeta potential (ZP) was 33.81±0.73mV with drug entrapment efficiency (EE%) of  92.42±2.31% and a loading capacity (DL%) of 7.69±0.17%. about 92% of drug was released in 24hr in a controlled manner, the ex-vivo intestinal permeation study using the non-everted sac model shows four folds increment in the permeation of DE-NLCs compared to dabigatran etexilate suspension (DE-S).

scholarly journals PREPARATION, CHARACTERIZATION, AND FORMULATION OF SOLID LIPID NANOPARTICLES LOTION FROM MULBERRY ROOTS (MORUS ALBA L.)

2020 ◽  
pp. 182-186
Author(s):  
MUHAMAD WILDAN NUGRAHA ◽  
RADITYA ISWANDANA ◽  
MAHDI JUFRI
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
High Speed ◽  
Tween 80 ◽  
Lipid Nanoparticles ◽  
Morus Alba ◽  
Glyceryl Monostearate ◽  
Optimum Result ◽  
Solid Lipid

Objective: Tween 80 has been used as a solvent for the extraction of phenolic compounds because this surfactant has both hydrophilic and hydrophobicproperties. Solid lipid nanoparticles (SLNs) have been developed to improve penetration through the skin layer. We investigated the efficacy of usingthe microwave-assisted micellar extraction (MAME) approach for extracting oxyresveratrol from Morus alba roots and also to develop an SLN lotion.Methods: The M. alba roots were extracted with Tween 80 in a microwave for 18 min, and the extract was used to develop SLN with differentconcentrations of glyceryl monostearate. The SLNs from M. alba root extracts were prepared by a high-speed homogenization technique (25,000 rpmfor 15 min). The SLNs produced were characterized as per particle size, polydispersity index (PDI), and zeta potential. The SLNs with the bestcharacteristics were used to formulate a lotion using a high-pressure homogenizer.Results: Extraction using MAME showed improved extraction efficiency. The oxyresveratrol concentration from the extract was 2.77%. The SLN with2.5% glyceryl monostearate showed the optimum result, with a particle size of 130.20 nm, a PDI of 0.278, and a zeta potential of −21.8 mV. The SLNlotion exhibited a particle size of 285.9 nm and a PDI of 0.360. The SLN lotion also had good penetration, with a flux of 4.70 μg cm−2/h.Conclusion: MAME is an efficient method for extracting oxyresveratrol from M. alba roots. The SLN with 2.5% glyceryl monostearate exhibited theoptimum characteristics, and the SLN lotion showed good characteristics, including skin penetration.

scholarly journals ENHANCEMENT OF THERAPEUTIC WINDOW OF METFORMIN HYDROCHLORIDE BY FABRICATION OF MICROSPHERES COMPRISING POLYMERIC INCULCATION WITH SEMI-SYNTHETIC AND SYNTHETIC POLYMERS BY IMPLEMENTATION OF BOX-BEHNKEN DESIGN

2021 ◽  
pp. 257-264
Author(s):  
MD AAMER QUAZI ◽  
NAZIA KHANAM
Keyword(s):  
Particle Size ◽  
Controlled Release ◽  
Ex Vivo ◽  
Hydroxypropyl Methylcellulose ◽  
Entrapment Efficiency ◽  
Synthetic Polymers ◽  
Therapeutic Window ◽  
Metformin Hydrochloride ◽  
Box Behnken Design ◽  
Mean Particle Size

