Praziquantel-loaded solid lipid nanoparticles: Production, physicochemical characterization, release profile, cytotoxicity and in vitro activity against Schistosoma mansoni

2020 ◽  
Vol 58 ◽  
pp. 101784 ◽  
Author(s):  
Luciana Nalone Andrade ◽  
Conrado Marques ◽  
Thallysson Barbosa ◽  
Rafael Santos ◽  
Marco Vinícius Chaud ◽  
...  
Keyword(s):  
Schistosoma Mansoni ◽  
Solid Lipid Nanoparticles ◽  
Physicochemical Characterization ◽  
Lipid Nanoparticles ◽  
Release Profile ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Solid Lipid

Development and In Vitro Characterization of Paclitaxel Loaded Solid Lipid Nanoparticles

2019 ◽  
Vol 9 (1) ◽  
pp. 76-85 ◽  
Author(s):  
R. Nithya ◽  
K. Siram ◽  
R. Hariprasad ◽  
H. Rahman
Keyword(s):  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Release Profile ◽  
Mcf7 Cells ◽  
Solid Lipid ◽  
Cancerous Cells ◽  
Vitro Release

Background: Paclitaxel (PTX) is a potent anticancer drug which is highly effective against several cancers. Solid lipid nanoparticles (SLNs) loaded with anticancer drugs can enhance its toxicity against tumor cells at low concentrations. Objective: To develop and characterize SLNs of PTX (PSLN) to enhance its toxicity against cancerous cells. Method: The solubility of PTX was screened in various lipids. Solid lipid nanoparticles of PTX (PSLN) were developed by hot homogenization method using Cutina HR and Gelucire 44/14 as lipid carriers and Solutol HS 15 as a surfactant. PSLNs were characterized for size, morphology, zeta potential, entrapment efficiency, physical state of the drug and in vitro release profile in 7.4 pH phosphate buffer saline (PBS). The ability of PTX to enhance toxicity towards cancerous cells was tested by performing cytoxicity assay in MCF7 cell line. Results: Solubility studies of PTX in lipids indicated better solubility when Cutina HR and Gelucire 44/14 were used. PSLNs were found to possess a neutral zeta potential with a size range of 155.4 ± 10.7 nm to 641.9 ± 4.2 nm. In vitro release studies showed a sustained release profile for PSLN over a period of 48 hours. SLNs loaded with PTX were found to be more toxic in killing MCF7 cells at a lower concentration than the free PTX.

Glyceryl Monostearate Based Solid Lipid Nanoparticles for Controlled Delivery of Docetaxel

2021 ◽  
Vol 18 ◽  
Author(s):  
Nadia Rai ◽  
Asadullah Madni ◽  
Amir Faisal ◽  
Talha Jamshaid ◽  
Muhammad Imran Khan ◽  
...  
Keyword(s):  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Release Profile ◽  
Controlled Delivery ◽  
Melting Transition ◽  
Glyceryl Monostearate ◽  
Tem Analysis ◽  
Solid Lipid

Background: Background: Solid Lipid Nanoparticles (SLNs) is the drug delivery systems that has the capability to improve drug release at the desired tumor site. The aim of present study was to develop Glyceryl Monostearate (GMS) based SLNs for the controlled delivery of docetaxel. Method: Hot Melt Encapsulation (HME) method was employed avoiding the use of organic solvents and therefore, regarded as green synthesis of SLNs. Results: Optimized DTX-SLNs showed desirable size (100 nm) with low poly dispersity index and excellent entrapment efficiency. Surface charge confirmed the stability of formulation. Transmission Electron Microscope (TEM) analysis showed spherical shaped particles and Fourier Transform Infrared Microscopy (FTIR) revealed compatibility among formulation excipients. Differential Scanning Calorimeter (DSC) analysis revealed that melting transition peak of optimized formulation was also greater than 40°C indicating that SLNs would be solid at body temperature. In-vitro release profile (68% in 24 hours) revealed the controlled release profile of DTX-SLNs indicating lipophilic docetaxel drug was entrapped inside high melting point lipid core. Cytotoxicity study revealed that blank SLNs were found to be biocompatible while dose dependent cytotoxicity was shown by DTX-SLNs. Conclusion: These studies suggest that DTX-SLNs have potential for controlled delivery of docetaxel and improved therapeutic outcome.

scholarly journals Praziquantel-Solid Lipid Nanoparticles Produced by Supercritical Carbon Dioxide Extraction: Physicochemical Characterization, Release Profile, and Cytotoxicity

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3881 ◽  
Author(s):  
Andrade ◽  
Oliveira ◽  
Chaud ◽  
Alves ◽  
Nery ◽  
...  
Keyword(s):  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Encapsulation Efficiency ◽  
Chemical Interaction ◽  
Scale Up ◽  
Physicochemical Characterization ◽  
Lipid Nanoparticles ◽  
Release Profile ◽  
Solid Lipid ◽  
Cetyl Palmitate

Solid lipid nanoparticles (SLNs) can be produced by various methods, but most of them are difficult to scale up. Supercritical fluid (SCF) is an important tool to produce micro/nanoparticles with a narrow size distribution and high encapsulation efficiency. The aim of this work was to produce cetyl palmitate SLNs using SCF to be loaded with praziquantel (PZQ) as an insoluble model drug. The mean particle size (nm), polydispersity index (PdI), zeta potential, and encapsulation efficiency (EE) were determined on the freshly prepared samples, which were also subject of Differential Scanning Calorimetry (DSC), Fourier-Transform Infrared Spectroscopy (FTIR), drug release profile, and in vitro cytotoxicity analyses. PZQ-SLN exhibited a mean size of ~25 nm, PdI ~ 0.5, zeta potential ~−28 mV, and EE 88.37%. The DSC analysis demonstrated that SCF reduced the crystallinity of cetyl palmitate and favored the loading of PZQ into the lipid matrices. No chemical interaction between the PZQ and cetyl palmitate was revealed by FTIR analysis, while the release or PZQ from SLN followed the Weibull model. PZQ-SLN showed low cytotoxicity against fibroblasts cell lines. This study demonstrates that SCF may be a suitable scale-up procedure for the production of SLN, which have shown to be an appropriate carrier for PZQ.

ASSESSMENT OF IN VITRO NARINGENIN RELEASE FROM SOLID LIPID NANOPARTICLES AND KINETIC MODEL PROFILING: APPLIED ULTRAVIOLET-VISIBLE SPECTROPHOTOMETER

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (11) ◽  
pp. 46-57
Author(s):  
A. K Sahu ◽  
◽  
G. K. Sahu ◽  
D K Dash ◽  
S. P Mishra ◽  
...  
Keyword(s):  
Standard Deviation ◽  
Relative Standard Deviation ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Lipid Nanoparticles ◽  
Release Profile ◽  
Solid Lipid ◽  
Relative Standard

A new, simple, specific, rapid, precise, highly accurate, reproducible and cost effective Ultraviolet-Visible spectrophotometric method was developed and validated, according to the International Harmonization Guidelines, for the determination of naringenin from solid lipid nanoparticles. Absorption maximum of Naringenin was found to be at 287.49nm in methanol. The linearity range was found to be 5-25μg/mL with high correlation coefficient value of 0.999. The detection and quantification limits were found to be 0.1879μg/mL and 0.5694μg/mL, respectively. This method was shown to be specific, selective, precise at the intra-day (relative standard deviation less than 0.7046%) and inter-day (relative standard deviation less than 1.5424%) level and accurate with recoveries between 98.77-100.43% (relative standard deviation less than 0.3924%). Method robustness observation indicates that method was robust. The suitability of the method for naringenin quantifications was assessed by the determination of entrapment parameters and by studying the naringenin release profile from SLNs. High entrapment efficiency (91.922 ± 0.717%) and drug loading (3.506 ± 0.027%) were observed. Kinetic models (zero order, first order, Higuchi, Hixson-Crowell, Korsmeyer-Peppas and Baker-Lonsdale) were used to fit the obtained release profile and to predict the in vivo performance of naringenin-loaded SLNs. An anomalous non-Fickian transport was found, which indicate a controlled drug release system.

In vitro evaluation of permeation, toxicity and effect of praziquantel-loaded solid lipid nanoparticles against Schistosoma mansoni as a strategy to improve efficacy of the schistosomiasis treatment

2014 ◽  
Vol 463 (1) ◽  
pp. 31-37 ◽  
Author(s):  
Ana Luiza Ribeiro de Souza ◽  
Tatiana Andreani ◽  
Rosimeire Nunes de Oliveira ◽  
Charlene Priscila Kiill ◽  
Fernanda Kolenyak dos Santos ◽  
...  
Keyword(s):  
Schistosoma Mansoni ◽  
Solid Lipid Nanoparticles ◽  
Lipid Nanoparticles ◽  
In Vitro Evaluation ◽  
Solid Lipid

Development of Solid Lipid Nanoparticles of Lamivudine for Brain Targeting

2009 ◽  
Vol 1 (1) ◽  
Author(s):  
Pravin Patil ◽  
Anil Sharma ◽  
Subhash Dadarwal ◽  
Vijay Sharma
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Rotation Speed ◽  
Lipid Nanoparticles ◽  
Brain Targeting ◽  
Brain Penetration ◽  
Solid Lipid ◽  
Diffusion Technique

The objective of present investigation was to enhance brain penetration of Lamivudine, one of the most widely used drugs for the treatment of AIDS. This was achieved through incorporating the drug into solid lipid nanoparticles (SLN) prepared by using emulsion solvent diffusion technique. The formulations were characterized for surface morphology, size and size distribution, percent drug entrapment and drug release. The optimum rotation speed, resulting into better drug entrapment and percent yield, was in the range of 1000-1250 r/min. In vitro cumulative % drug release from optimized SLN formulation was found 40-50 % in PBS (pH-7.4) and SGF (pH-1.2) respectively for 10 h. After 24 h more than 65 % of the drug was released from all formulations in both mediums meeting the requirement for drug delivery for prolong period of time.

Preparation, Characterization and In-vitro release of Piroxicam-loaded Solid Lipid Nanoparticles

2010 ◽  
Vol 3 (3) ◽  
pp. 1136-1146
Author(s):  
V K Verma ◽  
Ram A
Keyword(s):  
Electron Microscopy ◽  
Particle Size ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Diffusion Method ◽  
Solid Lipid ◽  
Vitro Release

 Solid lipid nanoparticles (SLNs) of piroxicam where produced by solvent emulsification diffusion method in a solvent saturated system. The SLNs where composed of tripamitin lipid, polyvinyl alcohol (PVAL) stabilizer, and solvent ethyl acetate. All the formulation were subjected to particle size analysis, zeta potential, drug entrapment efficiency, percent drug loading determination and in-vitro release studies. The SLNs formed were nano-size range with maximum entrapment efficiency. Formulation with 435nm in particle size and 85% drug entrapment was subjected to scanning electron microscopy (SEM) and transmission electron microscopy (TEM) for surface morphology, differential scanning calorimetry (DSC) for thermal analysis and short term stability studies. SEM and TEM confirm that the SLNs are nanometric size and circular in shape. The drug release behavior from SLNs suspension exhibited biphasic pattern with an initial burst and prolong release over 24 h. 

Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

2020 ◽  
Vol 12 (2) ◽  
pp. 4474-4491
Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Tem Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

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