Objective: Innovative enhancement of therapeutic window of Metformin hydrochloride (MFH) and bioavailability through mucoadhesive microspheres by polymeric inculcation of hydroxypropyl methylcellulose K4M grade (HPMC K4M), hydroxypropyl methylcellulose K100M grade (HPMC K100M) and Kollidon SR grade (KS). Methods: Controlled release system was developed by incorporating semi-synthetic and synthetic polymers by modified solvent evaporation technique. Fabrication of mucoadhesive microspheres was designed by the implementation of experimental designs to obtain most optimum concentration of selected factors. The method was optimized by Box Behnken design (BBD) with selected factors as concentrations of semi-synthetic and synthetic polymer with stirring speed influence for the obtained responses that were mean particle size (Y1) entrapment efficiency of drug (Y2) and percent mucoadhesion (Y3). Microspheres were characterized for particle size, entrapment efficiency of drug, ex-vivo mucoadhesion study, in vitro study, Fourier transform infrared spectroscopy (FTIR), x-ray diffraction (XRD) detection and H1 Nuclear magnetic resonance (NMR) quantification for optimized formulation. Results: Implementation of response surface method software for BBD yielded stable microspheres with mean particle size 274 µm, entrapment efficiency of drug 85.07% and percent mucoadhesion 67.03% for optimized formulation F5. Conclusion: Bridging of MFH with the highly innovative combination of semi-synthetic and synthetic polymers yielded stable, cost-effective microspheres with improved bioavailability with controlled-release effect as till date no literature is available that provide information with selected polymeric combination and analytical characterization.

scholarly journals Effect of Lipid Composition on Nanostructured Lipid Carrier (NLC) on Ubiquinone Effectiveness as an Anti-aging Cosmetics

2018 ◽  
Vol 8 (3) ◽  
Author(s):  
Tamara Gusti Ebtavanny ◽  
Widji Soeratri ◽  
Noorma Rosita
Keyword(s):  
Surface Tension ◽  
Particle Size ◽  
Lipid Composition ◽  
Entrapment Efficiency ◽  
Rapid Onset ◽  
Homogenization Method ◽  
Nanostructured Lipid Carrier ◽  
Onset Of Action ◽  
Solid Lipid ◽  
Ph Range

The purpose of this research is to determine the optimum composition of solid lipid and liquid lipid in order to increase the penetration and effectiveness of Q10 as antioxidant in anti-aging cosmetics. Solid lipid and liquid lipid used in this study were cetyl palmitate and caprylic, which were combined to four (4) different ratios, namely 10:0; 9:1; 7:3 and 5:5. NLC Q10 in this study was produced by high shear homogenization method at 3400 rpm for 5 cycles and at 24000 for 1 cycle. The fourth formula was evaluated in term of characteristics, penetration and effectiveness. From the pH test , it was known that all formulas met the skin pH range (4.0-6.0). For the particle size test , all formulas (NLC 1 - NLC 4) were in the range from 269.13 to 354.77 nm with NLC 3 (7: 3) had the smallest particle size. The results of viscosity and surface tension test were also consistent with the theory, where the addition of liquid lipid reduced viscosity and surface tension of the system. The entrapment efficiency (EE) demonstrated the EE of NLC 1: 22.24%; NLC 2: 24.71%; NLC 3: 58.21% and NLC 4:36.94%. The penetration test showed all systems were able to penetrate the dermis layer at the 5th hour. NLC 3 (7:3) had more rapid onset, while the NLC Q10 with the ratio of lipid 9:1, had slower onset of action but can penetrate farther than the other NLC Q10 system. The result of Q10 effectiveness test showed NLC 2 (9:1) has lowest total macrophage (23.33) and very dense collagen observation (score : 4). From this research, it can be concluded that NLC 2 (9:1) had the most optimal lipid composition to increase the penetration and effectiveness of Q10 as an antioxidant in anti-aging cosmetics.

Preparation and characterization of natural quercetin-based Mongolia Medicine SenDeng-4 nanoemulsion (N-QUE-NE) and its antibacterial activity..

2020 ◽  
Vol 18 ◽  
Author(s):  
Yanfang Zhang ◽  
Rina Du ◽  
Pengwei Zhao ◽  
Sha Lu ◽  
Rina Wu ◽  
...  
Keyword(s):  
Particle Size ◽  
Antibacterial Activity ◽  
Zeta Potential ◽  
High Speed ◽  
Antibacterial Effect ◽  
Average Particle Size ◽  
Antagonistic Effect ◽  
Dilution Method ◽  
Average Particle

Background: Quercetin is the main active ingredient of Xanthoceras sorbifolia Bunge. Traditional compatibility theory of traditional Chinese medicine has typically reported a synergistic interaction among multiple components, while the synergistic effects of nanoemulsion have not been fully clarified. Objective: To study preparation and characterization of quercetin-based Mongolia Medicine Sendeng-4 nanoemulsion (NQUE-NE) and its antibacterial activity and mechanisms. Methods: The morphology of the nanoemulsion was observed by transmission electron microscopy (TEM), and the zeta potential, polydispersity index (PDI), and particle size distribution were determined by the nanometer particle size analyze. The stability of nanoemulsion was investigated by light test, high speed centrifugal test and storage experiment at different temperature. The combined bacteriostatic effect of N-QUE-NE was studied in vitro by double-dilution method and checkerboard dilution method. Results: The appearance of N-QUE-NE was pale yellow, clear and transparent. The nanoemulsion particles were spherical and uniformly distributed under TEM. The PDI was 0.052, the average particle size was 19.6nm, and the Zeta potential was -0.2mV. When quercetin nanoemulsion (QUE-NE) was used in combination with tannin nanoemulsion (TAN-NE) and toosendanin nanoemulsion (TOO-NE), it exhibited a synergistic antibacterial effect. However, the combination of QUE-NE and geniposide nanoemulsion (GEN-NE) exhibited an antagonistic effect. It was revealed that the antibacterial effect was in order of quercetin-tannin-toosendanin nanoemulsion (QUE-TAN-TOO-NE) ＞ quercetin-tannin nanoemulsion (QUE-TANNE) ＞ QUE-NE ＞ quercetin-tannin-toosendanin-geniposide nanoemulsion (QUE-TAN-TOO-GEN-NE). Conclusion: This study explored the preparation and efficacy of N-QUE-NE, and the results showed that quercetin, tannin and toosendanin had satisfactory synergistic antibacterial effects. The antagonistic effect of quercetin and geniposide in nanoemulsion indicated that it is not beneficial to the antibacterial effect of Sendeng-4, and further research needs to be conducted to clarify its antibacterial effect.

Casuarina equisetifoliaExtract Loaded Phytosomes: Optimization, Characterization andIn vivoEvaluation of Antidiabetic and Antihyperlipidemic Activities in Wistar Rats

2019 ◽  
Vol 9 (2) ◽  
pp. 116-133 ◽  
Author(s):  
Anjana Rani ◽  
Sunil Kumar ◽  
Roop K. Khar
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Therapeutic Efficacy ◽  
Entrapment Efficiency ◽  
Herbal Extract ◽  
Casuarina Equisetifolia ◽  
Novel Drug

Background:Herbal extracts have brilliant in-vitro activity but less in-vivo action in light of their macromolecular size and poor lipid solubility bringing about poor absorption and low bioavailability. These issues can be corrected by designing novel drug delivery systems. Phytosomes provide better absorption and bioavailability when compared to conventional herbal extract.Objective:This paper deals with the preparation, optimization and characterization of Phytosome of plant extract and in vivo assessment of antidiabetic and antihyperlipidemic activity for improved therapeutic efficacy having sufficient stability.Methods:Preliminary distinctive strategies were utilized to get ready Phytosome and antisolvent precipitation method was chosen. The formulation was guided by a full factorial design to study the effect of Independent variable on various dependent variables and resulted in an optimised product. Response contour plots were generated for each response factor to predict a phytosomal composition that yields phytosome formulation having least particle size and maximum entrapment efficiency.Results:Mean particle size, entrapment efficiency and Span value were found to be 295 ± 0.53nm, 82.43 ± 1.65% and 0.34 ± 0.14 respectively. Zeta potential was found to be 19.35mv, indicating the formation of stable formulation. In vitro release study described that the drug release follows the Korsmeyer- Peppas kinetic model. The results proved that Phytosomes of Casuarina equisetifolia extract exhibited more antidiabetic potential and antihyperlipidemic properties as compared to crude Casuarina extract.Conclusion:Phytosomes of Casuarina equestifolia extract was successfully formulated having good entrapment efficiency and physico-chemical characterization of the optimized product, confirming the formation of stable formulation. In vivo antidiabetic activity confirmed better potential of the optimised formulation. Consequently, it has been presumed that Phytosomes of Casuarina equisetifolia extract serve as a useful novel drug delivery system and provide more therapeutic efficacy than conventional plant extracts.

Preparation of Metal Nanosuspensions by High-Pressure DC-Sputtering on Running Liquids

1996 ◽  
Vol 457 ◽  
Author(s):  
M. Wagener ◽  
B. S. Murty ◽  
B. Günther
Keyword(s):  
Particle Size ◽  
High Pressure ◽  
Particle Size Distribution ◽  
Pressure Range ◽  
Narrow Particle Size Distribution ◽  
Descriptive Model ◽  
Mean Particle Size ◽  
Dc Sputtering ◽  
The Mean ◽  
Argon Sputtering

ABSTRACTA modified VERL-process (Vacuum evaporation on running liquids) employing high pressure magnetron sputtering has been used for the preparation of suspensions with metal nanoparticles. The method has been tested for Ag- and Fe-suspensions by varying the pressure of the Argon sputtering atmosphere in the range of 1 to 30 Pa. A narrow particle size distribution with a mean particle size ranging from 5–18 nm has been found. The mean particle size increases with increasing Argon pressure in the pressure range under investigation. A descriptive model for the process of particle formation as a function of sputtering gas pressure is given.

Fabrication and characterization of nanostructured lipid carrier system for effective delivery of poorly water-soluble drug quetiapine fumarate

2021 ◽  
pp. 6235-6244
Author(s):  
Deepak Patil ◽  
Seema Pattewar ◽  
Sarvesh Palival ◽  
Gargi Patil ◽  
Swapnil Sharma
Keyword(s):  
Entrapment Efficiency ◽  
Water Soluble ◽  
Nanostructured Lipid Carrier ◽  
Quetiapine Fumarate ◽  
Water Soluble Drug ◽  
Effective Delivery ◽  
Capmul Mcm ◽  
Central Composite ◽  
Poorly Water Soluble Drug

The aim of present study is to investigate the potential of nanostructured lipid carriers (NLCs) in improving the oral bioavailability of quetiapine fumarate, a second-generation antipsychotic drug. Quetiapine Fumarate (QF) loaded NLC were prepared by hot homogenization followed by an ultrasonication method. Response surface methodology - central composite design (CCD) was used to systemically examine the influence of concentration of capmul MCM EP, concentration of poloxamer 188 and concentration of egg lecithin on particle size (PS) and % entrapment efficiency (% EE) and to optimize the NLC formulation. The CCD consists of three factored design with five levels, plus and minus alpha (axial points), plus and minus 1 (factorial points) and the centre point. A mathematical relationship between variables was created by using Design Expert software Version 12. The statistical evaluations revealed that three independent variables were the important factors that affected the PS and % EE of QF loaded NLC. The best fitted mathematical model was linear and quadratic for PS and % EE respectively. The optimized formulations found with 218.1±0.14nm of PS and 93±0.16% of % EE. Results illustrated the superiority of developed QF loaded NLC formulation as a stable drug delivery system, providing better bioavailability with the possibility of better treatment for psychological disorders.

Preparation and Characterization of Broad-Spectrum Sunscreens Loaded Nanostructured Lipid Carrier

2013 ◽  
Vol 669 ◽  
pp. 67-71
Author(s):  
Yan Ling Chen ◽  
Qiang Xia
Keyword(s):  
Particle Size ◽  
Physical State ◽  
Retention Rate ◽  
Nanostructured Lipid Carrier ◽  
High Pressure Homogenization ◽  
Spectrophotometric Detection ◽  
Ultraviolet Absorbance ◽  
Organic Uv Filters

A comprehensive photoprotective formulation was developed to enhance photoprotection ,compared to a conventional nanoemulsion ,having the concentration of two new molecular sunscreens, namely Diethylamino hydyoxybenzoyl hexyl benzoate(Uvinul ® A Plus) and Ethylhexyl triazone(Uvinul® T 150). In the present paper, the sunscreen mixture was incorporated into nanostructured lipid carriers (NLCs). After the production by hot high pressure homogenization, the NLC were analyzed in terms of particle size, physical state, particle shape, ultraviolet absorbance and stability. The particle size for all NLC was around 100-900 nm after production. The determination of 2 organic UV filters was performed by HPLC with UV spectrophotometric detection. The loading capacities for molecular sunscreens was up to 30%. In the sunlight, the retention rate of Uvinul ® A Plus and Uvinul ® T150 was still up to 80% after three months .

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